Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
90469674 336352 10 None 3467 3 Rat 10.7 pEC50 = 10.7 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 945 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4468523 336352 10 None 3467 3 Rat 10.7 pEC50 = 10.7 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 945 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
5311065 484177 30 None 218 4 Rat 10.5 pEC50 = 10.5 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
817 484177 30 None 218 4 Rat 10.5 pEC50 = 10.5 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
CHEMBL1429 484177 30 None 218 4 Rat 10.5 pEC50 = 10.5 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
DB00035 484177 30 None 218 4 Rat 10.5 pEC50 = 10.5 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
44419025 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/j.ejmech.2024.116733
44419026 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/j.ejmech.2024.116733
74992363 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/j.ejmech.2024.116733
CHEMBL221436 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/j.ejmech.2024.116733
CHEMBL435323 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/j.ejmech.2024.116733
CHEMBL6015151 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/j.ejmech.2024.116733
44419025 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
44419026 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
74992363 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL221436 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL435323 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL6015151 175267 18 None 218 3 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
146681949 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
2168 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
2810 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
644077 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
CHEMBL373742 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
DB00067 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
P01185 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
P01186 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
P35455 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
118476355 347940 5 None 5011 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1044 17 10 12 0.3 CCN(CC)C(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4539370 347940 5 None 5011 3 Rat 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant rat V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1044 17 10 12 0.3 CCN(CC)C(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
146681949 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
2168 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
2810 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
644077 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
CHEMBL373742 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
DB00067 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
P01185 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
P01186 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
P35455 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm200278m
146681949 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
2168 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
2810 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
644077 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
CHEMBL373742 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
DB00067 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
P01185 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
P01186 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
P35455 8624 35 None -7 5 Human 10.3 pEC50 = 10.3 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2005.10.107
155523986 335455 0 None 724 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4454891 335455 0 None 724 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
118476338 347488 0 None 2290 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4528032 347488 0 None 2290 3 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
118476361 347817 0 None 363 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1034 16 11 13 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4536454 347817 0 None 363 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1034 16 11 13 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
118476360 346637 0 None 2691 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4532363 346637 0 None 2691 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
155535667 336586 0 None 562 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1116 18 11 14 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4472007 336586 0 None 562 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1116 18 11 14 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
118476369 334749 0 None 3388 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 885 13 9 12 -0.4 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCN)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4444891 334749 0 None 3388 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 885 13 9 12 -0.4 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCN)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
118476336 335751 0 None 630 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1016 16 11 12 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4459424 335751 0 None 630 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1016 16 11 12 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
5311065 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1016/j.ejmech.2024.116733
817 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1016/j.ejmech.2024.116733
CHEMBL1429 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1016/j.ejmech.2024.116733
DB00035 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human vasopressin V2a receptorAgonist activity at human vasopressin V2a receptor
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1016/j.ejmech.2024.116733
132095331 349239 0 None 645 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4571464 349239 0 None 645 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
5311065 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
817 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
CHEMBL1429 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
DB00035 484177 30 None -218 4 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.9b00132
118476346 348563 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1060 17 12 13 -0.2 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4555263 348563 0 None 588 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1060 17 12 13 -0.2 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
118476341 335229 0 None 40 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
137554056 335229 0 None 40 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4451692 335229 0 None 40 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL6007190 335229 0 None 40 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
118476359 335947 0 None 524 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1026 16 12 12 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4462616 335947 0 None 524 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1026 16 12 12 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
155513872 334365 0 None 331 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1128 18 11 13 0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
CHEMBL4439313 334365 0 None 331 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1128 18 11 13 0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.9b00132
118476344 347475 0 None None None Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1034 16 11 13 -0.2 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4527761 347475 0 None None None Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1034 16 11 13 -0.2 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
155542670 347272 0 None None None Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 969 16 11 12 -0.7 CCc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1 10.1021/acs.jmedchem.9b00132
CHEMBL4521602 347272 0 None None None Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 969 16 11 12 -0.7 CCc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1 10.1021/acs.jmedchem.9b00132
CHEMBL1819440 484917 24 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1041 18 13 16 -4.7 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
DB13464 484917 24 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1041 18 13 16 -4.7 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
118476333 334181 0 None 1288 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1030 16 11 12 -0.1 CC(C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL4436571 334181 0 None 1288 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assayAgonist activity at recombinant human V2 receptor expressed in HEK293 cells measured after 5 hrs by cAMP response element driven luciferase reporter gene assay
ChEMBL 1030 16 11 12 -0.1 CC(C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/acs.jmedchem.9b00132
CHEMBL1819440 484917 24 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1041 18 13 16 -4.7 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
DB13464 484917 24 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1041 18 13 16 -4.7 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
3537 8682 25 None 45 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at V2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
5311500 8682 25 None 45 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at V2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL363910 8682 25 None 45 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at V2 receptor (unknown origin) by cAMP accumulation assayAgonist activity at V2 receptor (unknown origin) by cAMP accumulation assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
3537 8682 25 None 45 3 Human 9.1 pEC50 = 9.1 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
5311500 8682 25 None 45 3 Human 9.1 pEC50 = 9.1 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
CHEMBL363910 8682 25 None 45 3 Human 9.1 pEC50 = 9.1 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
44520851 443439 0 None None None Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 503 5 2 4 4.4 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL594026 443439 0 None None None Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 503 5 2 4 4.4 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
44520849 461472 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 503 5 2 4 4.4 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL606464 461472 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 503 5 2 4 4.4 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
44520852 432986 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 537 5 2 4 4.7 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL593325 432986 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 537 5 2 4 4.7 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
44520850 442440 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 537 5 2 4 4.7 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL594488 442440 0 None None None Human 9.0 pEC50 = 9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 537 5 2 4 4.7 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
44520880 26845 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1186825 26845 0 None None None Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1819441 484918 0 None -18 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1067 19 14 15 -4.9 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
CHEMBL1819441 484918 0 None -18 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1067 19 14 15 -4.9 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
9824954 155543 0 None None None Human 8.8 pEC50 = 8.8 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL201889 155543 0 None None None Human 8.8 pEC50 = 8.8 Functional
Binding to human V2 receptor expressed in LV2 cells by cAMP productionBinding to human V2 receptor expressed in LV2 cells by cAMP production
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
9959174 386967 0 None None None Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL528996 386967 0 None None None Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
9959174 386967 0 None None None Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL528996 386967 0 None None None Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
10281429 371565 0 None None None Human 8.0 pEC50 = 8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 568 7 1 4 4.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OCc2ccccc2)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL501078 371565 0 None None None Human 8.0 pEC50 = 8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 568 7 1 4 4.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OCc2ccccc2)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
25181105 372091 0 None None None Human 8.0 pEC50 = 8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 463 5 2 2 5.8 CCc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL507816 372091 0 None None None Human 8.0 pEC50 = 8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 463 5 2 2 5.8 CCc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
25178785 350703 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 449 4 1 4 3.8 COC(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL460303 350703 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 449 4 1 4 3.8 COC(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
18759824 372948 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 448 5 2 3 3.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCC1 10.1021/jm8008162
CHEMBL516629 372948 0 None None None Human 7.0 pEC50 = 7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 448 5 2 3 3.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCC1 10.1021/jm8008162
25180885 354218 0 None None None Human 6.0 pEC50 = 6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 464 4 1 4 3.2 Cc1cc(C(=O)N2CCCOc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475129 354218 0 None None None Human 6.0 pEC50 = 6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 464 4 1 4 3.2 Cc1cc(C(=O)N2CCCOc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
44520882 26849 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186831 26849 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
145963213 317022 0 None -36 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1095 17 11 14 -0.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccccc2CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
CHEMBL4127791 317022 0 None -36 3 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1095 17 11 14 -0.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccccc2CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
25178587 348636 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 465 5 2 3 5.3 COc1cc(CNC(=O)Nc2c(F)cccc2F)ccc1C(=O)N1CCCCc2ccccc21 10.1021/jm8008162
CHEMBL455696 348636 0 None None None Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 465 5 2 3 5.3 COc1cc(CNC(=O)Nc2c(F)cccc2F)ccc1C(=O)N1CCCCc2ccccc21 10.1021/jm8008162
11169 1650 39 None -173 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
165708555 1650 39 None -173 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
16681432 1650 39 None -173 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
495 1650 39 None -173 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
CHEMBL3301668 1650 39 None -173 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
DB01282 1650 39 None -173 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
44520881 26846 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1186826 26846 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1817671 484886 0 None -61 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1033 20 12 15 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817671 484886 0 None -61 3 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1033 20 12 15 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819548 484927 0 None -218 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 983 17 12 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819554 484932 0 None -1513 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 969 17 12 15 -4.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
25178963 354385 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475333 354385 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
18759822 373864 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 451 5 2 4 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL518349 373864 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 451 5 2 4 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL1819548 484927 0 None -218 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 983 17 12 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
53362156 136935 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O 10.1021/jm200278m
CHEMBL1817690 136935 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O 10.1021/jm200278m
CHEMBL1819553 484931 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 943 17 12 15 -5.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819554 484932 0 None -1513 4 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 969 17 12 15 -4.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
53362156 136935 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O 10.1021/jm200278m
CHEMBL1817690 136935 0 None -17 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1035 19 11 16 -4.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)N(C)OC)NC1=O 10.1021/jm200278m
CHEMBL1819553 484931 0 None -93 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 943 17 12 15 -5.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
10456892 138359 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837041 138359 0 None None None Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
44563579 348637 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455699 348637 0 None -6 2 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
25178591 347512 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 413 4 2 2 5.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1 10.1021/jm8008162
CHEMBL452853 347512 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 413 4 2 2 5.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1 10.1021/jm8008162
CHEMBL1817705 484891 0 None -512 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 19 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817705 484891 0 None -512 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 19 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817706 484892 0 None -1348 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1033 21 12 15 -3.6 CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
21083206 348302 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 430 4 3 3 4.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccc[nH]c1=O 10.1021/jm8008162
CHEMBL454894 348302 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 430 4 3 3 4.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccc[nH]c1=O 10.1021/jm8008162
15896091 350712 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 423 6 2 4 3.3 CCOC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL460319 350712 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 423 6 2 4 3.3 CCOC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
18759812 350713 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 437 6 2 4 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)C 10.1021/jm8008162
CHEMBL460320 350713 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 437 6 2 4 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OC(C)C 10.1021/jm8008162
25180887 385751 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2CCc3cccn3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL523596 385751 0 None None None Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 499 4 1 4 3.8 Cc1cc(C(=O)N2CCc3cccn3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1817706 484892 0 None -1348 5 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1033 21 12 15 -3.6 CCCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
25180697 353126 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 506 6 1 4 3.8 CCO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
CHEMBL472697 353126 0 None -3 2 Rat 7.8 pEC50 = 7.8 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 506 6 1 4 3.8 CCO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
18759808 350859 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 5 2 3 3.8 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCCC1 10.1021/jm8008162
CHEMBL461725 350859 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 5 2 3 3.8 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N1CCCCC1 10.1021/jm8008162
10298385 350829 38 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
25178787 350829 38 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL461520 350829 38 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL518043 350829 38 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
DB11734 350829 38 None -1 2 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1819542 484921 10 None -1258 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 18 12 15 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819542 484921 10 None -1258 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 18 12 15 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
44520861 354687 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL475684 354687 0 None None None Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
53362548 136948 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817751 136948 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817702 484888 0 None -4786 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 19 12 15 -4.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O 10.1021/jm200278m
53362548 136948 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817751 136948 0 None -602 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 991 17 12 15 -4.8 CCNC(=O)C[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
53362202 136936 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O 10.1021/jm200278m
CHEMBL1817691 136936 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O 10.1021/jm200278m
CHEMBL1817702 484888 0 None -4786 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 19 12 15 -4.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCC(N)=O)NC1=O 10.1021/jm200278m
53362155 137118 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O 10.1021/jm200278m
CHEMBL1819560 137118 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O 10.1021/jm200278m
53362202 136936 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O 10.1021/jm200278m
CHEMBL1817691 136936 0 None -13 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1007 18 13 16 -4.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NO)NC1=O 10.1021/jm200278m
25178962 354217 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 498 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(F)(F)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475128 354217 0 None None None Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 498 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(F)(F)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
53362155 137118 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O 10.1021/jm200278m
CHEMBL1819560 137118 0 None -1513 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1021 19 12 16 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NOC)NC1=O 10.1021/jm200278m
21083210 348635 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 453 4 2 2 5.4 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(F)c1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455695 348635 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 453 4 2 2 5.4 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(F)c1)Nc1c(F)cccc1F 10.1021/jm8008162
15896092 350711 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 395 5 3 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)O 10.1021/jm8008162
CHEMBL460318 350711 0 None None None Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 395 5 3 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)O 10.1021/jm8008162
CHEMBL1817708 484894 0 None -234 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1062 22 12 15 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNCCC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
2173 6017 25 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassay
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
3038506 6017 25 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassay
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
CHEMBL332447 6017 25 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassay
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
DB05838 6017 25 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as stimulation of cAMP accumulation by radioimmunoassay
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
145961670 316908 0 None -2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1139 19 14 15 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccccc2CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
CHEMBL4126100 316908 0 None -2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1139 19 14 15 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccccc2CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
CHEMBL1817708 484894 0 None -234 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1062 22 12 15 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNCCC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
44563579 348637 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455699 348637 0 None 6 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
10162731 350946 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL462574 350946 0 None 17 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
44520848 444355 0 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 534 5 2 5 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmc.2009.10.038
CHEMBL594953 444355 0 None None None Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 534 5 2 5 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmc.2009.10.038
44563371 352839 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 536 7 1 5 3.6 COC(OC)C1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
CHEMBL470326 352839 0 None None None Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 536 7 1 5 3.6 COC(OC)C1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
CHEMBL1819549 484928 0 None -323 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 983 17 12 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819549 484928 0 None -323 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 983 17 12 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccsc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
53363016 137115 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O 10.1021/jm200278m
CHEMBL1819557 137115 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O 10.1021/jm200278m
2042 8014 41 None -43 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
2176 8014 41 None -43 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
439302 8014 41 None -43 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
CHEMBL395429 8014 41 None -43 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
18759802 350931 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 394 5 3 3 2.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(N)=O 10.1021/jm8008162
CHEMBL462409 350931 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 394 5 3 3 2.3 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(N)=O 10.1021/jm8008162
53363016 137115 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O 10.1021/jm200278m
CHEMBL1819557 137115 0 None -34 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1005 18 12 15 -4.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NC)NC1=O 10.1021/jm200278m
10345610 138358 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837040 138358 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
25180884 353400 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 476 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(C)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL474120 353400 0 None None None Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 476 4 1 3 4.3 Cc1cc(C(=O)N2CCCC(C)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
25178961 353398 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 2 4 3.2 Cc1cc(C(=O)N2CCCC(O)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL474119 353398 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 2 4 3.2 Cc1cc(C(=O)N2CCCC(O)c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
135506374 275287 21 None -48 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 581 5 4 8 4.1 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCN(Cc2cc(O)cc(O)c2)CC1 10.1021/acs.jmedchem.8b00697
CHEMBL3763342 275287 21 None -48 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 581 5 4 8 4.1 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCN(Cc2cc(O)cc(O)c2)CC1 10.1021/acs.jmedchem.8b00697
10298385 350829 38 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
25178787 350829 38 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL461520 350829 38 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL518043 350829 38 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
DB11734 350829 38 None 1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1819547 484926 0 None -131 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 984 17 12 17 -5.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cscn2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819547 484926 0 None -131 4 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 984 17 12 17 -5.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cscn2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817707 484893 0 None -1621 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 20 12 15 -4.0 CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
CHEMBL1817707 484893 0 None -1621 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 20 12 15 -4.0 CCNCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
53362259 136940 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O 10.1021/jm200278m
CHEMBL1817696 136940 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O 10.1021/jm200278m
53363017 137116 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819558 137116 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
11454 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
53330936 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
CHEMBL1817709 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
DB12495 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
53362259 136940 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O 10.1021/jm200278m
CHEMBL1817696 136940 0 None -645 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 993 17 13 16 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NO)NC1=O 10.1021/jm200278m
53363017 137116 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819558 137116 0 None -67 3 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 19 12 15 -4.0 CCNC(=O)CC[C@@H]1NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
11237434 138354 15 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837037 138354 15 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
25178960 353151 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 476 4 1 4 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(=O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL472900 353151 0 None None None Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 476 4 1 4 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(=O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
25178784 350706 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 484 7 3 3 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)NCc1ccccc1 10.1021/jm8008162
CHEMBL460308 350706 0 None None None Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 484 7 3 3 4.1 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)NCc1ccccc1 10.1021/jm8008162
11454 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
53330936 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
CHEMBL1817709 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
DB12495 7271 15 None -4786 5 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 21 12 15 -3.2 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCNC(C)C)C 10.1021/jm200278m
CHEMBL1817704 484890 0 None -2238 5 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1033 20 12 15 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
2042 8014 41 None -43 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1016/j.bmc.2018.03.019
2176 8014 41 None -43 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1016/j.bmc.2018.03.019
439302 8014 41 None -43 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1016/j.bmc.2018.03.019
CHEMBL395429 8014 41 None -43 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1016/j.bmc.2018.03.019
CHEMBL1817704 484890 0 None -2238 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1033 20 12 15 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
44520879 27000 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187728 27000 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
25180696 350905 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 1 3 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/jm8008162
CHEMBL462212 350905 0 None None None Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 1 3 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/jm8008162
25180311 348640 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 431 4 2 2 5.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1F 10.1021/jm8008162
CHEMBL455717 348640 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 431 4 2 2 5.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1ccccc1F 10.1021/jm8008162
53362154 137117 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O 10.1021/jm200278m
CHEMBL1819559 137117 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O 10.1021/jm200278m
53362154 137117 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O 10.1021/jm200278m
CHEMBL1819559 137117 0 None -144 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1047 20 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(=O)NCC(C)C)NC1=O 10.1021/jm200278m
56672570 138355 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 438 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837038 138355 0 None None None Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human V2 receptorAgonist activity at human V2 receptor
ChEMBL 438 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1819550 484929 0 None -151 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 967 17 12 16 -5.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819550 484929 0 None -151 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 967 17 12 16 -5.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
25180695 350828 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 490 6 1 3 4.5 CCN(CC)C(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL461519 350828 0 None None None Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 490 6 1 3 4.5 CCN(CC)C(=O)[C@@H]1CCCN1C(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
145960494 317101 0 None -33 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1081 17 11 14 -0.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccc(cc2)SC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
CHEMBL4128839 317101 0 None -33 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1081 17 11 14 -0.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2ccc(cc2)SC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
15896094 372966 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 409 5 2 4 3.0 COC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL516788 372966 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 409 5 2 4 3.0 COC(=O)CNC(=O)NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1C 10.1021/jm8008162
CHEMBL1817752 484896 0 None -2691 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 19 12 15 -4.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817752 484896 0 None -2691 4 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1019 19 12 15 -4.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
10298385 350829 38 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
25178787 350829 38 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL461520 350829 38 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL518043 350829 38 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
DB11734 350829 38 None 1 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1819556 484934 0 None -407 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 927 15 12 15 -5.7 CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819556 484934 0 None -407 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 927 15 12 15 -5.7 CC[C@H](C)[C@@H]1NC(=O)C2(CCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817761 484905 0 None -1202 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1039 20 12 16 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
25178786 350952 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 491 4 1 4 5.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL462595 350952 0 None None None Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 491 4 1 4 5.0 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)(C)C 10.1021/jm8008162
CHEMBL1817761 484905 0 None -1202 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1039 20 12 16 -3.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
145962220 317117 0 None -114 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1095 17 11 14 -0.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2cccc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
CHEMBL4129142 317117 0 None -114 3 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assayAgonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
ChEMBL 1095 17 11 14 -0.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCc2cccc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/j.bmc.2018.03.019
145976595 328683 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as cAMP accumulation incubated for 10 mins by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as cAMP accumulation incubated for 10 mins by radioimmunoassay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4205046 328683 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human V2 receptor expressed in human HeLa cells assessed as cAMP accumulation incubated for 10 mins by radioimmunoassayAgonist activity at human V2 receptor expressed in human HeLa cells assessed as cAMP accumulation incubated for 10 mins by radioimmunoassay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL1819541 484920 0 None -17 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1007 18 13 16 -4.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819541 484920 0 None -17 4 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1007 18 13 16 -4.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
42629368 366052 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478902 366052 0 None None None Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
25180697 353126 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 506 6 1 4 3.8 CCO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
CHEMBL472697 353126 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 506 6 1 4 3.8 CCO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
10206789 372834 0 None 13 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 492 5 1 4 3.4 CO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
CHEMBL515607 372834 0 None 13 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 492 5 1 4 3.4 CO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
25181104 372242 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 469 4 2 2 5.9 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL509960 372242 0 None None None Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 469 4 2 2 5.9 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1)Nc1c(F)cccc1F 10.1021/jm8008162
10444 4740 20 None -9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
145711714 4740 20 None -9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
CHEMBL4204210 4740 20 None -9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
10162731 350946 0 None -17 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL462574 350946 0 None -17 2 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 478 4 2 4 2.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](O)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
25178959 372453 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 534 5 1 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OC(C)(C)C)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL512349 372453 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 534 5 1 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1C[C@H](OC(C)(C)C)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL1819552 484930 0 None -42 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 957 16 12 15 -4.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
9954641 348641 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 435 4 2 2 5.3 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455718 348641 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 435 4 2 2 5.3 O=C(NCc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL1819552 484930 0 None -42 3 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 957 16 12 15 -4.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
44563370 353274 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 512 5 1 3 4.2 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(C(F)F)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL473917 353274 0 None None None Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 512 5 1 3 4.2 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CC(C(F)F)C[C@H]1C(=O)N(C)C 10.1021/jm8008162
6918573 137577 2 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
CHEMBL182852 137577 2 None 1 2 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
53362547 136947 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O 10.1021/jm200278m
CHEMBL1817750 136947 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O 10.1021/jm200278m
53362547 136947 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O 10.1021/jm200278m
CHEMBL1817750 136947 0 None -1348 3 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 977 16 12 15 -5.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)NC)NC1=O 10.1021/jm200278m
6918573 137577 2 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
CHEMBL182852 137577 2 None -1 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 422 5 2 3 2.9 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)N(C)C 10.1021/jm8008162
42629369 356021 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478283 356021 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP levelAgonist activity at human V2 receptor expressed in CHO cells assessed as increase in cAMP level
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
42629369 356021 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
CHEMBL478283 356021 0 None None None Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
44520872 26878 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186989 26878 0 None None None Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44520883 26961 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187505 26961 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assayAgonist activity at human vasopressin V2 receptor expressed in CHO cells assessed as cAMP accumulation by HTRF assay
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
10206789 372834 0 None -13 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 492 5 1 4 3.4 CO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
CHEMBL515607 372834 0 None -13 2 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 492 5 1 4 3.4 CO[C@@H]1C[C@@H](C(=O)N(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4ccccc43)cc2C)C1 10.1021/jm8008162
10444 4740 20 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
145711714 4740 20 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
CHEMBL4204210 4740 20 None -9 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
11169 1650 39 None -173 5 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
165708555 1650 39 None -173 5 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
16681432 1650 39 None -173 5 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
495 1650 39 None -173 5 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
CHEMBL3301668 1650 39 None -173 5 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
DB01282 1650 39 None -173 5 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assayAgonist activity at human V2 receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/acs.jmedchem.8b00697
25180508 350950 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 435 4 2 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)O 10.1021/jm8008162
CHEMBL462590 350950 0 None None None Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 435 4 2 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)O 10.1021/jm8008162
CHEMBL1819543 484922 0 None -144 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 977 17 12 15 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817703 484889 0 None -24 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 963 16 12 15 -5.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817703 484889 0 None -24 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 963 16 12 15 -5.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819543 484922 0 None -144 4 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 977 17 12 15 -5.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
25180507 373015 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 485 7 2 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OCc1ccccc1 10.1021/jm8008162
CHEMBL516985 373015 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 485 7 2 4 4.5 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)OCc1ccccc1 10.1021/jm8008162
CHEMBL1819555 484933 0 None -3019 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 983 17 12 15 -4.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1819555 484933 0 None -3019 4 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 983 17 12 15 -4.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
2042 8014 41 None -43 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
2176 8014 41 None -43 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
439302 8014 41 None -43 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
CHEMBL395429 8014 41 None -43 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assayAgonist activity at human V2 receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/acs.jmedchem.8b00697
21083212 348299 1 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 463 4 2 2 5.9 Cc1cc(C(=O)N2CCCCc3ccccc32)cc(C)c1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL454892 348299 1 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 463 4 2 2 5.9 Cc1cc(C(=O)N2CCCCc3ccccc32)cc(C)c1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
25178592 350930 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 471 6 2 4 4.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)Oc1ccccc1 10.1021/jm8008162
CHEMBL462408 350930 0 None None None Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 471 6 2 4 4.4 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)NCC(=O)Oc1ccccc1 10.1021/jm8008162
25180886 354731 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 510 4 1 3 4.6 Cc1cc(C(=O)N2CCc3ccccc3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL475733 354731 0 None None None Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 510 4 1 3 4.6 Cc1cc(C(=O)N2CCc3ccccc3-c3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)N(C)C 10.1021/jm8008162
135413563 241495 20 None -28 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human V2 receptor expressed in CHO cells co-expressing CRE-luciferase incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human V2 receptor expressed in CHO cells co-expressing CRE-luciferase incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/acs.jmedchem.8b00697
CHEMBL360648 241495 20 None -28 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human V2 receptor expressed in CHO cells co-expressing CRE-luciferase incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human V2 receptor expressed in CHO cells co-expressing CRE-luciferase incubated for 5 hrs by luciferase reporter gene assay
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/acs.jmedchem.8b00697
CHEMBL1819540 484919 0 None -64 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1025 18 12 15 -4.4 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
CHEMBL1819540 484919 0 None -64 3 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1025 18 12 15 -4.4 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm200278m
25180509 372946 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 477 5 1 4 4.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)C 10.1021/jm8008162
CHEMBL516627 372946 0 None None None Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assayAgonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
ChEMBL 477 5 1 4 4.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=O)OC(C)C 10.1021/jm8008162
CHEMBL1817756 484900 0 None -1548 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1023 20 12 16 -4.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817756 484900 0 None -1548 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1023 20 12 16 -4.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccco2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817770 484914 0 None -691 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1026 19 12 15 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
CHEMBL1817770 484914 0 None -691 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assayAgonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
ChEMBL 1026 19 12 15 -3.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](CC2CCCCC2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm200278m
10411308 462175 0 None 4 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at V2 receptor (unknown origin)Antagonist activity at V2 receptor (unknown origin)
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
CHEMBL603708 462175 0 None 4 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at V2 receptor (unknown origin)Antagonist activity at V2 receptor (unknown origin)
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
44357890 333091 0 None 39 3 Human 9.0 pIC50 = 9.0 Functional
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
CHEMBL434654 333091 0 None 39 3 Human 9.0 pIC50 = 9.0 Functional
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
121301508 350186 8 None 2 4 Human 8.8 pIC50 = 8.8 Functional
Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
CHEMBL4594444 350186 8 None 2 4 Human 8.8 pIC50 = 8.8 Functional
Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
DB16279 350186 8 None 2 4 Human 8.8 pIC50 = 8.8 Functional
Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
11432362 194550 0 None -1 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 518 4 2 3 6.1 O=C(O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL249340 194550 0 None -1 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 518 4 2 3 6.1 O=C(O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
10461417 212920 0 None -7 2 Human 7.0 pIC50 = 7 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL317243 212920 0 None -7 2 Human 7.0 pIC50 = 7 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
44352783 235671 0 None 4 2 Human 7.0 pIC50 = 7 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL337725 235671 0 None 4 2 Human 7.0 pIC50 = 7 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
44336404 220478 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL326225 220478 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
25132999 310912 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 572 5 2 5 6.0 COc1cc(C(=O)N2CC[C@]3(C=C(C4=NCCN4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL400860 310912 0 None -3 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 572 5 2 5 6.0 COc1cc(C(=O)N2CC[C@]3(C=C(C4=NCCN4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
151171 2408 36 None -3 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
2203 2408 36 None -3 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
732 2408 36 None -3 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1755 2408 36 None -3 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
DB00872 2408 36 None -3 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
25133000 194606 0 None 2 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 626 6 3 6 4.4 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)NS(N)(=O)=O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL249740 194606 0 None 2 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 626 6 3 6 4.4 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)NS(N)(=O)=O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
216237 8365 53 None 66 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
2226 8365 53 None 66 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
4110 8365 53 None 66 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
CHEMBL344159 8365 53 None 66 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
DB06212 8365 53 None 66 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
11261339 308698 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL399289 308698 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
145976595 328683 0 None 1 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human V2 receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassayAntagonist activity at human V2 receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4205046 328683 0 None 1 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human V2 receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassayAntagonist activity at human V2 receptor expressed in human HeLa cells assessed as inhibition of AVP-induced cAMP accumulation incubated for 10 mins by radioimmunoassay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
23598597 194511 0 None 91 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
CHEMBL249133 194511 0 None 91 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
11238362 333545 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL438523 333545 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
11683187 444222 42 None -20 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced calcium release by Aequorin based assayAntagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced calcium release by Aequorin based assay
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
CHEMBL594828 444222 42 None -20 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced calcium release by Aequorin based assayAntagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of AVP-induced calcium release by Aequorin based assay
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
168289573 374890 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5198918 374890 0 None None None Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44336636 329116 0 None -7 2 Human 6.8 pIC50 = 6.8 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL421039 329116 0 None -7 2 Human 6.8 pIC50 = 6.8 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
23598642 310825 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400267 310825 0 None -2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
23598641 194687 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
CHEMBL250346 194687 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
171391764 391803 3 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin induced cAMP production incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin induced cAMP production incubated for 1 hr
ChEMBL 1255 35 15 13 -0.1 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5575063 391803 3 None None None Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin induced cAMP production incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin induced cAMP production incubated for 1 hr
ChEMBL 1255 35 15 13 -0.1 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
44336784 218784 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL321656 218784 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
155753110 392355 5 None -239 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 452 3 0 7 4.3 Clc1ccc2c(c1)CC1(Cc3nnc([C@H]4CC[C@H](Oc5ccccn5)CC4)n3-2)OCCO1 10.1021/acs.jmedchem.3c01868
CHEMBL5594994 392355 5 None -239 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 452 3 0 7 4.3 Clc1ccc2c(c1)CC1(Cc3nnc([C@H]4CC[C@H](Oc5ccccn5)CC4)n3-2)OCCO1 10.1021/acs.jmedchem.3c01868
135192997 347907 0 None -489 4 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 461 8 0 7 3.7 COc1ccc(-n2c(COCCF)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
CHEMBL4538696 347907 0 None -489 4 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 461 8 0 7 3.7 COc1ccc(-n2c(COCCF)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
168294659 375432 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5207885 375432 0 None None None Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
135192979 349818 0 None -125 4 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 485 7 0 8 3.5 COc1ccc(-n2c(CO[C@H]3CCOC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
CHEMBL4585239 349818 0 None -125 4 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 485 7 0 8 3.5 COc1ccc(-n2c(CO[C@H]3CCOC3)nnc2N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)cn1 10.1021/acsmedchemlett.9b00186
135192928 348934 0 None -851 4 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3cccc(F)c3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
CHEMBL4564411 348934 0 None -851 4 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3cccc(F)c3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
11683187 444222 42 None -20 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assayAntagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
CHEMBL594828 444222 42 None -20 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assayAntagonist activity at human V2 receptor expressed in HEK293FT cells assessed as inhibition of LIT-001-induced response incubated for 30 mins by beta-arrestin recruitment assay
ChEMBL 419 7 0 8 2.9 COCc1nnc(N2CC(Oc3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acs.jmedchem.8b00697
11157078 194607 8 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL249741 194607 8 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
44352804 42816 0 None 24 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL128688 42816 0 None 24 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
9828129 235526 0 None 91 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL336825 235526 0 None 91 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44336379 217038 0 None -6 2 Human 7.5 pIC50 = 7.5 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL318083 217038 0 None -6 2 Human 7.5 pIC50 = 7.5 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
135192983 346716 24 None -2137 4 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
CHEMBL4591825 346716 24 None -2137 4 Human 4.5 pIC50 = 4.5 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 429 6 0 7 3.4 COCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
44377836 120328 0 None None None Human 6.5 pIC50 = 6.5 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL166261 120328 0 None None None Human 6.5 pIC50 = 6.5 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
44336768 328335 0 None -1 2 Human 6.5 pIC50 = 6.5 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL419183 328335 0 None -1 2 Human 6.5 pIC50 = 6.5 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
44444762 308702 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL399888 308702 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
54582950 125772 0 None -3 4 Human 7.4 pIC50 = 7.4 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788220 125772 0 None -3 4 Human 7.4 pIC50 = 7.4 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
44352757 237255 0 None 58 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL341173 237255 0 None 58 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
23598595 310824 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400266 310824 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
216237 8365 53 None 66 2 Human 8.4 pIC50 = 8.4 Functional
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
2226 8365 53 None 66 2 Human 8.4 pIC50 = 8.4 Functional
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
4110 8365 53 None 66 2 Human 8.4 pIC50 = 8.4 Functional
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
CHEMBL344159 8365 53 None 66 2 Human 8.4 pIC50 = 8.4 Functional
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
DB06212 8365 53 None 66 2 Human 8.4 pIC50 = 8.4 Functional
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
25132666 194935 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 572 5 2 6 5.7 COc1cc(C(=O)N2CC[C@]3(C=C(c4nnn[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL251715 194935 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 572 5 2 6 5.7 COc1cc(C(=O)N2CC[C@]3(C=C(c4nnn[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
44352768 232002 0 None 47 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL334777 232002 0 None 47 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
9871426 235876 0 None 44 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL338901 235876 0 None 44 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cellsInhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44444760 308697 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL399288 308697 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
44336418 217804 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL319636 217804 0 None -2 2 Human 6.4 pIC50 = 6.4 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
10345610 138358 0 None -933 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837040 138358 0 None -933 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 422 2 0 6 3.6 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
23598598 19306 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 19306 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
23598600 19703 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL106938 19703 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
172997 4754 54 None -4 5 Human 8.3 pIC50 = 8.3 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
2238 4754 54 None -4 5 Human 8.3 pIC50 = 8.3 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
CHEMBL49429 4754 54 None -4 5 Human 8.3 pIC50 = 8.3 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
DB06666 4754 54 None -4 5 Human 8.3 pIC50 = 8.3 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
11157078 194607 8 None -3 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL249741 194607 8 None -3 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
9937535 116561 1 None -26 4 Human 6.2 pIC50 = 6.2 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788221 116561 1 None -26 4 Human 6.2 pIC50 = 6.2 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptorEvaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
9826033 120258 0 None -37 3 Human 7.2 pIC50 = 7.2 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165670 120258 0 None -37 3 Human 7.2 pIC50 = 7.2 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
9869993 330428 0 None None None Human 7.2 pIC50 = 7.2 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL424183 330428 0 None None None Human 7.2 pIC50 = 7.2 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
10456892 138359 0 None -549 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837041 138359 0 None -549 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 458 3 0 7 3.0 CS(=O)(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
25133001 194904 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 570 5 2 4 6.9 COc1cc(C(=O)N2CC[C@]3(C=C(c4ncc[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL251561 194904 0 None -7 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 570 5 2 4 6.9 COc1cc(C(=O)N2CC[C@]3(C=C(c4ncc[nH]4)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
135192932 336061 0 None -794 4 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 443 7 0 7 3.8 CCOCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
CHEMBL4464246 336061 0 None -794 4 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assayAntagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
ChEMBL 443 7 0 7 3.8 CCOCc1nnc(N2C[C@@H]3C[C@]3(c3ccc(F)cc3Cl)C2)n1-c1ccc(OC)nc1 10.1021/acsmedchemlett.9b00186
46890707 21056 0 None -20 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1083703 21056 0 None -20 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulationAntagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
11237434 138354 15 None -588 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
CHEMBL1837037 138354 15 None -588 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human V2 receptorAntagonist activity at human V2 receptor
ChEMBL 394 2 0 6 3.6 CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CCN(c3ccccn3)CC2)C1 10.1016/j.bmcl.2011.08.038
23598598 19306 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 19306 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
168294720 375496 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
CHEMBL5208751 375496 0 None None None Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hrAntagonist activity at human V2 receptor expressed in CHO cells assessed as inhibition of vasopressin-induced cAMP accumulation incubated for 1 hr
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
172997 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
2238 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
CHEMBL49429 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
DB06666 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
172997 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
2238 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
CHEMBL49429 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
DB06666 4754 54 None -4 5 Human 7.0 pIC50 = 7.0 Functional
Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.Inhibitory activity of the human V2 receptor was assessed by the accumulation of cAMP in transfected HEK293 cells.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)01059-4
164946750 373223 1 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5173331 373223 1 None None None Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 minsAntagonist activity at human V2 receptor expressed in CHO cells assessed as reduction in vasopressin induced cAMP production preincubated for 30 mins followed by vasopressin stimulation and measured after 30 mins
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44335330 315841 0 None None None Rat 8.0 pKd = 8.0 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1181 36 13 13 -2.0 CCOc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL410838 315841 0 None None None Rat 8.0 pKd = 8.0 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1181 36 13 13 -2.0 CCOc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
71458135 161161 0 None None None Pig 7.0 pKd = 7 Functional
Binding affinity towards V2-receptor in LLCPK cellsBinding affinity towards V2-receptor in LLCPK cells
ChEMBL 1171 20 11 15 1.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(N=[N+]=[N-])cc2)NC(=O)C(C)(C)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00079a020
CHEMBL2115364 161161 0 None None None Pig 7.0 pKd = 7 Functional
Binding affinity towards V2-receptor in LLCPK cellsBinding affinity towards V2-receptor in LLCPK cells
ChEMBL 1171 20 11 15 1.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(N=[N+]=[N-])cc2)NC(=O)C(C)(C)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00079a020
CHEMBL2373423 477760 0 None None None Rat 7.0 pKd = 7 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1054 31 11 12 -1.2 COc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44335436 197381 0 None None None Rat 7.9 pKd = 7.9 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1161 35 13 13 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL267111 197381 0 None None None Rat 7.9 pKd = 7.9 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1161 35 13 13 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44294575 163541 0 None None None Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
44335358 163541 0 None None None Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
44375638 163541 0 None None None Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
CHEMBL216606 163541 0 None None None Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
CHEMBL406184 163541 0 None None None Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
CHEMBL438014 163541 0 None None None Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00173a027
CHEMBL2370376 477653 0 None None None Rat 7.8 pKd = 7.8 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1126 32 11 12 0.6 CCOc1ccc(C[C@@H](NC(=O)CC23CC4CC(CC(C4)C2)C3)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2370381 477655 0 None None None Rat 7.7 pKd = 7.7 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1282 38 14 14 -0.9 CCOc1ccc(C[C@@H](NC(=O)CC23CC4CC(CC(C4)C2)C3)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2370380 477654 0 None None None Rat 7.7 pKd = 7.7 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1282 36 16 14 -2.7 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)CC12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00173a027
14730755 197635 0 None None None Rat 6.6 pKd = 6.6 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1064 32 12 12 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL269251 197635 0 None None None Rat 6.6 pKd = 6.6 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1064 32 12 12 -1.8 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2373516 477762 0 None None None Rat 7.4 pKd = 7.4 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1068 32 11 12 -0.8 CCOc1ccc(C[C@@H](NC(=O)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44335434 316286 0 None None None Rat 7.2 pKd = 7.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1083 30 10 11 0.9 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL411320 316286 0 None None None Rat 7.2 pKd = 7.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1083 30 10 11 0.9 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL2373374 477759 0 None None None Rat 7.2 pKd = 7.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1069 32 13 13 -2.9 NCCCC[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)Cc1ccccc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm00173a027
CHEMBL2373441 477761 0 None None None Rat 5.2 pKd = 5.2 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1077 33 12 13 -2.0 CCOc1ccc(C[C@@H](NC(=O)CC(C)(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)cc1 10.1021/jm00173a027
44335231 313459 0 None None None Rat 8.1 pKd = 8.1 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1239 36 13 13 -0.6 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
CHEMBL408038 313459 0 None None None Rat 8.1 pKd = 8.1 Functional
Vasopressin V2 receptor antagonistic activity in vivo in anesthetized ratsVasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
ChEMBL 1239 36 13 13 -0.6 CCOc1ccc(C[C@@H](NC(=O)CC23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)C(C)C)cc1 10.1021/jm00173a027
44385657 256141 0 None None None Pig 8.9 pKi = 8.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44386594 256141 0 None None None Pig 8.9 pKi = 8.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL366552 256141 0 None None None Pig 8.9 pKi = 8.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL433614 256141 0 None None None Pig 8.9 pKi = 8.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL2372280 477731 0 None None None Pig 8.8 pKi = 8.8 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL 1138 22 13 14 -1.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
44579442 370091 0 None None None Human 6.0 pKi = 6 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 391 7 0 9 2.7 CCOc1ccc(-c2nnc(Cn3nccn3)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
CHEMBL489387 370091 0 None None None Human 6.0 pKi = 6 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 391 7 0 9 2.7 CCOc1ccc(-c2nnc(Cn3nccn3)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
11384094 352494 0 None None None Human 7.0 pKi = 7.0 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 6 0 8 3.6 COCc1nnc(-c2cnc(-c3cccc(C)c3C)cn2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
CHEMBL467186 352494 0 None None None Human 7.0 pKi = 7.0 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 6 0 8 3.6 COCc1nnc(-c2cnc(-c3cccc(C)c3C)cn2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
44325538 222041 0 None None None Human 8.0 pKi = 8.0 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL330016 222041 0 None None None Human 8.0 pKi = 8.0 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
46225153 428769 0 None None None Human 5.9 pKi = 5.9 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 399 7 0 8 2.5 COCc1nnc(N2CC(Oc3ccc(F)cc3C)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
CHEMBL589128 428769 0 None None None Human 5.9 pKi = 5.9 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 399 7 0 8 2.5 COCc1nnc(N2CC(Oc3ccc(F)cc3C)C2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2009.11.097
44325345 221059 0 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL328079 221059 0 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
44325505 474335 0 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL94133 474335 0 None None None Human 7.9 pKi = 7.9 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44581241 349862 0 None None None Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 495 8 0 6 5.2 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3Cl)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL458634 349862 0 None None None Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 495 8 0 6 5.2 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3Cl)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
44386688 260433 0 None None None Pig 7.9 pKi = 7.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 981 17 10 12 1.2 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL369806 260433 0 None None None Pig 7.9 pKi = 7.9 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 981 17 10 12 1.2 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
10414302 222004 0 None None None Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329903 222004 0 None None None Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325332 474287 0 None None None Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93861 474287 0 None None None Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44577937 352493 0 None None None Human 6.8 pKi = 6.8 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 7 0 7 4.2 COCc1nnc(-c2ccc(-c3ccccc3OC)cc2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
CHEMBL467185 352493 0 None None None Human 6.8 pKi = 6.8 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 402 7 0 7 4.2 COCc1nnc(-c2ccc(-c3ccccc3OC)cc2)n1-c1ccc(OC)nc1 10.1016/j.bmcl.2008.06.098
44325691 27259 0 None None None Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1189693 27259 0 None None None Human 7.8 pKi = 7.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
9807250 155107 0 None None None Human 6.8 pKi = 6.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL2110044 155107 0 None None None Human 6.8 pKi = 6.8 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325695 332751 0 None None None Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL432043 332751 0 None None None Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
44325362 474244 0 None None None Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93603 474244 0 None None None Human 8.7 pKi = 8.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44385657 256141 0 None None None Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44386594 256141 0 None None None Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL366552 256141 0 None None None Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL433614 256141 0 None None None Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 967 16 10 12 0.8 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44386593 314318 0 None None None Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1024 18 11 13 -0.1 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL409054 314318 0 None None None Pig 8.6 pKi = 8.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1024 18 11 13 -0.1 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
73354746 180313 0 None None None Pig 8.5 pKi = 8.5 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL 981 16 10 12 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
CHEMBL2372281 180313 0 None None None Pig 8.5 pKi = 8.5 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL 981 16 10 12 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
9849525 220928 0 None None None Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327365 220928 0 None None None Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325558 222049 0 None None None Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330094 222049 0 None None None Human 7.7 pKi = 7.7 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
172997 4754 54 None None None Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
2238 4754 54 None None None Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
CHEMBL49429 4754 54 None None None Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
DB06666 4754 54 None None None Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
44325804 474213 0 None None None Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
CHEMBL93366 474213 0 None None None Human 7.6 pKi = 7.6 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
44386687 255848 0 None None None Pig 7.6 pKi = 7.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 968 16 10 12 1.4 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL366473 255848 0 None None None Pig 7.6 pKi = 7.6 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 968 16 10 12 1.4 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
46830095 22579 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 376 5 0 5 4.2 COc1ccc(N(C(=O)c2cnc(-c3cccc(C)c3C)cn2)C(C)C)cn1 10.1016/j.bmcl.2010.02.018
CHEMBL1092459 22579 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 376 5 0 5 4.2 COc1ccc(N(C(=O)c2cnc(-c3cccc(C)c3C)cn2)C(C)C)cn1 10.1016/j.bmcl.2010.02.018
46830094 22748 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 392 7 0 6 3.5 COCCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
CHEMBL1093599 22748 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 392 7 0 6 3.5 COCCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
44581242 349863 0 None None None Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 475 8 0 6 4.9 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL458635 349863 0 None None None Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 475 8 0 6 4.9 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
46225118 451494 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 369 5 0 7 2.7 COc1ccc(-n2c(C)nnc2N2CC(Oc3cc(F)ccc3C)C2)cn1 10.1016/j.bmcl.2009.11.097
CHEMBL602641 451494 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
ChEMBL 369 5 0 7 2.7 COc1ccc(-n2c(C)nnc2N2CC(Oc3cc(F)ccc3C)C2)cn1 10.1016/j.bmcl.2009.11.097
46830096 22312 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 362 5 0 5 3.8 CCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
CHEMBL1090654 22312 0 None None None Human 5.6 pKi = 5.6 Functional
Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 362 5 0 5 3.8 CCN(C(=O)c1cnc(-c2cccc(C)c2C)cn1)c1ccc(OC)nc1 10.1016/j.bmcl.2010.02.018
44325607 221643 0 None None None Human 8.5 pKi = 8.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL329026 221643 0 None None None Human 8.5 pKi = 8.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL2372316 477733 0 None None None Pig 8.5 pKi = 8.5 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL 1043 17 10 11 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)CCCC(C(=O)N3CCC[C@@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
CHEMBL2372291 477424 0 None None None Pig 8.4 pKi = 8.4 Functional
In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pigIn vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSCC(C(=O)N3CCC[C@@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00403a001
122322 2781 0 None None None Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00156a015
2217 2781 0 None None None Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00156a015
44294542 2781 0 None None None Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00156a015
44382370 2781 0 None None None Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00156a015
CHEMBL262423 2781 0 None None None Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00156a015
CHEMBL384776 2781 0 None None None Pig 8.4 pKi = 8.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00156a015
44325915 222215 0 None None None Human 6.5 pKi = 6.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330494 222215 0 None None None Human 6.5 pKi = 6.5 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
2198 6959 2 None None None Human 8.4 pKi = 8.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
9807249 6959 2 None None None Human 8.4 pKi = 8.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1192593 6959 2 None None None Human 8.4 pKi = 8.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
44325895 473118 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96731 473118 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325896 474681 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96255 474681 0 None None None Human 7.4 pKi = 7.4 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44385658 314715 0 None None None Pig 7.4 pKi = 7.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1025 18 11 13 0.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL409486 314715 0 None None None Pig 7.4 pKi = 7.4 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1025 18 11 13 0.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44325363 216275 0 None None None Human 8.3 pKi = 8.3 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL314290 216275 0 None None None Human 8.3 pKi = 8.3 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
73348612 180302 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 939 16 9 12 1.9 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL2371680 180302 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 939 16 9 12 1.9 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@@H](CCN)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44577936 352492 0 None None None Human 6.3 pKi = 6.3 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 371 5 0 5 4.9 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cc1 10.1016/j.bmcl.2008.06.098
CHEMBL467184 352492 0 None None None Human 6.3 pKi = 6.3 Functional
Antagonist activity at vasopressin V2 receptorAntagonist activity at vasopressin V2 receptor
ChEMBL 371 5 0 5 4.9 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cc1 10.1016/j.bmcl.2008.06.098
44581240 372840 0 None None None Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 486 8 0 7 4.4 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C#N)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL515660 372840 0 None None None Human 6.3 pKi = 6.3 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 486 8 0 7 4.4 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3C#N)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
44325703 220906 0 None None None Human 8.2 pKi = 8.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327242 220906 0 None None None Human 8.2 pKi = 8.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44294575 163541 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44335358 163541 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44375638 163541 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL216606 163541 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL406184 163541 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
CHEMBL438014 163541 0 None None None Pig 8.2 pKi = 8.2 Functional
Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membraneInhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00156a015
44581266 349398 0 None None None Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 479 8 0 6 4.7 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3F)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
CHEMBL457544 349398 0 None None None Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assayAntagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
ChEMBL 479 8 0 6 4.7 COc1ccc(S(=O)(=O)N(Cc2ccc(-c3ccccc3F)cn2)c2ccc(OC)nc2)cc1 10.1016/j.bmcl.2008.11.018
11486351 385523 0 None None None Human 5.2 pKi = 5.2 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 398 10 0 8 3.2 CCOc1ccc(-c2nnc(COCCOC)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
CHEMBL522255 385523 0 None None None Human 5.2 pKi = 5.2 Functional
Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assayAntagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
ChEMBL 398 10 0 8 3.2 CCOc1ccc(-c2nnc(COCCOC)n2-c2ccc(OC)nc2)cc1C 10.1016/j.bmcl.2008.08.066
44325704 221794 0 None None None Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329141 221794 0 None None None Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325905 329225 0 None None None Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL421180 329225 0 None None None Human 7.2 pKi = 7.2 Functional
Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptorInhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
2042 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
2174 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
439302 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
CHEMBL395429 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
DB00107 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
P01178 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
P01179 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
P35454 6074 0 None 1 3 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
3514 371491 78 None -18 4 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
5280343 371491 78 None -18 4 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 371491 78 None -18 4 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
DB04216 371491 78 None -18 4 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2812 19119 69 None -16 35 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
719 19119 69 None -16 35 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 19119 69 None -16 35 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
DB00257 19119 69 None -16 35 Human 8.3 pIC50 = 8.3 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
1513 468245 48 None -2 3 Human 8.2 pIC50 = 8.2 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
3793 468245 48 None -2 3 Human 8.2 pIC50 = 8.2 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
CHEMBL64391 468245 48 None -2 3 Human 8.2 pIC50 = 8.2 Functional
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
3537 8682 25 None -1 4 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621
5311500 8682 25 None -1 4 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621
CHEMBL363910 8682 25 None -1 4 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
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ligand		 Fold
selectivity		 # Tested
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 p-value
(-log)		 Activity
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Type		 Assay
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weight		 Rot
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3686 195065 71 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 338 12 1 5 3.5 COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O 10.1038/s41467-023-40064-9
CHEMBL252556 195065 71 None None None Human 5.0 pAC50 = 5.0 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 338 12 1 5 3.5 COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O 10.1038/s41467-023-40064-9
2335 26122 15 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
3018 26122 15 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 26122 15 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
DB11125 26122 15 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
41684 64851 70 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 64851 70 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
DB00507 64851 70 None None None Human 4.9 pAC50 = 4.9 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
2600 8239 59 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 8239 59 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 8239 59 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 8239 59 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 8239 59 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
216416 221077 40 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 221077 40 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
DB06202 221077 40 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
107771 238918 50 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
5485198 238918 50 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
CHEMBL35228 238918 50 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
DB12975 238918 50 None None None Human 4.8 pAC50 = 4.8 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 517 7 2 7 6.1 COc1ccc2nc3cc(Cl)ccc3c(Nc3cc(CN4CCCC4)c(O)c(CN4CCCC4)c3)c2n1 10.1038/s41467-023-40064-9
214 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 8400 48 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
156419 1933 51 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
3308 1933 51 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
647 1933 51 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1201284 1933 51 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
DB01012 1933 51 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 6 1 1 6.1 C[C@H](c1cccc2c1cccc2)NCCCc1cccc(c1)C(F)(F)F 10.1038/s41467-023-40064-9
2436 470362 35 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
68617 470362 35 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 470362 35 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
DB01104 470362 35 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
212 8291 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 8291 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 8291 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 8291 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 8291 39 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
135409453 8225 26 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 8225 26 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
2579 8225 26 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
5362436 8225 26 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 8225 26 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
DB01079 8225 26 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
5328940 200386 70 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 200386 70 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
DB06616 200386 70 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
9915743 126249 63 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
CHEMBL180022 126249 63 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
DB11828 126249 63 None None None Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 556 11 2 8 5.9 CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C 10.1038/s41467-023-40064-9
1222 3419 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3396 3419 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
85 3419 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL46516 3419 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
DB04842 3419 44 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
16362 6358 55 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 6358 55 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 6358 55 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 6358 55 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 6358 55 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
191 833 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 833 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 833 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 833 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 833 62 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
6436173 117955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL1617 117955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
DB01220 117955 32 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 785 2 5 13 6.2 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
4495 393509 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56367 393509 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
DB04743 393509 69 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 10.1038/s41467-023-40064-9
2435 7298 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 7298 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 7298 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 7298 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 7298 64 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
176 823 54 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2157 823 54 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
2566 823 54 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
CHEMBL633 823 54 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
DB01118 823 54 None None None Human 4.6 pAC50 = 4.6 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 10.1038/s41467-023-40064-9
1887 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 5630 45 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
135398735 270475 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
136262914 270475 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
5381226 270475 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL374478 270475 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
DB01045 270475 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 822 4 6 15 4.3 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c(/C=N/N5CCN(C)CC5)c(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
4046 5045 22 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 5045 22 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 5045 22 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 5045 22 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
1478 41858 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
21722 41858 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 41858 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
DB13496 41858 30 None None None Human 4.5 pAC50 = 4.5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
54585 38412 52 None None None Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
6335412 38412 52 None None None Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
CHEMBL1201346 38412 52 None None None Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
DB01014 38412 52 None None None Human 4.4 pAC50 = 4.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 357 7 4 6 2.7 O=C(O)CCNC(=O)c1ccc(/N=N/c2ccc(O)c(C(=O)O)c2)cc1 10.1038/s41467-023-40064-9
2213 1072 37 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1038/s41467-023-40064-9
3008 1072 37 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1038/s41467-023-40064-9
5311010 1072 37 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1038/s41467-023-40064-9
68613 1072 37 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1038/s41467-023-40064-9
CHEMBL378642 1072 37 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1038/s41467-023-40064-9
CHEMBL382301 1072 37 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1038/s41467-023-40064-9
DB09059 1072 37 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1038/s41467-023-40064-9
2713 470127 64 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 470127 64 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 470127 64 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 470127 64 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 470127 64 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 470127 64 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
DB00878 470127 64 None None None Human 5.4 pAC50 = 5.4 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5329102 387203 55 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 387203 55 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
DB01268 387203 55 None None None Human 5.3 pAC50 = 5.3 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
11980903 38402 12 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
22526 38402 12 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
5281035 38402 12 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201303 38402 12 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
DB06816 38402 12 None None None Human 5.2 pAC50 = 5.2 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 382 4 0 2 5.3 Cc1cc(/C=C/c2ccc3cc(N(C)C)ccc3[n+]2C)c(C)n1-c1ccccc1 10.1038/s41467-023-40064-9
3149 26881 13 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1187011 26881 13 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
DB11594 26881 13 None None None Human 5.1 pAC50 = 5.1 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 334 15 0 1 6.1 CCCCCCCCCCCC[N+](C)(C)CCOc1ccccc1 10.1038/s41467-023-40064-9
72093 78550 5 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 78550 5 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
DB13500 78550 5 None None None Human 5.0 pAC50 = 5 Binding
Binding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human AVPR2 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
146681949 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
2168 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
2810 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
644077 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
CHEMBL373742 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
DB00067 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
P01185 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
P01186 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
P35455 8624 35 None None None Human 10.3 pEC50 = 10.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm500365s
5311065 484177 30 None None None Human 9.7 pEC50 = 9.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm500365s
817 484177 30 None None None Human 9.7 pEC50 = 9.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm500365s
CHEMBL1429 484177 30 None None None Human 9.7 pEC50 = 9.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm500365s
DB00035 484177 30 None None None Human 9.7 pEC50 = 9.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm500365s
118719821 234681 0 None None None Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1005 19 11 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353932 234681 0 None None None Human 8.7 pEC50 = 8.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1005 19 11 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719829 234689 0 None None None Human 7.0 pEC50 = 7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1035 23 11 14 -1.1 CCCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3353940 234689 0 None None None Human 7.0 pEC50 = 7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1035 23 11 14 -1.1 CCCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118719832 234692 0 None None None Human 7.0 pEC50 = 7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1009 21 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353943 234692 0 None None None Human 7.0 pEC50 = 7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1009 21 12 15 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720286 234795 0 None None None Human 7.0 pEC50 = 7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 21 11 13 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354598 234795 0 None None None Human 7.0 pEC50 = 7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 21 11 13 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44393912 136872 0 None None None Human 7.0 pEC50 = 7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 643 6 1 6 5.6 CO[C@@H]1C[C@@H](C(=S)N2CCC(N3CCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL181487 136872 0 None None None Human 7.0 pEC50 = 7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 643 6 1 6 5.6 CO[C@@H]1C[C@@H](C(=S)N2CCC(N3CCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118476384 335418 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 939 14 11 11 -0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4454160 335418 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 939 14 11 11 -0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
90469675 335955 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4462743 335955 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
118476337 347681 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1034 16 11 13 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4533159 347681 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1034 16 11 13 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476357 349584 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1032 16 12 13 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4579754 349584 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1032 16 12 13 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
137554057 445087 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 969 15 12 12 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL5957651 445087 0 None None None Human 7.0 pEC50 = 7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 969 15 12 12 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720277 234784 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 988 22 10 12 -1.5 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3354587 234784 0 None None None Human 6.0 pEC50 = 6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 988 22 10 12 -1.5 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118719828 234688 0 None None None Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1019 19 11 14 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353939 234688 0 None None None Human 8.0 pEC50 = 8.0 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1019 19 11 14 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720275 234782 0 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1004 22 11 13 -1.8 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3354585 234782 0 None None None Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1004 22 11 13 -1.8 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
137554060 446442 0 None None None Human 7.0 pEC50 = 7.0 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1020 16 11 13 -0.9 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL5971939 446442 0 None None None Human 7.0 pEC50 = 7.0 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1020 16 11 13 -0.9 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118720266 234774 0 None None None Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 975 21 10 13 -3.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354577 234774 0 None None None Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 975 21 10 13 -3.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
10282736 251877 0 None None None Human 6.0 pEC50 = 6.0 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 627 6 1 6 4.8 CO[C@@H]1C[C@@H](C(=O)N2CCC(N3CCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL362382 251877 0 None None None Human 6.0 pEC50 = 6.0 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 627 6 1 6 4.8 CO[C@@H]1C[C@@H](C(=O)N2CCC(N3CCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118476343 348162 0 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 963 14 10 12 -0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4544907 348162 0 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 963 14 10 12 -0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720274 234781 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 974 21 10 12 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3354584 234781 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 974 21 10 12 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
44394045 334075 0 None None None Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 641 6 1 6 5.2 CO[C@@H]1C[C@@H](C(=O)N2CCC(N3CCCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL443300 334075 0 None None None Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 641 6 1 6 5.2 CO[C@@H]1C[C@@H](C(=O)N2CCC(N3CCCCC3)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118720267 234775 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 975 21 10 13 -3.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354578 234775 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 975 21 10 13 -3.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44393965 254175 0 None None None Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 587 5 1 6 3.8 CO[C@@H]1C[C@@H](C(=O)N2CCCN(C)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL364994 254175 0 None None None Human 5.9 pEC50 = 5.9 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 587 5 1 6 3.8 CO[C@@H]1C[C@@H](C(=O)N2CCCN(C)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118720278 234785 0 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1023 20 11 13 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354588 234785 0 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1023 20 11 13 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720284 234792 0 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354595 234792 0 None None None Human 6.9 pEC50 = 6.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
90469675 335955 0 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4462743 335955 0 None None None Human 6.9 pEC50 = 6.9 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720262 234770 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1048 21 12 15 -2.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCC2CCCN2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354573 234770 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1048 21 12 15 -2.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCC2CCCN2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720263 234771 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1064 21 11 16 -3.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCN2CCOCC2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354574 234771 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1064 21 11 16 -3.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCN2CCOCC2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720285 234793 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1025 20 10 12 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354596 234793 0 None None None Human 5.9 pEC50 = 5.9 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1025 20 10 12 -1.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720269 234777 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354580 234777 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44232512 234794 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 21 11 13 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354597 234794 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 21 11 13 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720283 234790 0 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1022 20 10 12 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354593 234790 0 None None None Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1022 20 10 12 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
11169 1650 39 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/jm500365s
165708555 1650 39 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/jm500365s
16681432 1650 39 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/jm500365s
495 1650 39 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/jm500365s
CHEMBL3301668 1650 39 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/jm500365s
DB01282 1650 39 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C 10.1021/jm500365s
118719840 234700 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccnc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353951 234700 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccnc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476370 427376 0 None None None Human 6.8 pEC50 = 6.8 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1102 17 11 14 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL5875120 427376 0 None None None Human 6.8 pEC50 = 6.8 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1102 17 11 14 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720272 234779 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 990 21 11 13 -2.2 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3354582 234779 0 None None None Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 990 21 11 13 -2.2 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118719839 234699 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353950 234699 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccn2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719843 234703 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1056 21 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccccn2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353954 234703 0 None None None Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1056 21 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccccn2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44393998 138568 0 None None None Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 561 8 2 6 3.4 CO[C@@H]1C[C@@H](C(=O)NCCN(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL184696 138568 0 None None None Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 561 8 2 6 3.4 CO[C@@H]1C[C@@H](C(=O)NCCN(C)C)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
44394063 138653 0 None None None Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 573 4 1 5 5.0 CN1CCCN(C(=S)[C@@H]2CCCN2C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)CC1 10.1016/j.bmcl.2004.04.107
CHEMBL185152 138653 0 None None None Human 5.8 pEC50 = 5.8 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 573 4 1 5 5.0 CN1CCCN(C(=S)[C@@H]2CCCN2C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)CC1 10.1016/j.bmcl.2004.04.107
118476344 347475 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1034 16 11 13 -0.2 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4527761 347475 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1034 16 11 13 -0.2 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476365 347926 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1078 17 11 12 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4539100 347926 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1078 17 11 12 0.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
137554053 424975 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 927 14 11 12 -0.9 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL5849041 424975 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 927 14 11 12 -0.9 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
44393911 137526 0 None None None Human 6.7 pEC50 = 6.7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 611 8 2 6 5.7 CO[C@@H]1C[C@@H](/C(S)=N/CCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL182627 137526 0 None None None Human 6.7 pEC50 = 6.7 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 611 8 2 6 5.7 CO[C@@H]1C[C@@H](/C(S)=N/CCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118476331 347619 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4531173 347619 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118720273 234780 0 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 974 21 10 12 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3354583 234780 0 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 974 21 10 12 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118720281 234788 0 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 20 11 13 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354591 234788 0 None None None Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 20 11 13 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476362 335492 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1048 17 11 13 -0.2 CCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4455496 335492 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1048 17 11 13 -0.2 CCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CSCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476356 336733 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1042 17 11 12 -0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCC2CC2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4473843 336733 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1042 17 11 12 -0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCC2CC2)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720276 234783 0 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1004 22 11 13 -1.8 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3354586 234783 0 None None None Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1004 22 11 13 -1.8 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118476335 334871 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4446853 334871 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476329 347276 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476342 347276 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4521807 347276 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4557118 347276 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476347 349341 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4574065 349341 0 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
5311065 484177 30 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O nan
817 484177 30 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O nan
CHEMBL1429 484177 30 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O nan
DB00035 484177 30 None None None Human 6.7 pEC50 = 6.7 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O nan
118720261 234769 0 None None None Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1035 20 11 15 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)CC2CCCO2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354572 234769 0 None None None Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1035 20 11 15 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)CC2CCCO2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44394044 251895 0 None None None Human 6.6 pEC50 = 6.6 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 603 5 1 6 4.6 CO[C@@H]1C[C@@H](C(=S)N2CCCN(C)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL362483 251895 0 None None None Human 6.6 pEC50 = 6.6 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 603 5 1 6 4.6 CO[C@@H]1C[C@@H](C(=S)N2CCCN(C)CC2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118476358 335216 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1028 16 11 12 -0.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NC2CC2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4451555 335216 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1028 16 11 12 -0.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NC2CC2)NC(=O)[C@H](CC(N)=O)NC1=O nan
118476331 347619 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4531173 347619 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1060 17 12 13 -0.8 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118720288 234797 0 None None None Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354600 234797 0 None None None Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476355 347940 5 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 10 12 0.3 CCN(CC)C(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4539370 347940 5 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 10 12 0.3 CCN(CC)C(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476366 348119 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 18 11 12 0.3 CCCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4543908 348119 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 18 11 12 0.3 CCCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
137554061 443871 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1078 17 12 14 -0.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL5944729 443871 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1078 17 12 14 -0.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720270 234452 0 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 975 21 11 13 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3352839 234452 0 None None None Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 975 21 11 13 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476341 335229 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
137554056 335229 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4451692 335229 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL6007190 335229 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1002 15 11 12 -0.8 CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476385 348655 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1038 17 11 11 0.1 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4557473 348655 0 None None None Human 6.6 pEC50 = 6.6 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1038 17 11 11 0.1 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476329 347276 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118476342 347276 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4521807 347276 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4557118 347276 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1044 17 11 12 0.2 CC(C)CNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
90468623 348224 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1016 16 11 12 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4546884 348224 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1016 16 11 12 -0.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
137554059 425477 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1026 16 12 12 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL5854291 425477 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1026 16 12 12 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CCSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
449224 333602 12 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 17 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL439044 333602 12 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 17 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
DB13798 333602 12 None None None Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 17 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719835 234695 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353946 234695 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720289 234798 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354601 234798 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1029 20 11 14 -1.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476368 409404 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1114 17 11 13 0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL5785589 409404 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1114 17 11 13 0.8 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2cccs2)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720287 234796 0 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1022 21 10 12 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354599 234796 0 None None None Human 5.5 pEC50 = 5.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1022 21 10 12 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476383 334327 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 957 14 10 10 0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4438723 334327 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 957 14 10 10 0.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
118476348 347615 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1096 17 11 13 0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4531053 347615 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1096 17 11 13 0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CSC[C@H]2C(=O)N[C@H](CCCNC(=N)N)C(=O)NCc2ccccc2)NC(=O)[C@H](CC(N)=O)NC1=O nan
137554058 464600 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1032 16 12 13 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL6061847 464600 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1032 16 12 13 -1.5 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
76073634 234791 7 None None None Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354594 234791 7 None None None Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
DB12932 234791 7 None None None Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1041 20 11 13 -1.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476367 334759 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1030 17 11 12 -0.1 CCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4445168 334759 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1030 17 11 12 -0.1 CCCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118719833 234693 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1041 20 11 14 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353944 234693 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1041 20 11 14 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719820 234680 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1007 21 11 14 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3353931 234680 0 None None None Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1007 21 11 14 -1.9 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118476332 334113 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 987 15 11 11 -0.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4435502 334113 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 987 15 11 11 -0.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
137554055 450450 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 969 16 11 12 -0.7 CCc1ccc(C[C@@H]2NC(=O)CCSCC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1 nan
CHEMBL6015152 450450 0 None None None Human 6.5 pEC50 = 6.5 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 969 16 11 12 -0.7 CCc1ccc(C[C@@H]2NC(=O)CCSCC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1 nan
118720279 234786 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1023 20 11 13 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354589 234786 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1023 20 11 13 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
2252 4546 39 None None None Human 4.4 pEC50 = 4.4 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901084f
6918320 4546 39 None None None Human 4.4 pEC50 = 4.4 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901084f
CHEMBL24781 4546 39 None None None Human 4.4 pEC50 = 4.4 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901084f
118719841 234701 0 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccncc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353952 234701 0 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1042 20 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccncc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118476339 346925 0 None None None Human 6.4 pEC50 = 6.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1028 16 11 12 -0.3 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL4513567 346925 0 None None None Human 6.4 pEC50 = 6.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1028 16 11 12 -0.3 CCNC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
3537 8682 25 None None None Human 7.4 pEC50 = 7.4 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
5311500 8682 25 None None None Human 7.4 pEC50 = 7.4 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
CHEMBL363910 8682 25 None None None Human 7.4 pEC50 = 7.4 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
90469676 348456 0 None None None Human 6.4 pEC50 = 6.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 955 15 11 12 -0.9 Cc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1 nan
CHEMBL4552500 348456 0 None None None Human 6.4 pEC50 = 6.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 955 15 11 12 -0.9 Cc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3cccs3)NC2=O)cc1 nan
118719818 234678 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 19 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353929 234678 0 None None None Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 19 11 14 -2.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719824 234684 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1017 19 11 14 -3.1 CCOc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3C[C@@H](O)C[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm500365s
CHEMBL3353935 234684 0 None None None Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1017 19 11 14 -3.1 CCOc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3C[C@@H](O)C[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm500365s
146681949 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
2168 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
2810 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
644077 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
CHEMBL373742 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
DB00067 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
P01185 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
P01186 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
P35455 8624 35 None None None Human 7.4 pEC50 = 7.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N nan
118719825 234685 0 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1032 20 10 14 -2.5 CCOc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3C[C@@H](OC)C[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm500365s
CHEMBL3353936 234685 0 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1032 20 10 14 -2.5 CCOc1ccc(C[C@@H]2NC(=O)CCCSC[C@@H](C(=O)N3C[C@@H](OC)C[C@H]3C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm500365s
118719826 234686 0 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 947 19 11 13 -3.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353937 234686 0 None None None Human 6.4 pEC50 = 6.4 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 947 19 11 13 -3.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
137554054 424593 0 None None None Human 6.4 pEC50 = 6.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1046 16 12 13 -1.1 CC(C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
CHEMBL5844597 424593 0 None None None Human 6.4 pEC50 = 6.4 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1046 16 12 13 -1.1 CC(C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H]1C[C@@H](O)CN1C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N1 nan
118719844 234704 0 None None None Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1056 21 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccncc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353955 234704 0 None None None Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1056 21 11 15 -2.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccncc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44419025 175267 18 None None None Human 7.3 pEC50 = 7.3 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O nan
44419026 175267 18 None None None Human 7.3 pEC50 = 7.3 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O nan
74992363 175267 18 None None None Human 7.3 pEC50 = 7.3 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL221436 175267 18 None None None Human 7.3 pEC50 = 7.3 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL435323 175267 18 None None None Human 7.3 pEC50 = 7.3 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL6015151 175267 18 None None None Human 7.3 pEC50 = 7.3 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720268 234776 0 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354579 234776 0 None None None Human 6.3 pEC50 = 6.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 12 14 -3.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCCO)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720265 234773 0 None None None Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 11 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354576 234773 0 None None None Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 11 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720282 234789 0 None None None Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 20 11 13 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354592 234789 0 None None None Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1038 20 11 13 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccc(C)c2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719830 234690 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1033 19 11 14 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCCCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353941 234690 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1033 19 11 14 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C2CCCCC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719845 234705 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1047 20 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353956 234705 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1047 20 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44393941 335393 0 None None None Human 6.2 pEC50 = 6.2 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 595 8 2 6 4.4 CO[C@@H]1C[C@@H](C(=O)NCCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
CHEMBL445393 335393 0 None None None Human 6.2 pEC50 = 6.2 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 595 8 2 6 4.4 CO[C@@H]1C[C@@H](C(=O)NCCc2ccccn2)N(C(=O)NCc2ccc(C(=O)N3CCCCc4sccc43)cc2Cl)C1 10.1016/j.bmcl.2004.04.107
118720259 234767 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1031 20 11 15 -1.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccco2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354570 234767 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1031 20 11 15 -1.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccco2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719842 234702 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 21 11 14 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353953 234702 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 21 11 14 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719823 234683 0 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1033 19 10 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2C[C@H](SC)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353934 234683 0 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1033 19 10 14 -2.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2C[C@H](SC)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719834 234694 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353945 234694 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719822 234682 0 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1017 19 10 14 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2C[C@H](OC)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353933 234682 0 None None None Human 6.2 pEC50 = 6.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1017 19 10 14 -2.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2C[C@H](OC)C[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
2042 8014 41 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm500365s
2176 8014 41 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm500365s
439302 8014 41 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm500365s
CHEMBL395429 8014 41 None None None Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm500365s
10411308 462175 0 None None None Human 8.1 pEC50 = 8.1 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
CHEMBL603708 462175 0 None None None Human 8.1 pEC50 = 8.1 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
118720264 234772 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 11 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354575 234772 0 None None None Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 991 21 11 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
90469674 336352 10 None None None Human 7.2 pEC50 = 7.2 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 945 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4468523 336352 10 None None None Human 7.2 pEC50 = 7.2 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 945 14 10 11 0.0 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)NCCCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
118720280 234787 0 None None None Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1007 20 10 12 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354590 234787 0 None None None Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1007 20 10 12 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118720271 234778 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 990 21 11 13 -2.2 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3354581 234778 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 990 21 11 13 -2.2 CCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118720290 234799 0 None None None Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1013 20 10 13 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354602 234799 0 None None None Human 6.1 pEC50 = 6.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1013 20 10 13 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSCC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2cccs2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719827 234687 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1021 22 11 14 -1.5 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
CHEMBL3353938 234687 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1021 22 11 14 -1.5 CCCCCN(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm500365s
118719838 234698 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1071 21 11 15 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(OC)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353949 234698 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1071 21 11 15 -1.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(OC)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719831 234691 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1009 21 11 15 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353942 234691 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1009 21 11 15 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCOC)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
90469608 336784 0 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCSCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL4474518 336784 0 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 975 15 11 12 -0.6 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)CCSCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
87056222 461281 0 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
CHEMBL6046074 461281 0 None None None Human 7.1 pEC50 = 7.1 Binding
In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.In Vitro V2 Receptor Assay: Agonist activity of compounds on the human V2 receptor (h V2R) was determined in a transcriptional reporter gene assay by transiently transfecting an h V2 receptor expression DNA into HEK-293 (human embryonic kidney 293 cell line) cells in concert with a reporter DNA containing intracellular calcium responsive promoter elements regulating expression of firefly luciferase. See Boss, V., Talpade, D. J., Murphy, T. J. J. Biol. Chem. 1996, May 3; 271(18), 10429-10432 for further guidance on this assay. Cells were exposed to serial dilutions of compounds diluted 10-fold per dose for 5 h, followed by lysis of cells, determination of luciferase activity, and determination of compound efficacies and EC50 values through non-linear regression. Desmopressin (dDAVP) was used as an internal control in each experiment.
ChEMBL 957 15 12 13 -1.5 CC(C)[C@@H]1NC(=O)[C@H](Cc2cccs2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC1=O nan
118719837 234697 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1059 20 11 14 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353948 234697 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1059 20 11 14 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(F)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
118719836 234696 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(C)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353947 234696 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1055 20 11 14 -1.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)Cc2ccc(C)cc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
135413563 241495 20 None None None Human 6.1 pEC50 = 6.1 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
CHEMBL360648 241495 20 None None None Human 6.1 pEC50 = 6.1 Binding
Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assayActivity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
135413563 241495 20 None None None Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
CHEMBL360648 241495 20 None None None Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 600 4 2 7 4.3 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
118720260 234768 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1061 21 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2cccs2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3354571 234768 0 None None None Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1061 21 11 15 -1.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CCc2cccs2)CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
10187625 255252 0 None None None Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 553 4 1 5 4.7 Cc1cc(C(=O)N2CCCCc3sccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
CHEMBL365862 255252 0 None None None Human 6.1 pEC50 = 6.1 Binding
Effective concentration for human Vasopressin V2 receptorEffective concentration for human Vasopressin V2 receptor
ChEMBL 553 4 1 5 4.7 Cc1cc(C(=O)N2CCCCc3sccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1016/j.bmcl.2004.04.107
118719819 234679 0 None None None Human 8.0 pEC50 = 8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1005 20 11 14 -2.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)CC2CC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
CHEMBL3353930 234679 0 None None None Human 8.0 pEC50 = 8 Binding
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assayAgonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
ChEMBL 1005 20 11 14 -2.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(CC(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)CC2CC2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm500365s
44332239 18879 0 None None None Human 9.7 pIC50 = 9.7 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 466 4 1 3 6.3 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
CHEMBL102311 18879 0 None None None Human 9.7 pIC50 = 9.7 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 466 4 1 3 6.3 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
172997 4754 54 None None None Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
2238 4754 54 None None None Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
CHEMBL49429 4754 54 None None None Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
DB06666 4754 54 None None None Rat 9.3 pIC50 = 9.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00279-6
10648029 215113 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 469 3 1 3 6.2 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1C 10.1021/jm980179c
CHEMBL311931 215113 0 None None None Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 469 3 1 3 6.2 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1C 10.1021/jm980179c
10743786 328452 0 None None None Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 493 3 1 3 6.4 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1Cl 10.1021/jm980179c
CHEMBL420031 328452 0 None None None Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 493 3 1 3 6.4 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1Cl 10.1021/jm980179c
15308000 370586 0 None None None Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
CHEMBL49322 370586 0 None None None Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
9826033 120258 0 None None None Rat 9.0 pIC50 = 9 Binding
Binding affinity towards V2 receptorBinding affinity towards V2 receptor
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165670 120258 0 None None None Rat 9.0 pIC50 = 9 Binding
Binding affinity towards V2 receptorBinding affinity towards V2 receptor
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
56848490 293450 0 None None None Human 9.0 pIC50 = 9 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 575 10 3 8 2.9 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3924331 293450 0 None None None Human 9.0 pIC50 = 9 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 575 10 3 8 2.9 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
44213443 350973 0 None None None Rat 9.0 pIC50 = 9 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL46295 350973 0 None None None Rat 9.0 pIC50 = 9 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
10742418 214204 0 None None None Human 9.0 pIC50 = 9 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
CHEMBL310416 214204 0 None None None Human 9.0 pIC50 = 9 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
172997 4754 54 None None None Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
2238 4754 54 None None None Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
CHEMBL49429 4754 54 None None None Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
DB06666 4754 54 None None None Human 9.0 pIC50 = 9 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2005.08.007
11490613 317266 0 None None None Rat 9.0 pIC50 = 9 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL413748 317266 0 None None None Rat 9.0 pIC50 = 9 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
11490514 258583 0 None None None Human 9.0 pIC50 = 9 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368354 258583 0 None None None Human 9.0 pIC50 = 9 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
44213442 202130 0 None None None Rat 9.0 pIC50 = 9.0 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccc(F)cc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL301788 202130 0 None None None Rat 9.0 pIC50 = 9.0 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccc(F)cc1Cl 10.1016/s0960-894x(99)00279-6
21467141 238395 0 None None None Rat 8.9 pIC50 = 8.9 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL347020 238395 0 None None None Rat 8.9 pIC50 = 8.9 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
172997 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
2238 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
CHEMBL49429 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
DB06666 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
172997 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
2238 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
CHEMBL49429 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
DB06666 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.08.053
172997 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
2238 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
CHEMBL49429 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
DB06666 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00095-0
172997 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
2238 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
CHEMBL49429 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
DB06666 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
172997 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
2238 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
CHEMBL49429 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
DB06666 4754 54 None None None Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(99)00278-4
44378719 120214 0 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 629 6 1 5 7.0 CN1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL165340 120214 0 None None None Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 629 6 1 5 7.0 CN1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
89701036 298440 0 None None None Human 8.9 pIC50 = 8.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 496 7 2 7 3.2 O=c1n(Cc2nnc(Cc3ccccc3F)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3965167 298440 0 None None None Human 8.9 pIC50 = 8.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 496 7 2 7 3.2 O=c1n(Cc2nnc(Cc3ccccc3F)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10459252 105870 0 None None None Rat 8.8 pIC50 = 8.8 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159359 105870 0 None None None Rat 8.8 pIC50 = 8.8 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
69940391 295231 0 None None None Human 8.8 pIC50 = 8.8 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 512 7 2 7 3.7 O=c1n(Cc2nnc(Cc3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3938717 295231 0 None None None Human 8.8 pIC50 = 8.8 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 512 7 2 7 3.7 O=c1n(Cc2nnc(Cc3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10003306 468761 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL68085 468761 0 None None None Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
10003306 468761 0 None None None Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL68085 468761 0 None None None Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 439 3 1 3 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
18917497 201834 0 None None None Rat 8.8 pIC50 = 8.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 486 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Br 10.1016/s0960-894x(99)00279-6
CHEMBL299532 201834 0 None None None Rat 8.8 pIC50 = 8.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 486 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Br 10.1016/s0960-894x(99)00279-6
10098338 238788 0 None None None Human 8.8 pIC50 = 8.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 524 4 2 4 6.9 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL350973 238788 0 None None None Human 8.8 pIC50 = 8.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 524 4 2 4 6.9 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
44213444 202021 0 None None None Rat 8.7 pIC50 = 8.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 442 3 1 4 5.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL300963 202021 0 None None None Rat 8.7 pIC50 = 8.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 442 3 1 4 5.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1Cl 10.1016/s0960-894x(99)00279-6
10672170 470243 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
CHEMBL80029 470243 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
10696913 470401 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 505 4 1 4 6.3 COc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL81269 470401 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 505 4 1 4 6.3 COc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
44336418 217804 0 None None None Human 8.0 pIC50 = 8 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL319636 217804 0 None None None Human 8.0 pIC50 = 8 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 569 6 2 5 5.0 COC(=O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3C)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
56848557 293373 0 None None None Human 8.0 pIC50 = 8 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 607 9 3 7 3.5 CC(=O)NC(C)(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
CHEMBL3923775 293373 0 None None None Human 8.0 pIC50 = 8 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 607 9 3 7 3.5 CC(=O)NC(C)(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
44335345 19510 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL105961 19510 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
11386922 123207 0 None None None Rat 8.0 pIC50 = 8 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175212 123207 0 None None None Rat 8.0 pIC50 = 8 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
11272841 123564 0 None None None Rat 8.0 pIC50 = 8 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL176146 123564 0 None None None Rat 8.0 pIC50 = 8 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
10840974 124530 0 None None None Rat 8.0 pIC50 = 8 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
CHEMBL177285 124530 0 None None None Rat 8.0 pIC50 = 8 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
11763684 259245 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368818 259245 0 None None None Human 8.0 pIC50 = 8 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
11798757 469207 0 None None None Rat 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1021/jm980179c
CHEMBL71305 469207 0 None None None Rat 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1021/jm980179c
44352767 234108 0 None None None Human 7.0 pIC50 = 7 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 528 6 1 3 7.8 O=C(Nc1ccc(C(=O)N2CCC(CC(F)F)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL334363 234108 0 None None None Human 7.0 pIC50 = 7 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 528 6 1 3 7.8 O=C(Nc1ccc(C(=O)N2CCC(CC(F)F)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
69940642 298417 0 None None None Human 7.0 pIC50 = 7 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 509 6 1 7 4.4 O=c1n(Cc2ccnc(-c3ccccc3Cl)n2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3964983 298417 0 None None None Human 7.0 pIC50 = 7 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 509 6 1 7 4.4 O=c1n(Cc2ccnc(-c3ccccc3Cl)n2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10603742 256607 0 None None None Rat 7.0 pIC50 = 7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 607 6 1 6 5.7 CN1CCCN(CC(=O)N2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
CHEMBL366816 256607 0 None None None Rat 7.0 pIC50 = 7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 607 6 1 6 5.7 CN1CCCN(CC(=O)N2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
44386548 260234 0 None None None Rat 7.0 pIC50 = 7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 433 4 1 4 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3sccc32)cc1 10.1021/jm00137a004
CHEMBL369712 260234 0 None None None Rat 7.0 pIC50 = 7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 433 4 1 4 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3sccc32)cc1 10.1021/jm00137a004
10527137 27052 0 None None None Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 441 4 0 3 5.3 Cc1ccccc1C(=O)N(C)c1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL118805 27052 0 None None None Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 441 4 0 3 5.3 Cc1ccccc1C(=O)N(C)c1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
10499401 28273 0 None None None Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 4 1 2 4.5 O=C(Cc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119730 28273 0 None None None Rat 6.0 pIC50 = 6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 4 1 2 4.5 O=C(Cc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
44433372 180754 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 426 5 3 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL237987 180754 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 426 5 3 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
44433375 181015 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 505 7 3 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2Cn2cccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL238206 181015 0 None None None Human 6.0 pIC50 = 6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 505 7 3 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)Nc2ccccc2Cn2cccc2C(=O)O)c(Cl)c1 10.1016/j.bmcl.2007.08.053
10710850 238021 0 None None None Human 6.0 pIC50 = 6 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 320 2 0 2 4.3 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL343538 238021 0 None None None Human 6.0 pIC50 = 6 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 320 2 0 2 4.3 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
11756081 42758 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 510 6 1 5 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cn1ccnc1)C2 10.1021/jm00077a002
CHEMBL128398 42758 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 510 6 1 5 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cn1ccnc1)C2 10.1021/jm00077a002
10098227 42814 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1cccnc1)C2 10.1021/jm00077a002
CHEMBL128680 42814 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1cccnc1)C2 10.1021/jm00077a002
9983763 43239 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 508 7 1 4 3.8 CCCS(=O)(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL129234 43239 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 508 7 1 4 3.8 CCCS(=O)(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10436744 45019 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccncc1)C2 10.1021/jm00077a002
CHEMBL131269 45019 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccncc1)C2 10.1021/jm00077a002
10256140 45363 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 520 6 1 3 4.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@H](NC(=O)Cc1ccccc1)C2 10.1021/jm00077a002
CHEMBL131613 45363 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 520 6 1 3 4.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@H](NC(=O)Cc1ccccc1)C2 10.1021/jm00077a002
44352440 235661 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1ccncc1)C2 10.1021/jm00077a002
CHEMBL337667 235661 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1ccncc1)C2 10.1021/jm00077a002
44352497 235921 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 472 5 2 4 3.1 CC(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL339151 235921 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 472 5 2 4 3.1 CC(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10324129 333224 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 512 6 1 7 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cn1cnnn1)C2 10.1021/jm00077a002
CHEMBL435613 333224 0 None None None Rat 5.0 pIC50 = 5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 512 6 1 7 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cn1cnnn1)C2 10.1021/jm00077a002
10432863 193666 0 None None None Rat 4.0 pIC50 = 4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 430 4 2 4 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@](O)(CN)C2 10.1021/jm00077a002
CHEMBL274955 193666 0 None None None Rat 4.0 pIC50 = 4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 430 4 2 4 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@](O)(CN)C2 10.1021/jm00077a002
CHEMBL2332718 485345 0 None None None Human 5.0 pIC50 = 5.0 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assay
ChEMBL 695 10 10 10 -4.2 NC[C@@H]1NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1016/j.bmcl.2012.12.041
135177391 427841 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 422 6 0 8 3.3 COCc1nnc(N2CC(n3cc(C)c4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5880656 427841 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 422 6 0 8 3.3 COCc1nnc(N2CC(n3cc(C)c4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
10461417 212920 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL317243 212920 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
44336636 329116 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL421039 329116 0 None None None Human 8.0 pIC50 = 8.0 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 585 7 3 4 6.0 O=C(NCCO)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
67409933 296735 0 None None None Human 8.0 pIC50 = 8.0 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 554 8 1 7 5.5 COc1ccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)cc1 nan
CHEMBL3950716 296735 0 None None None Human 8.0 pIC50 = 8.0 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 554 8 1 7 5.5 COc1ccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)cc1 nan
56848553 292339 0 None None None Human 8.0 pIC50 = 8.0 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 651 9 3 8 5.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(Cl)c1Cl nan
CHEMBL3915616 292339 0 None None None Human 8.0 pIC50 = 8.0 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 651 9 3 8 5.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(Cl)c1Cl nan
9869993 330428 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL424183 330428 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 485 4 2 2 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4c[nH]c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
44433363 293356 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 489 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C=C3CCC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL392363 293356 0 None None None Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 489 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C=C3CCC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
9961036 26002 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 643 5 1 5 6.7 CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL1181319 26002 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 643 5 1 5 6.7 CN1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
53378729 279601 0 None None None Human 7.0 pIC50 = 7.0 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 473 7 0 6 5.2 C=CCn1c(-c2ccc(Cl)cc2)nn(Cc2cncn2Cc2c(Cl)cccc2Cl)c1=O nan
CHEMBL3890193 279601 0 None None None Human 7.0 pIC50 = 7.0 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 473 7 0 6 5.2 C=CCn1c(-c2ccc(Cl)cc2)nn(Cc2cncn2Cc2c(Cl)cccc2Cl)c1=O nan
10620180 232548 0 None None None Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCOc3ccccc32)cc1 10.1021/jm960133o
CHEMBL332060 232548 0 None None None Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCOc3ccccc32)cc1 10.1021/jm960133o
23598597 194511 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
CHEMBL249133 194511 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 528 5 2 4 5.8 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1CCC2(C=C(C(=O)O)CC2)Cc2ccccc21 10.1016/j.bmcl.2007.09.059
CHEMBL338018 486995 0 None None None Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 807 10 4 7 3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
69940703 292908 0 None None None Human 6.0 pIC50 = 6.0 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 490 6 0 6 5.8 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)s2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
CHEMBL3920097 292908 0 None None None Human 6.0 pIC50 = 6.0 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 490 6 0 6 5.8 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)s2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
CHEMBL2112248 485096 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 754 6 5 8 1.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00099a019
44273368 199036 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 584 9 1 6 3.2 CN(C)CCCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL278377 199036 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 584 9 1 6 3.2 CN(C)CCCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
10031372 42735 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 592 7 2 6 2.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCS(N)(=O)=O)C1=O)C2 10.1021/jm00077a002
CHEMBL128258 42735 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 592 7 2 6 2.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCS(N)(=O)=O)C1=O)C2 10.1021/jm00077a002
44352433 236125 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 622 10 3 7 1.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)NC(=O)CN)C2 10.1021/jm00077a002
CHEMBL339498 236125 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 622 10 3 7 1.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)NC(=O)CN)C2 10.1021/jm00077a002
9881053 238916 0 None None None Pig 5.0 pIC50 = 5.0 Binding
Ability to displace [3H]AVP from Vasopressin V2 receptorAbility to displace [3H]AVP from Vasopressin V2 receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL35226 238916 0 None None None Pig 5.0 pIC50 = 5.0 Binding
Ability to displace [3H]AVP from Vasopressin V2 receptorAbility to displace [3H]AVP from Vasopressin V2 receptor
ChEMBL 339 5 1 4 4.1 CCCN1CCC(COc2nc3ccccc3c3c2CCCN3)CC1 10.1021/jm020954v
CHEMBL129733 484608 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 726 6 3 6 2.7 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
CHEMBL338020 486996 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 755 6 5 7 1.9 CC(C)C[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10030575 45952 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 5 2 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NC1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL132210 45952 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 5 2 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NC1CN3CCC1CC3)C2 10.1021/jm00077a002
44273077 199110 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
44273316 199110 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL279022 199110 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL281361 199110 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
135177394 450491 0 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 422 6 0 8 3.1 COCc1nnc(N2CC(c3cn(C)c4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
CHEMBL6015635 450491 0 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 422 6 0 8 3.1 COCc1nnc(N2CC(c3cn(C)c4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
1513 468245 48 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 468245 48 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 468245 48 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44352777 45231 0 None None None Human 7.9 pIC50 = 7.9 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 572 7 2 5 6.4 O=C(Nc1ccc(C(=O)N2CCC(CCS(=O)(=O)O)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL131439 45231 0 None None None Human 7.9 pIC50 = 7.9 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 572 7 2 5 6.4 O=C(Nc1ccc(C(=O)N2CCC(CCS(=O)(=O)O)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
53378841 292611 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2cncc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
CHEMBL3917760 292611 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2cncc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
53378731 309821 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 556 8 2 9 3.3 O=C(O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
CHEMBL3981686 309821 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 556 8 2 9 3.3 O=C(O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
119369 5304 49 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
2197 5304 49 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
4004 5304 49 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
CHEMBL420762 5304 49 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm960133o
44377961 120310 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 585 5 3 4 6.6 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL166135 120310 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 585 5 3 4 6.6 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
19699093 238730 0 None None None Rat 6.9 pIC50 = 6.9 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350383 238730 0 None None None Rat 6.9 pIC50 = 6.9 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
10595255 60212 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 368 2 0 2 5.3 O=C(c1ccc(N2CCCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL136065 60212 0 None None None Human 6.9 pIC50 = 6.9 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 368 2 0 2 5.3 O=C(c1ccc(N2CCCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
56848685 298432 0 None None None Human 5.9 pIC50 = 5.9 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 603 10 2 9 4.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NC(=O)OC(C)(C)C)c2ccccc2C(F)(F)F)c1=O nan
CHEMBL3965109 298432 0 None None None Human 5.9 pIC50 = 5.9 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 603 10 2 9 4.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NC(=O)OC(C)(C)C)c2ccccc2C(F)(F)F)c1=O nan
10810069 25999 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1C 10.1021/jm960133o
CHEMBL118128 25999 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1C 10.1021/jm960133o
443894 327675 32 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of Vasopressin V2 receptor (unknown origin)Inhibition of Vasopressin V2 receptor (unknown origin)
ChEMBL 448 3 2 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cc(Cl)ccc32)c(C)c1 10.1016/j.ejmech.2024.116556
CHEMBL344159 327675 32 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of Vasopressin V2 receptor (unknown origin)Inhibition of Vasopressin V2 receptor (unknown origin)
ChEMBL 448 3 2 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cc(Cl)ccc32)c(C)c1 10.1016/j.ejmech.2024.116556
CHEMBL4303142 327675 32 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of Vasopressin V2 receptor (unknown origin)Inhibition of Vasopressin V2 receptor (unknown origin)
ChEMBL 448 3 2 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cc(Cl)ccc32)c(C)c1 10.1016/j.ejmech.2024.116556
DB06212 327675 32 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of Vasopressin V2 receptor (unknown origin)Inhibition of Vasopressin V2 receptor (unknown origin)
ChEMBL 448 3 2 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cc(Cl)ccc32)c(C)c1 10.1016/j.ejmech.2024.116556
11441742 461611 2 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of Vasopressin V2 receptor (unknown origin)Inhibition of Vasopressin V2 receptor (unknown origin)
ChEMBL 427 4 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](N(C)C)c3ccccc32)cc1 10.1016/j.ejmech.2024.116556
CHEMBL6151557 461611 2 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition of Vasopressin V2 receptor (unknown origin)Inhibition of Vasopressin V2 receptor (unknown origin)
ChEMBL 427 4 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](N(C)C)c3ccccc32)cc1 10.1016/j.ejmech.2024.116556
CHEMBL2370623 485596 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 739 6 2 7 2.7 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00099a019
10391259 42755 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 5 1 4 3.3 CNC1CCN([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
CHEMBL128388 42755 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 5 1 4 3.3 CNC1CCN([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
10052640 44977 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 527 6 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CC1CCCNC1)C2 10.1021/jm00077a002
CHEMBL131239 44977 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 527 6 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CC1CCCNC1)C2 10.1021/jm00077a002
10257352 160035 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
10483039 160035 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL2111851 160035 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL2112666 160035 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
135177568 409960 0 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 394 4 0 7 2.8 COc1ccc(-n2c(C)nnc2N2CC(N3CCCc4cc(F)ccc43)C2)cn1 nan
CHEMBL5791271 409960 0 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 394 4 0 7 2.8 COc1ccc(-n2c(C)nnc2N2CC(N3CCCc4cc(F)ccc43)C2)cn1 nan
44433360 180286 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 418 2 0 4 4.5 Cc1ccn(-c2ccc(C(=O)N3C=C4CCC(=O)N4Cc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2007.08.053
CHEMBL237120 180286 0 None None None Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 418 2 0 4 4.5 Cc1ccn(-c2ccc(C(=O)N3C=C4CCC(=O)N4Cc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2007.08.053
135177401 405457 0 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 425 6 0 8 3.8 COCc1nnc(N2CC(c3csc4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5745774 405457 0 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 425 6 0 8 3.8 COCc1nnc(N2CC(c3csc4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
1513 468245 48 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 468245 48 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 468245 48 None None None Human 4.9 pIC50 = 4.9 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
88064173 298266 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 530 7 1 6 5.4 O=c1n(Cc2nnc(Cc3c(Cl)cccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1CCC(F)(F)F nan
CHEMBL3963751 298266 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 530 7 1 6 5.4 O=c1n(Cc2nnc(Cc3c(Cl)cccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1CCC(F)(F)F nan
56848556 293735 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 579 10 3 7 2.9 O=CNC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
CHEMBL3926829 293735 0 None None None Human 7.9 pIC50 = 7.9 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 579 10 3 7 2.9 O=CNC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
10838493 28159 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccc(Cl)cc3Cl)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL119638 28159 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccc(Cl)cc3Cl)cc2)c2ccccc21 10.1021/jm960133o
10742994 219914 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 470 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC(N)=O)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL324251 219914 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 470 6 2 4 4.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC(N)=O)c3ccccc32)cc1 10.1021/jm960133o
9850567 120246 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 551 5 3 4 5.9 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165554 120246 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 551 5 3 4 5.9 O=C(Nc1ccc(C(=O)N2CCCc3c(S(=O)(=O)O)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
21837162 202600 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 453 4 1 4 5.7 CSc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL304060 202600 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 453 4 1 4 5.7 CSc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10503021 202796 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1016/s0960-894x(03)00388-3
CHEMBL304956 202796 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1016/s0960-894x(03)00388-3
10570880 60263 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 365 2 0 3 4.8 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/jm000108p
CHEMBL136109 60263 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 365 2 0 3 4.8 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/jm000108p
10498917 234941 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 362 2 0 2 5.0 CN(C)c1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL335592 234941 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 362 2 0 2 5.0 CN(C)c1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
44335343 217096 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL318392 217096 0 None None None Human 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
14981580 160371 0 None None None Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 637 11 3 8 1.9 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCNCC2)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112895 160371 0 None None None Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 637 11 3 8 1.9 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCNCC2)C3(C)C)CC1 10.1021/jm00031a004
19699093 238730 0 None None None Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350383 238730 0 None None None Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 428 3 2 4 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL2112247 485095 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 769 6 4 8 2.0 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cn(C)c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
44272997 143949 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
9805972 143949 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL19658 143949 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL276990 143949 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
44273346 327964 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 570 8 1 6 2.8 CN(C)CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL417458 327964 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 570 8 1 6 2.8 CN(C)CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
44352492 42827 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 593 9 1 6 3.0 CN(C)C(CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL128749 42827 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 593 9 1 6 3.0 CN(C)C(CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10413998 37968 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 510 6 2 4 3.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@H](NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL128879 37968 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 510 6 2 4 3.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@H](NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
44352150 42724 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 515 7 2 5 2.8 CC(C(N)=O)[C@@H](N)C(=O)[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL128194 42724 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 515 7 2 5 2.8 CC(C(N)=O)[C@@H](N)C(=O)[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
44352299 235691 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 416 3 1 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)/C(=N\O)C2 10.1021/jm00077a002
CHEMBL337842 235691 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 416 3 1 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)/C(=N\O)C2 10.1021/jm00077a002
10347314 235801 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 542 8 2 4 4.9 CCC(C)(C)C(=O)NCC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL338499 235801 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 542 8 2 4 4.9 CCC(C)(C)C(=O)NCC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10459672 236333 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 1 5 4.0 CCOC(=O)CCC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL340016 236333 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 1 5 4.0 CCOC(=O)CCC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10574499 222446 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)c1 10.1021/jm960133o
CHEMBL331098 222446 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)c1 10.1021/jm960133o
10524974 233087 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 399 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL332685 233087 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 399 3 1 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3ccccc32)cc1 10.1021/jm960133o
10984131 238734 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 517 4 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(00)00095-0
CHEMBL350408 238734 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 517 4 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(00)00095-0
10789117 469509 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL73286 469509 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
23598595 310824 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400266 310824 0 None None None Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
21837107 468872 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL68948 468872 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(03)00388-3
10789117 469509 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL73286 469509 0 None None None Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 437 4 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
44378886 119477 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 556 6 2 5 6.4 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1O)C2 10.1016/s0960-894x(00)00095-0
CHEMBL164226 119477 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 556 6 2 5 6.4 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1O)C2 10.1016/s0960-894x(00)00095-0
10601045 28204 0 None None None Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 487 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2CCCC(N3CCCCC3)c3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
CHEMBL119671 28204 0 None None None Rat 6.9 pIC50 = 6.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 487 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2CCCC(N3CCCCC3)c3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
19699060 118959 0 None None None Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL162588 118959 0 None None None Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
10690528 232555 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.8 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
CHEMBL332090 232555 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.8 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
135177442 463824 0 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 438 7 0 8 3.0 CCOCc1nnc(N2CC(N3CCCc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL6053580 463824 0 None None None Human 5.9 pIC50 = 5.9 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 438 7 0 8 3.0 CCOCc1nnc(N2CC(N3CCCc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL338294 486999 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 757 10 4 7 2.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10347928 237266 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
CHEMBL341289 237266 0 None None None Rat 5.9 pIC50 = 5.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
44352165 237351 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 552 7 3 6 1.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CS(N)(=O)=O)C2 10.1021/jm00077a002
CHEMBL341507 237351 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 552 7 3 6 1.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CS(N)(=O)=O)C2 10.1021/jm00077a002
10324995 329279 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 539 7 3 4 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NCCc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL421248 329279 0 None None None Rat 4.9 pIC50 = 4.9 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 539 7 3 4 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NCCc1c[nH]cn1)C2 10.1021/jm00077a002
44352804 42816 0 None None None Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL128688 42816 0 None None None Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
56848624 316375 0 None None None Human 7.8 pIC50 = 7.8 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 566 9 3 7 3.0 O=C(Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)N[C@@H](CO)Cc1cccc(C(F)(F)F)c1 nan
CHEMBL4114132 316375 0 None None None Human 7.8 pIC50 = 7.8 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 566 9 3 7 3.0 O=C(Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)N[C@@H](CO)Cc1cccc(C(F)(F)F)c1 nan
44377903 120097 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165076 120097 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1Cl)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
44310163 202312 0 None None None Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL302955 202312 0 None None None Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/s0960-894x(03)00388-3
11757222 217626 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL319418 217626 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
10043741 237004 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
CHEMBL340893 237004 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
10043741 237004 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards rat Vasopressin V2 receptorBinding affinity towards rat Vasopressin V2 receptor
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL340893 237004 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Binding affinity towards rat Vasopressin V2 receptorBinding affinity towards rat Vasopressin V2 receptor
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
86690916 297578 0 None None None Human 6.8 pIC50 = 6.8 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 549 6 1 8 4.9 O=c1n(Cc2nnc(-c3ccccc3C(F)(F)F)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3957738 297578 0 None None None Human 6.8 pIC50 = 6.8 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 549 6 1 8 4.9 O=c1n(Cc2nnc(-c3ccccc3C(F)(F)F)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10527129 28097 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 441 4 2 3 4.9 CC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL119591 28097 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 441 4 2 3 4.9 CC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
19699133 238630 0 None None None Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL349506 238630 0 None None None Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL340204 487025 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 807 10 4 7 3.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
44272990 199743 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
44273369 199743 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL283524 199743 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL283994 199743 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
44352481 235886 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 621 11 1 6 3.8 CCN(CC)C(CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL338951 235886 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 621 11 1 6 3.8 CCN(CC)C(CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10347928 237266 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
CHEMBL341289 237266 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
22405325 271041 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 427 4 0 4 5.5 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(-c3cccs3)cc1)C2 10.1016/j.bmcl.2005.08.007
CHEMBL371055 271041 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 427 4 0 4 5.5 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(-c3cccs3)cc1)C2 10.1016/j.bmcl.2005.08.007
10098755 45332 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 538 7 2 4 4.5 CCC(C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C)c1c[nH]cn1 10.1021/jm00077a002
CHEMBL131581 45332 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 538 7 2 4 4.5 CCC(C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C)c1c[nH]cn1 10.1021/jm00077a002
9985844 235551 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 588 6 2 4 4.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1[nH]cnc1Br)C2 10.1021/jm00077a002
CHEMBL336992 235551 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 588 6 2 4 4.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1[nH]cnc1Br)C2 10.1021/jm00077a002
2812 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
719 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
DB00257 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
3514 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
5280343 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
DB04216 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
3514 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
5280343 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
DB04216 371491 78 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
2812 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
719 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
DB00257 19119 69 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
44332208 18594 0 None None None Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.02.103
CHEMBL100447 18594 0 None None None Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.02.103
44352768 232002 0 None None None Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL334777 232002 0 None None None Human 7.8 pIC50 = 7.8 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 536 7 2 4 7.0 O=C(O)CC[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44336784 218784 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL321656 218784 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 626 9 2 4 7.0 CN(C)CCCNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
56849411 309314 0 None None None Human 7.8 pIC50 = 7.8 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 609 10 3 8 3.3 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
CHEMBL3976964 309314 0 None None None Human 7.8 pIC50 = 7.8 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 609 10 3 8 3.3 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
10528416 214442 0 None None None Rat 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 471 4 1 4 5.6 COc1cc(Cl)ccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL310581 214442 0 None None None Rat 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 471 4 1 4 5.6 COc1cc(Cl)ccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
10691737 60853 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 388 2 0 2 5.6 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
CHEMBL136628 60853 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 388 2 0 2 5.6 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
18917508 371303 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 453 4 1 6 4.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1[N+](=O)[O-] 10.1016/s0960-894x(99)00279-6
CHEMBL49796 371303 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 453 4 1 6 4.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1[N+](=O)[O-] 10.1016/s0960-894x(99)00279-6
14981581 160369 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 686 11 2 9 1.7 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCS(=O)(=O)CC2)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112893 160369 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 686 11 2 9 1.7 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCS(=O)(=O)CC2)C3(C)C)CC1 10.1021/jm00031a004
10763869 26149 1 None None None Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 406 4 1 3 4.5 O=C(c1ccc(NS(=O)(=O)c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/jm960133o
CHEMBL118244 26149 1 None None None Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 406 4 1 3 4.5 O=C(c1ccc(NS(=O)(=O)c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/jm960133o
CHEMBL338308 487001 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 742 9 4 8 1.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCN)NC(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00099a019
44352141 45297 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 501 7 2 5 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](C(=O)[C@H](N)CC(N)=O)C2 10.1021/jm00077a002
CHEMBL131538 45297 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 501 7 2 5 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](C(=O)[C@H](N)CC(N)=O)C2 10.1021/jm00077a002
10323684 235909 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 4 1 5 2.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(=O)C1=O)C2 10.1021/jm00077a002
CHEMBL339096 235909 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 4 1 5 2.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(=O)C1=O)C2 10.1021/jm00077a002
44273080 198876 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 571 7 1 7 2.4 COC(=O)CNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL277022 198876 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 571 7 1 7 2.4 COC(=O)CNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
10834761 233545 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 399 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)Cc3ccccc32)cc1 10.1021/jm960133o
CHEMBL333652 233545 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 399 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)Cc3ccccc32)cc1 10.1021/jm960133o
23505561 238686 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 527 4 1 4 7.1 CC(=O)n1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
CHEMBL349965 238686 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 527 4 1 4 7.1 CC(=O)n1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
67412584 297431 0 None None None Human 5.8 pIC50 = 5.8 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 473 6 1 5 5.1 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)[nH]2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
CHEMBL3956553 297431 0 None None None Human 5.8 pIC50 = 5.8 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 473 6 1 5 5.1 O=c1n(Cc2ncc(Cc3cccc(C(F)(F)F)c3)[nH]2)nc(-c2ccc(Cl)cc2)n1C1CC1 nan
10832492 233797 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 362 3 1 3 4.6 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccsc1 10.1021/jm960133o
CHEMBL334009 233797 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 362 3 1 3 4.6 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccsc1 10.1021/jm960133o
44309805 469203 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 434 3 1 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Oc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71283 469203 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 434 3 1 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Oc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL405289 487856 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 755 7 5 7 2.1 CCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10100280 197144 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 610 9 0 7 3.9 COC(=O)CCN(C(=O)Cc1cn(C)cn1)[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL265073 197144 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 610 9 0 7 3.9 COC(=O)CCN(C(=O)Cc1cn(C)cn1)[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10346739 235892 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 5 0 5 3.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CC#N)C1=O)C2 10.1021/jm00077a002
CHEMBL338984 235892 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 5 0 5 3.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CC#N)C1=O)C2 10.1021/jm00077a002
10368075 333140 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 484 4 0 4 3.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CCC1=O)C2 10.1021/jm00077a002
CHEMBL435019 333140 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 484 4 0 4 3.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CCC1=O)C2 10.1021/jm00077a002
10436379 155022 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 510 6 2 4 3.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1c[nH]cn1)C2 10.1016/0960-894X(94)00469-V
CHEMBL20230 155022 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 510 6 2 4 3.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1c[nH]cn1)C2 10.1016/0960-894X(94)00469-V
10413997 4534 5 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 510 6 2 4 3.6 O=C(Cc1cnc[nH]1)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCC2(CC1)CCc1c2cccc1)(C)C 10.1021/jm00077a002
2246 4534 5 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 510 6 2 4 3.6 O=C(Cc1cnc[nH]1)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCC2(CC1)CCc1c2cccc1)(C)C 10.1021/jm00077a002
CHEMBL338522 4534 5 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 510 6 2 4 3.6 O=C(Cc1cnc[nH]1)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCC2(CC1)CCc1c2cccc1)(C)C 10.1021/jm00077a002
135177427 411045 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 425 6 0 8 3.0 COCc1nnc(N2CC(C3CCOc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5803370 411045 0 None None None Human 4.8 pIC50 = 4.8 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 425 6 0 8 3.0 COCc1nnc(N2CC(C3CCOc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
44336768 328335 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL419183 328335 0 None None None Human 7.8 pIC50 = 7.8 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 599 7 3 4 6.1 O=C(O)CNC(=O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
11740743 38028 0 None None None Rat 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119793 38028 0 None None None Rat 7.8 pIC50 = 7.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
10495509 234114 1 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor expressed in HeLa cells after 2 hrs by liquid scintillation counterDisplacement of [3H]AVP from human Vasopressin V2 receptor expressed in HeLa cells after 2 hrs by liquid scintillation counter
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/acs.jmedchem.5b00982
CHEMBL334376 234114 1 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor expressed in HeLa cells after 2 hrs by liquid scintillation counterDisplacement of [3H]AVP from human Vasopressin V2 receptor expressed in HeLa cells after 2 hrs by liquid scintillation counter
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/acs.jmedchem.5b00982
23598641 194687 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
CHEMBL250346 194687 0 None None None Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 528 5 2 3 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=C(CO)CC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2007.09.059
9974701 60334 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 342 4 1 2 5.1 CCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL136177 60334 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 342 4 1 2 5.1 CCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
10711405 238064 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 328 2 0 2 4.4 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL343935 238064 0 None None None Human 7.8 pIC50 = 7.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 328 2 0 2 4.4 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
10810133 232831 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 385 3 2 2 5.3 O=C(Nc1ccccc1)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL332450 232831 0 None None None Rat 6.8 pIC50 = 6.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 385 3 2 2 5.3 O=C(Nc1ccccc1)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm960133o
44377894 238599 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL349062 238599 0 None None None Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
44332209 18670 0 None None None Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 470 3 1 2 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/j.bmcl.2004.02.103
CHEMBL100893 18670 0 None None None Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 470 3 1 2 6.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/j.bmcl.2004.02.103
10587836 238183 4 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 266 1 1 2 3.3 Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm000108p
CHEMBL344848 238183 4 None None None Human 6.8 pIC50 = 6.8 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 266 1 1 2 3.3 Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm000108p
10524202 28011 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 4 1 3 4.5 COc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
CHEMBL119534 28011 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 4 1 3 4.5 COc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)cc1 10.1021/jm960133o
10258045 42728 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 601 11 4 6 1.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)CCN)C2 10.1021/jm00077a002
CHEMBL128219 42728 0 None None None Rat 5.8 pIC50 = 5.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 601 11 4 6 1.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)CCN)C2 10.1021/jm00077a002
44352393 235748 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 555 6 3 4 4.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)NC1CCCCC1)C2 10.1021/jm00077a002
CHEMBL338177 235748 0 None None None Rat 4.8 pIC50 = 4.8 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 555 6 3 4 4.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)NC1CCCCC1)C2 10.1021/jm00077a002
9931699 156719 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.0 Cn1ccc(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL203513 156719 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.0 Cn1ccc(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
21467152 106370 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 478 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL159831 106370 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 478 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
15307999 201532 0 None None None Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 492 3 1 3 7.1 O=C(Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(99)00278-4
CHEMBL297293 201532 0 None None None Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 492 3 1 3 7.1 O=C(Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(99)00278-4
11792631 234211 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 356 4 0 2 5.2 CCN(CC)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL334688 234211 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 356 4 0 2 5.2 CCN(CC)c1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
44335357 217118 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 517 3 1 3 6.4 Cc1cc(F)cc(C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4ccccc43)c(Cl)c2)c1 10.1016/s0960-894x(02)00649-2
CHEMBL318530 217118 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 517 3 1 3 6.4 Cc1cc(F)cc(C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4ccccc43)c(Cl)c2)c1 10.1016/s0960-894x(02)00649-2
10550481 27139 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 428 4 2 4 4.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3N)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118878 27139 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 428 4 2 4 4.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3N)cc2)c2ccccc21 10.1021/jm960133o
44377837 120329 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL166265 120329 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 427 3 2 2 5.5 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1 10.1016/s0960-894x(02)01059-4
10668163 28040 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1 10.1021/jm960133o
CHEMBL119551 28040 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1 10.1021/jm960133o
10054982 235818 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 645 10 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)N(CCc1c[nH]cn1)CCS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL338576 235818 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 645 10 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)N(CCc1c[nH]cn1)CCS(C)(=O)=O)C2 10.1021/jm00077a002
10054203 236875 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 593 8 0 6 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CCCn3ccnc3)C1=O)C2 10.1021/jm00077a002
CHEMBL340388 236875 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 593 8 0 6 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CCCn3ccnc3)C1=O)C2 10.1021/jm00077a002
CHEMBL2112654 485104 0 None None None Rat 4.7 pIC50 = 4.7 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 716 6 4 7 1.5 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
69940428 296542 0 None None None Human 8.7 pIC50 = 8.7 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 568 8 2 7 5.2 O=C(O)c1cccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)c1 nan
CHEMBL3949118 296542 0 None None None Human 8.7 pIC50 = 8.7 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 568 8 2 7 5.2 O=C(O)c1cccc(Cn2c(-c3ccc(Cl)cc3)nn(Cc3nnc(Cc4c(Cl)cccc4Cl)[nH]3)c2=O)c1 nan
56848625 291929 0 None None None Human 8.7 pIC50 = 8.7 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 595 9 3 8 3.5 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(Cl)c1Cl nan
CHEMBL3912406 291929 0 None None None Human 8.7 pIC50 = 8.7 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 595 9 3 8 3.5 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(Cl)c1Cl nan
56848623 298320 0 None None None Human 8.7 pIC50 = 8.7 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 561 9 3 8 2.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3964135 298320 0 None None None Human 8.7 pIC50 = 8.7 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 561 9 3 8 2.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
10673295 214598 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL311230 214598 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
10766720 215143 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 469 4 1 4 5.4 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1Cc2cccn2Cc2ccccc21 10.1021/jm980179c
CHEMBL312036 215143 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 469 4 1 4 5.4 COc1cc(NC(=O)c2cc(F)ccc2C)ccc1C(=O)N1Cc2cccn2Cc2ccccc21 10.1021/jm980179c
44378702 238778 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 657 7 1 5 7.8 CN(C)C1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL350869 238778 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 657 7 1 5 7.8 CN(C)C1CCN(Cc2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
9939024 260439 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 622 9 1 6 7.1 CN1CCCN(CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL369832 260439 0 None None None Human 8.7 pIC50 = 8.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 622 9 1 6 7.1 CN1CCCN(CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
10503858 470389 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 453 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(C)c1 10.1021/jm980179c
CHEMBL81133 470389 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 453 3 1 3 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(C)c1 10.1021/jm980179c
44378703 120203 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 697 7 1 5 8.7 O=C(Nc1ccc(C(=O)N2Cc3ccc(CN4CCC(N5CCCCC5)CC4)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
CHEMBL165200 120203 0 None None None Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 697 7 1 5 8.7 O=C(Nc1ccc(C(=O)N2Cc3ccc(CN4CCC(N5CCCCC5)CC4)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
172997 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
2238 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
CHEMBL49429 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
DB06666 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(00)00084-6
132088270 412483 0 None None None Human 8.6 pIC50 = 8.6 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 540 7 1 9 3.8 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 nan
CHEMBL5819244 412483 0 None None None Human 8.6 pIC50 = 8.6 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 540 7 1 9 3.8 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 nan
172997 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
2238 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
CHEMBL49429 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
DB06666 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1021/jm980179c
172997 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
2238 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
CHEMBL49429 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
DB06666 4754 54 None None None Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(03)00388-3
9935001 106363 0 None None None Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 483 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159823 106363 0 None None None Rat 8.6 pIC50 = 8.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 483 4 1 3 6.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
9874047 238613 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 631 9 1 5 7.3 CN(C)CCN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
CHEMBL349237 238613 0 None None None Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 631 9 1 5 7.3 CN(C)CCN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
10459252 105870 0 None None None Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159359 105870 0 None None None Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 517 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
132103227 425124 0 None None None Human 8.6 pIC50 = 8.6 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 540 7 1 9 3.8 CC(O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(CC(=O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 nan
CHEMBL5850651 425124 0 None None None Human 8.6 pIC50 = 8.6 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 540 7 1 9 3.8 CC(O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(CC(=O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 nan
44352776 45435 0 None None None Human 7.7 pIC50 = 7.7 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptor at 0.2 uMAbility to displace [3H]arginine vasopressin in cloned human V2 receptor at 0.2 uM
ChEMBL 560 7 1 7 6.2 O=C(Nc1ccc(C(=O)N2CCC(CCn3cnnn3)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL131727 45435 0 None None None Human 7.7 pIC50 = 7.7 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptor at 0.2 uMAbility to displace [3H]arginine vasopressin in cloned human V2 receptor at 0.2 uM
ChEMBL 560 7 1 7 6.2 O=C(Nc1ccc(C(=O)N2CCC(CCn3cnnn3)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
44336404 220478 0 None None None Human 7.7 pIC50 = 7.7 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL326225 220478 0 None None None Human 7.7 pIC50 = 7.7 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 568 7 2 4 5.4 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
10838492 27718 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3cc(Cl)cc(Cl)c3)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL119318 27718 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 481 4 1 3 6.3 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3cc(Cl)cc(Cl)c3)cc2)c2ccccc21 10.1021/jm960133o
9826033 120258 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL165670 120258 0 None None None Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 471 4 2 2 6.7 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
11239468 258582 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL368353 258582 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11167861 259238 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL368791 259238 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
10578000 333180 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
CHEMBL435331 333180 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
11386922 123207 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175212 123207 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 525 6 1 5 6.7 COc1cc(C(=O)N2CCCC(N(C)C)c3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
9939929 332361 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL430083 332361 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
10548464 39274 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc(Cl)c1 10.1021/jm960133o
CHEMBL121455 39274 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc(Cl)c1 10.1021/jm960133o
10666852 222522 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL331164 222522 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
11270497 123206 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 435 4 2 2 5.9 O=C(Nc1ccc(C(=O)N2CCCCc3[nH]ccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175211 123206 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 435 4 2 2 5.9 O=C(Nc1ccc(C(=O)N2CCCCc3[nH]ccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
11418441 333890 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 410 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1Cl 10.1021/jm00137a004
CHEMBL441498 333890 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 410 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1Cl 10.1021/jm00137a004
11272841 123564 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL176146 123564 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 550 7 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCCC3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL2332717 485344 0 None None None Human 5.7 pIC50 = 5.7 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression competition binding assay
ChEMBL 772 11 10 10 -2.2 NC(=O)CC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CNC(=O)[C@H](CC(N)=O)NC1=O 10.1016/j.bmcl.2012.12.041
10156521 144688 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccccc1-c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/j.bmcl.2005.08.007
CHEMBL198931 144688 0 None None None Human 5.7 pIC50 = 5.7 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccccc1-c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/j.bmcl.2005.08.007
10347928 237266 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
CHEMBL341289 237266 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
10052468 44972 0 None None None Rat 4.7 pIC50 = 4.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 522 6 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)/C=C/c1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL131235 44972 0 None None None Rat 4.7 pIC50 = 4.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 522 6 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)/C=C/c1c[nH]cn1)C2 10.1021/jm00077a002
135177396 462576 0 None None None Human 4.7 pIC50 = 4.7 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 442 6 0 8 3.6 COCc1nnc(N2CC(n3cc(Cl)c4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL6041216 462576 0 None None None Human 4.7 pIC50 = 4.7 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 442 6 0 8 3.6 COCc1nnc(N2CC(n3cc(Cl)c4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
18917500 370682 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 423 3 2 5 3.9 Nc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL49392 370682 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 423 3 2 5 3.9 Nc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
10667727 25314 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c(C)c1 10.1021/jm960133o
CHEMBL117566 25314 0 None None None Rat 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 3 1 2 5.1 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c(C)c1 10.1021/jm960133o
9935694 120182 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 499 4 1 3 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4cn(C)c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
CHEMBL165183 120182 0 None None None Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 499 4 1 3 7.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCc4cn(C)c5cccc3c45)cc2)cc1 10.1016/s0960-894x(02)01059-4
10784361 234377 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
CHEMBL335040 234377 0 None None None Human 6.7 pIC50 = 6.7 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
10834036 27888 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 4 1 3 4.5 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119442 27888 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 4 1 3 4.5 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
10458629 42820 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 4 1 4 3.4 CC1NC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
CHEMBL128712 42820 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 4 1 4 3.4 CC1NC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
10029477 44560 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 514 5 2 5 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CN)C1=O)C2 10.1021/jm00077a002
CHEMBL130905 44560 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 514 5 2 5 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CN)C1=O)C2 10.1021/jm00077a002
10051081 235777 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 485 4 1 4 3.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CNC1=O)C2 10.1021/jm00077a002
CHEMBL338383 235777 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 485 4 1 4 3.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CNC1=O)C2 10.1021/jm00077a002
10256281 42763 0 None None None Rat 4.7 pIC50 = 4.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 7 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL128422 42763 0 None None None Rat 4.7 pIC50 = 4.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 7 2 4 4.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCc1c[nH]cn1)C2 10.1021/jm00077a002
56848626 290482 0 None None None Human 7.7 pIC50 = 7.7 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 557 9 2 7 4.2 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(Cc2ccccc2F)c1=O)c1ccccc1Cl nan
CHEMBL3900528 290482 0 None None None Human 7.7 pIC50 = 7.7 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 557 9 2 7 4.2 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(Cc2ccccc2F)c1=O)c1ccccc1Cl nan
10766187 27119 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 455 6 1 3 6.1 CCCN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118863 27119 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 455 6 1 3 6.1 CCCN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
11798757 469207 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(03)00388-3
CHEMBL71305 469207 0 None None None Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(03)00388-3
10737018 64277 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 356 5 1 2 5.5 CCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL139415 64277 0 None None None Human 7.7 pIC50 = 7.7 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 356 5 1 2 5.5 CCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
44374839 238846 0 None None None Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL351587 238846 0 None None None Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
44352373 46150 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 543 8 3 5 3.4 CC(C)C[C@H](N)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL132389 46150 0 None None None Rat 5.7 pIC50 = 5.7 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 543 8 3 5 3.4 CC(C)C[C@H](N)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
8105663 27684 2 None None None Rat 4.7 pIC50 = 4.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccccc1C(=O)N1CCCc2ccccc21)c1ccccc1 10.1021/jm960133o
CHEMBL119291 27684 2 None None None Rat 4.7 pIC50 = 4.7 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccccc1C(=O)N1CCCc2ccccc21)c1ccccc1 10.1021/jm960133o
44336379 217038 0 None None None Human 7.6 pIC50 = 7.6 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL318083 217038 0 None None None Human 7.6 pIC50 = 7.6 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 582 8 2 4 5.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCCN(C)C)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
86690920 292266 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 548 6 1 7 5.5 O=c1n(Cc2cnc(-c3ccccc3C(F)(F)F)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3915055 292266 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 548 6 1 7 5.5 O=c1n(Cc2cnc(-c3ccccc3C(F)(F)F)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
69940395 295757 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 514 6 1 7 5.1 O=c1n(Cc2ncc(-c3ccccc3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3943019 295757 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 514 6 1 7 5.1 O=c1n(Cc2ncc(-c3ccccc3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
87388676 298502 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 533 6 1 8 4.4 O=c1n(Cc2nc(-c3ccccc3C(F)(F)F)no2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3965602 298502 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 533 6 1 8 4.4 O=c1n(Cc2nc(-c3ccccc3C(F)(F)F)no2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
69939726 291767 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 1 8 3.6 O=c1n(Cc2cn(-c3ccccc3Cl)nn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3911148 291767 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 1 8 3.6 O=c1n(Cc2cn(-c3ccccc3Cl)nn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
2173 6017 25 None None None Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
3038506 6017 25 None None None Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
CHEMBL332447 6017 25 None None None Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
DB05838 6017 25 None None None Rat 6.6 pIC50 = 6.6 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
19699114 106587 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 434 3 1 5 4.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)C3CCCCC3)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL160029 106587 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 434 3 1 5 4.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)C3CCCCC3)cc1)CC2 10.1016/s0960-894x(00)00084-6
14981577 160376 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 636 11 2 7 3.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCCCC2)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112900 160376 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 636 11 2 7 3.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCCCC2)C3(C)C)CC1 10.1021/jm00031a004
2241 4522 5 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00099a019
9810632 4522 5 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00099a019
CHEMBL127686 4522 5 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00099a019
44273425 199139 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.6 C[C@@H](O)CNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL279281 199139 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.6 C[C@@H](O)CNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
44272990 199743 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
44273369 199743 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL283524 199743 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL283994 199743 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 500 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](O)C1=O)C2 10.1016/0960-894X(94)00469-V
10007685 198858 0 None None None Rat 4.6 pIC50 = 4.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 548 7 2 4 4.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)c1ccccc1)C2 10.1021/jm00077a002
CHEMBL276906 198858 0 None None None Rat 4.6 pIC50 = 4.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 548 7 2 4 4.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)c1ccccc1)C2 10.1021/jm00077a002
44374839 238846 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL351587 238846 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 442 3 1 5 4.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cn(C)nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
10716676 219948 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 413 4 2 3 4.9 CNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL324488 219948 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 413 4 2 3 4.9 CNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
44293784 371120 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 444 3 1 4 4.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(F)ccc1F 10.1016/s0960-894x(99)00279-6
CHEMBL49657 371120 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 444 3 1 4 4.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(F)ccc1F 10.1016/s0960-894x(99)00279-6
71450903 160377 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 614 12 3 9 0.8 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)N(CO)CO)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112901 160377 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 614 12 3 9 0.8 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)N(CO)CO)C3(C)C)CC1 10.1021/jm00031a004
71449109 160378 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 565 8 2 6 2.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCS(C)(=O)=O)C2 10.1021/jm00031a004
CHEMBL2112902 160378 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 565 8 2 6 2.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCS(C)(=O)=O)C2 10.1021/jm00031a004
10257352 160035 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
10483039 160035 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL2111851 160035 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL2112666 160035 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 8 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
10326385 311623 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 609 7 2 8 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CC(=O)Nc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
CHEMBL405016 311623 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 609 7 2 8 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CC(=O)Nc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
146681949 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
2168 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
2810 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
644077 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
CHEMBL373742 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
DB00067 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
P01185 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
P01186 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
P35455 8624 35 None None None Human 6.6 pIC50 = 6.6 Binding
Binding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assayBinding affinity to vasopression V2 receptor (unknown origin) on isolated cell membrane by vasopression-self competition binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmcl.2012.12.041
10647295 219811 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 452 5 1 4 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC#N)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL323802 219811 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 452 5 1 4 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)CC#N)c3ccccc32)cc1 10.1021/jm960133o
44212554 213401 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 432 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL308741 213401 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 432 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10622282 27425 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm960133o
CHEMBL119087 27425 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm960133o
22405331 272778 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 400 2 0 2 5.6 O=C(c1ccc(-c2cc(F)cc(F)c2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL372766 272778 0 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 400 2 0 2 5.6 O=C(c1ccc(-c2cc(F)cc(F)c2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
44273473 144997 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 542 5 0 6 3.2 CC(=O)OC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL20002 144997 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 542 5 0 6 3.2 CC(=O)OC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
10392579 235593 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 542 6 1 5 3.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CC(=O)O)C1=O)C2 10.1021/jm00077a002
CHEMBL337221 235593 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 542 6 1 5 3.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CC(=O)O)C1=O)C2 10.1021/jm00077a002
44352455 333293 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 701 12 4 8 1.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C(CCS(C)(=O)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL436189 333293 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 701 12 4 8 1.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C(CCS(C)(=O)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
2812 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
719 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
DB00257 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
135177395 449291 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 409 6 0 8 3.3 COCc1nnc(N2CC(c3coc4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
CHEMBL6003024 449291 0 None None None Human 4.6 pIC50 = 4.6 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 409 6 0 8 3.3 COCc1nnc(N2CC(c3coc4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
44335386 217633 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
CHEMBL319433 217633 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
44352171 44665 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 7 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)C1=CCC(=O)N=C1)C2 10.1021/jm00077a002
CHEMBL130993 44665 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 7 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)C1=CCC(=O)N=C1)C2 10.1021/jm00077a002
10366192 235590 0 None None None Rat 4.6 pIC50 = 4.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 444 4 1 3 3.6 CC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL337212 235590 0 None None None Rat 4.6 pIC50 = 4.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 444 4 1 3 3.6 CC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
53378951 291527 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 507 6 1 5 5.7 O=c1n(Cc2cccc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
CHEMBL3909196 291527 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 507 6 1 5 5.7 O=c1n(Cc2cccc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
10837161 26194 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 447 4 1 3 5.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3Cl)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118270 26194 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 447 4 1 3 5.6 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3Cl)cc2)c2ccccc21 10.1021/jm960133o
10716675 233907 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 413 4 1 3 5.0 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL334225 233907 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 413 4 1 3 5.0 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3)cc2)c2ccccc21 10.1021/jm960133o
14981578 160373 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 638 11 2 8 2.3 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCOCC2)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112897 160373 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 638 11 2 8 2.3 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)NC2CCOCC2)C3(C)C)CC1 10.1021/jm00031a004
10074681 235917 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 4 0 4 3.4 CN1CC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
CHEMBL339132 235917 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 499 4 0 4 3.4 CN1CC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
2812 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
719 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
DB00257 19119 69 None None None Human 5.6 pIC50 = 5.6 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
44332207 216898 0 None None None Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.02.103
CHEMBL316958 216898 0 None None None Human 6.6 pIC50 = 6.6 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 504 3 1 2 7.6 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.02.103
53378730 309100 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 548 7 1 7 5.4 O=c1n(Cc2nnc(Cc3ccccc3C(F)(F)F)[nH]2)nc(-c2ccc(Cl)s2)n1Cc1ccccc1F nan
CHEMBL3975038 309100 0 None None None Human 7.6 pIC50 = 7.6 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 548 7 1 7 5.4 O=c1n(Cc2nnc(Cc3ccccc3C(F)(F)F)[nH]2)nc(-c2ccc(Cl)s2)n1Cc1ccccc1F nan
10692266 38050 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 398 3 1 2 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL119806 38050 0 None None None Rat 7.6 pIC50 = 7.6 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 398 3 1 2 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCCc3ccccc32)cc1 10.1021/jm960133o
44335356 19563 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL106229 19563 0 None None None Human 7.6 pIC50 = 7.6 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
44352185 45253 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 673 11 3 7 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL131477 45253 0 None None None Rat 6.6 pIC50 = 6.6 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 673 11 3 7 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
44272997 143949 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
9805972 143949 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL19658 143949 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL276990 143949 0 None None None Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 499 4 1 5 2.6 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@H](N)C1=O)C2 10.1016/0960-894X(94)00469-V
10715974 26196 2 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL118271 26196 2 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/jm960133o
10835094 26357 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 404 3 1 2 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
CHEMBL118387 26357 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 404 3 1 2 5.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
10598596 27203 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 5 2 3 5.3 CCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118922 27203 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 5 2 3 5.3 CCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
10743970 222523 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 499 7 1 5 5.2 CCOC(=O)CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL331173 222523 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 499 7 1 5 5.2 CCOC(=O)CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
22099567 201469 0 None None None Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [3H]AVP binding to rat V2 receptorIn vitro inhibition of [3H]AVP binding to rat V2 receptor
ChEMBL 457 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00278-4
CHEMBL296814 201469 0 None None None Rat 7.5 pIC50 = 7.5 Binding
In vitro inhibition of [3H]AVP binding to rat V2 receptorIn vitro inhibition of [3H]AVP binding to rat V2 receptor
ChEMBL 457 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00278-4
23598560 18799 0 None None None Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 512 4 1 2 7.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.02.103
CHEMBL101678 18799 0 None None None Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 512 4 1 2 7.9 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.02.103
44309960 469202 1 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cccc(Cl)c1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL71282 469202 1 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1cccc(Cl)c1Cl 10.1016/s0960-894x(03)00388-3
15307971 469455 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 418 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL72945 469455 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 418 3 1 2 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
18917519 370589 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 525 7 0 5 5.1 Cc1ccc(F)cc1C(=O)N(CCCN(C)C)c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL49323 370589 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 525 7 0 5 5.1 Cc1ccc(F)cc1C(=O)N(CCCN(C)C)c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
14981575 160372 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 582 10 1 7 2.1 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)N(C)C)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112896 160372 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 582 10 1 7 2.1 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@H](CCS(C)(=O)=O)N(C)C)C3(C)C)CC1 10.1021/jm00031a004
10483940 236124 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 616 9 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)c1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL339497 236124 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 616 9 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)c1c[nH]cn1)C2 10.1021/jm00077a002
9868852 156960 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 459 2 1 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Br)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL203739 156960 0 None None None Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 459 2 1 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Br)c2)n1 10.1016/j.bmcl.2005.10.107
56848622 294632 0 None None None Human 8.5 pIC50 = 8.5 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 595 9 3 8 3.3 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
CHEMBL3933782 294632 0 None None None Human 8.5 pIC50 = 8.5 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 595 9 3 8 3.3 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
44293763 201631 0 None None None Rat 8.5 pIC50 = 8.5 Binding
In vitro inhibition of (P[3H]-AVP binding towards isolated rat kidney medullary Vasopre ssin V2 receptorIn vitro inhibition of (P[3H]-AVP binding towards isolated rat kidney medullary Vasopre ssin V2 receptor
ChEMBL 422 3 1 4 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL297990 201631 0 None None None Rat 8.5 pIC50 = 8.5 Binding
In vitro inhibition of (P[3H]-AVP binding towards isolated rat kidney medullary Vasopre ssin V2 receptorIn vitro inhibition of (P[3H]-AVP binding towards isolated rat kidney medullary Vasopre ssin V2 receptor
ChEMBL 422 3 1 4 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
9826254 328298 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL418890 328298 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(03)00388-3
11763684 259245 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368818 259245 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 650 9 1 6 7.0 CN1CCCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
9939929 332361 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL430083 332361 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 664 10 1 6 7.4 CN(C)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
9826254 328298 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL418890 328298 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
9826254 328298 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL418890 328298 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
44374781 106394 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
CHEMBL159856 106394 0 None None None Rat 8.5 pIC50 = 8.5 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 486 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2CCCCc3sc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00084-6
9826254 328298 0 None None None Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL418890 328298 0 None None None Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
9826254 328298 0 None None None Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL418890 328298 0 None None None Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 475 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1016/s0960-894x(00)00084-6
69940338 297286 0 None None None Human 8.5 pIC50 = 8.5 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cn(-c3ccccc3Cl)cn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3955416 297286 0 None None None Human 8.5 pIC50 = 8.5 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cn(-c3ccccc3Cl)cn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
146681949 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
2168 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
2810 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
644077 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
CHEMBL373742 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
DB00067 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
P01185 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
P01186 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
P35455 8624 35 None None None Pig 8.5 pIC50 = 8.5 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/S0960-894X(97)00050-4
44374802 238698 0 None None None Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
CHEMBL350089 238698 0 None None None Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 442 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
20825285 218774 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 595 4 1 3 8.2 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)c(Cl)c2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL321561 218774 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 595 4 1 3 8.2 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)c(Cl)c2)cc1 10.1016/s0960-894x(02)00649-2
10578460 123198 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175182 123198 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11190868 123328 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
CHEMBL175930 123328 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
11190868 123328 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
CHEMBL175930 123328 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 482 5 1 4 6.7 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCCc2sccc21 10.1021/jm00137a004
11239468 258582 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL368353 258582 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 704 10 1 6 8.3 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1OCCCC(=O)N1CCC(N2CCCCC2)CC1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11167861 259238 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL368791 259238 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 495 5 1 4 6.7 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
56848686 291287 0 None None None Human 6.5 pIC50 = 6.5 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 653 9 2 8 6.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)s2)n(Cc2ccccc2F)c1=O)c1ccccc1C(F)(F)F nan
CHEMBL3907257 291287 0 None None None Human 6.5 pIC50 = 6.5 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 653 9 2 8 6.0 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)s2)n(Cc2ccccc2F)c1=O)c1ccccc1C(F)(F)F nan
10762739 233399 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL333135 233399 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOCc3ccccc32)cc1 10.1021/jm960133o
44404614 330619 0 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
CHEMBL424663 330619 0 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 378 2 0 2 5.7 Cc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
119369 5304 49 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
2197 5304 49 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
4004 5304 49 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
CHEMBL420762 5304 49 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
11476070 123238 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 436 4 1 3 6.2 O=C(Nc1ccc(C(=O)N2CCCCc3occc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175411 123238 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 436 4 1 3 6.2 O=C(Nc1ccc(C(=O)N2CCCCc3occc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
137484925 405343 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 420 3 0 6 4.0 CCN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
CHEMBL5744732 405343 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 420 3 0 6 4.0 CCN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
137485320 405640 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 464 3 0 6 4.7 CC1(N2Cc3cc(Cl)ccc3-n3c(nnc3C3CC4(C3)CN(c3ccc(F)cn3)C4)C2)CC1 nan
CHEMBL5747556 405640 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 464 3 0 6 4.7 CC1(N2Cc3cc(Cl)ccc3-n3c(nnc3C3CC4(C3)CN(c3ccc(F)cn3)C4)C2)CC1 nan
137485061 409182 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 456 4 0 6 4.3 FC(F)CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
CHEMBL5783103 409182 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 456 4 0 6 4.3 FC(F)CN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
137484963 412090 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 432 3 0 6 4.2 Clc1ccc2c(c1)CN(C1CC1)Cc1nnc(C3CC4(C3)CN(c3ccccn3)C4)n1-2 nan
CHEMBL5815032 412090 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 432 3 0 6 4.2 Clc1ccc2c(c1)CN(C1CC1)Cc1nnc(C3CC4(C3)CN(c3ccccn3)C4)n1-2 nan
137485029 413448 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 482 3 0 7 4.3 CCOC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL5829896 413448 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 482 3 0 7 4.3 CCOC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137485455 413454 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 492 3 0 6 4.6 CC1c2nnc(C3CC4(C3)CN(c3ccccn3)C4)n2-c2ccc(Cl)cc2CN1C(=O)C1(F)CC1 nan
CHEMBL5829963 413454 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 492 3 0 6 4.6 CC1c2nnc(C3CC4(C3)CN(c3ccccn3)C4)n2-c2ccc(Cl)cc2CN1C(=O)C1(F)CC1 nan
137485333 427110 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 512 3 0 6 5.0 CC1c2nnc(C3CC4(C3)CN(c3ccc(F)cn3)C4)n2-c2ccc(Cl)cc2CN1C(=O)C(C)(C)F nan
CHEMBL5872268 427110 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 512 3 0 6 5.0 CC1c2nnc(C3CC4(C3)CN(c3ccc(F)cn3)C4)n2-c2ccc(Cl)cc2CN1C(=O)C(C)(C)F nan
137484964 428343 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 3 0 6 4.6 CC(C)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL5886591 428343 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 3 0 6 4.6 CC(C)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137484954 429118 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 468 2 0 7 3.9 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL5894664 429118 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 468 2 0 7 3.9 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137485329 432207 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 478 2 0 7 4.7 COC(=O)N1Cc2cc(Cl)ccc2-n2c(C3CC4(C3)CN(c3cccc(C)n3)C4)nnc2C1C nan
CHEMBL5925462 432207 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 478 2 0 7 4.7 COC(=O)N1Cc2cc(Cl)ccc2-n2c(C3CC4(C3)CN(c3cccc(C)n3)C4)nnc2C1C nan
137484970 444058 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 438 3 0 6 4.2 CCN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL5946775 444058 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 438 3 0 6 4.2 CCN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137484985 446800 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 2 0 6 3.7 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL5976379 446800 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 2 0 6 3.7 CC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137485118 447598 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 514 4 0 7 4.6 CC(CF)OC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL5985111 447598 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 514 4 0 7 4.6 CC(CF)OC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137485028 450320 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 450 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
CHEMBL6014034 450320 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 450 2 0 7 3.8 COC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
137484960 451853 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 466 3 0 6 4.1 CCC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL6030339 451853 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 466 3 0 6 4.1 CCC(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137485130 464901 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 470 3 0 6 3.8 O=C(C(F)F)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
CHEMBL6065033 464901 0 None None None Human 6.5 pIC50 = 6.5 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 470 3 0 6 3.8 O=C(C(F)F)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
44273426 158748 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.6 C[C@H](CO)NC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL20757 158748 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.6 C[C@H](CO)NC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
44352311 42809 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](Cc1c[nH]cn1)NC(=O)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL128652 42809 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](Cc1c[nH]cn1)NC(=O)CCC(N)=O)C2 10.1021/jm00077a002
44352372 44491 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 558 9 4 6 1.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL130848 44491 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 558 9 4 6 1.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00077a002
10460052 45953 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 544 8 2 5 2.3 CN(C)CC(=O)NCC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL132211 45953 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 544 8 2 5 2.3 CN(C)CC(=O)NCC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
71449094 160290 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 581 8 3 7 1.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@](O)(CNC(=O)C(N)CS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL2112663 160290 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 581 8 3 7 1.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@](O)(CNC(=O)C(N)CS(C)(=O)=O)C2 10.1021/jm00077a002
10392298 235699 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 532 8 2 6 2.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CC[N+](=O)[O-])C2 10.1021/jm00077a002
CHEMBL337888 235699 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 532 8 2 6 2.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CC[N+](=O)[O-])C2 10.1021/jm00077a002
9982888 333139 0 None None None Rat 4.5 pIC50 = 4.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 486 6 2 4 3.5 CC(=O)NCC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL435009 333139 0 None None None Rat 4.5 pIC50 = 4.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 486 6 2 4 3.5 CC(=O)NCC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
44273259 155213 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 1 6 2.5 CN(CCO)C1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL20171 155213 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 1 6 2.5 CN(CCO)C1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
11793558 62047 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 370 6 1 2 5.9 CCCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL137500 62047 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 370 6 1 2 5.9 CCCCCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
14981576 160370 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 610 12 1 7 2.9 CCN(CC)[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1021/jm00031a004
CHEMBL2112894 160370 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 610 12 1 7 2.9 CCN(CC)[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1021/jm00031a004
21467167 123301 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175813 123301 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL1790937 484815 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Ability to inhibit AVP stimulation of adenylate cyclase activity in the rat kidney medulla (AVP-V2) receptorAbility to inhibit AVP stimulation of adenylate cyclase activity in the rat kidney medulla (AVP-V2) receptor
ChEMBL 755 6 5 7 1.9 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
67412781 310330 0 None None None Human 7.5 pIC50 = 7.5 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 499 6 1 8 4.0 O=c1n(Cc2nnc(-c3ccccc3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3986461 310330 0 None None None Human 7.5 pIC50 = 7.5 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 499 6 1 8 4.0 O=c1n(Cc2nnc(-c3ccccc3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10692311 328996 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 399 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL420880 328996 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 399 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N)c3ccccc32)cc1 10.1021/jm960133o
53378731 309821 0 None None None Human 7.5 pIC50 = 7.5 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 556 8 2 9 3.3 O=C(O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
CHEMBL3981686 309821 0 None None None Human 7.5 pIC50 = 7.5 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 556 8 2 9 3.3 O=C(O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
10591515 237669 0 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 316 2 0 2 4.5 O=C(c1ccc(-n2cccc2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL342251 237669 0 None None None Human 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 316 2 0 2 4.5 O=C(c1ccc(-n2cccc2)cc1)N1CCCCc2ccccc21 10.1021/jm000108p
44352164 42753 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 4 1 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C3CC(O)CN3C1=O)C2 10.1021/jm00077a002
CHEMBL128383 42753 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 4 1 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C3CC(O)CN3C1=O)C2 10.1021/jm00077a002
18917554 372927 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 497 5 1 5 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL51645 372927 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 497 5 1 5 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
21837085 202343 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 421 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL303176 202343 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 421 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
2173 6017 25 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
3038506 6017 25 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
CHEMBL332447 6017 25 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
DB05838 6017 25 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/jm020133q
CHEMBL126765 484594 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 781 9 5 8 2.0 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCN)NC(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00099a019
10483940 236124 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 616 9 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)c1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL339497 236124 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 616 9 2 6 3.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(CCS(C)(=O)=O)c1c[nH]cn1)C2 10.1021/jm00077a002
44433367 180676 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 489 3 1 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3C=CC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
CHEMBL237772 180676 0 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 489 3 1 3 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3C=CC(=O)N3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2007.08.053
11157078 194607 8 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL249741 194607 8 None None None Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
10758700 58555 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 328 3 1 2 4.8 CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL134525 58555 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 328 3 1 2 4.8 CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
19699060 118959 0 None None None Rat 6.5 pIC50 = 6.5 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
CHEMBL162588 118959 0 None None None Rat 6.5 pIC50 = 6.5 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 466 3 2 4 5.4 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(00)00084-6
44352442 328436 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 567 8 2 5 3.5 CN(C)[C@H](Cc1c[nH]cn1)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL419973 328436 0 None None None Rat 5.5 pIC50 = 5.5 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 567 8 2 5 3.5 CN(C)[C@H](Cc1c[nH]cn1)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
9937535 116561 1 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788221 116561 1 None None None Human 6.5 pIC50 = 6.5 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
21837086 334026 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 425 3 1 3 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1F 10.1016/s0960-894x(03)00388-3
CHEMBL442743 334026 0 None None None Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 425 3 1 3 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1F 10.1016/s0960-894x(03)00388-3
10519373 235573 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 314 2 1 2 4.4 CNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL337098 235573 0 None None None Human 7.5 pIC50 = 7.5 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 314 2 1 2 4.4 CNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
14981574 160374 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1021/jm00031a004
CHEMBL2112898 160374 0 None None None Rat 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1CC2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1021/jm00031a004
10483105 174420 1 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1016/j.bmcl.2012.10.116
CHEMBL2391300 174420 1 None None None Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1016/j.bmcl.2012.10.116
56848687 297143 0 None None None Human 5.5 pIC50 = 5.5 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 581 11 2 9 2.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NS(C)(=O)=O)c2ccccc2C(F)(F)F)c1=O nan
CHEMBL3954357 297143 0 None None None Human 5.5 pIC50 = 5.5 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 581 11 2 9 2.5 COCCn1c(-c2ccc(Cl)s2)nn(CC(=O)NCC(NS(C)(=O)=O)c2ccccc2C(F)(F)F)c1=O nan
19699076 238879 0 None None None Rat 7.4 pIC50 = 7.4 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 500 3 2 4 6.0 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1cc(Cl)ccc1F 10.1016/s0960-894x(00)00084-6
CHEMBL351970 238879 0 None None None Rat 7.4 pIC50 = 7.4 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 500 3 2 4 6.0 O=C(Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1)c1cc(Cl)ccc1F 10.1016/s0960-894x(00)00084-6
44352441 44539 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1ccccn1)C2 10.1021/jm00077a002
CHEMBL130887 44539 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1ccccn1)C2 10.1021/jm00077a002
3514 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
5280343 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
DB04216 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
19699133 238630 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
CHEMBL349506 238630 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat V2 receptorBinding affinity to rat V2 receptor
ChEMBL 496 3 1 5 5.9 Cn1cc2c(n1)-c1sccc1N(C(=O)c1ccc(NC(=O)c3ccc(Cl)cc3Cl)cc1)CC2 10.1016/s0960-894x(00)00084-6
44357890 333091 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards rat Vasopressin V2 receptor after peroral administration of the compoundBinding affinity towards rat Vasopressin V2 receptor after peroral administration of the compound
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
CHEMBL434654 333091 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Binding affinity towards rat Vasopressin V2 receptor after peroral administration of the compoundBinding affinity towards rat Vasopressin V2 receptor after peroral administration of the compound
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
44332272 216875 0 None None None Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 450 3 1 2 6.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)c1 10.1016/j.bmcl.2004.02.103
CHEMBL316849 216875 0 None None None Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 450 3 1 2 6.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCC4(C=CCCC4)Cc4ccccc43)cc2)c1 10.1016/j.bmcl.2004.02.103
11351397 123768 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
CHEMBL176264 123768 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
CHEMBL339118 487010 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 740 6 2 6 3.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
44352496 43411 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 538 4 1 5 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C3CCC(=N)N3C1=O)C2 10.1021/jm00077a002
CHEMBL129983 43411 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 538 4 1 5 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C3CCC(=N)N3C1=O)C2 10.1021/jm00077a002
23598598 19306 0 None None None Human 7.4 pIC50 = 7.4 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 19306 0 None None None Human 7.4 pIC50 = 7.4 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
23598600 19703 0 None None None Human 7.4 pIC50 = 7.4 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL106938 19703 0 None None None Human 7.4 pIC50 = 7.4 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 594 7 2 4 5.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
11070458 37960 5 None None None Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
CHEMBL125878 37960 5 None None None Rat 6.4 pIC50 = 6.4 Binding
Binding affinity against Vasopressin V2 receptor was determined in Brattleboro ratsBinding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
9801970 277994 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2005.10.107
CHEMBL381763 277994 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2005.10.107
44332168 18833 0 None None None Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 436 3 1 2 6.3 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1 10.1016/j.bmcl.2004.02.103
CHEMBL101935 18833 0 None None None Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 436 3 1 2 6.3 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1 10.1016/j.bmcl.2004.02.103
9799174 277852 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 364 2 0 2 5.4 O=C(c1ccc(-c2ccccc2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL381248 277852 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 364 2 0 2 5.4 O=C(c1ccc(-c2ccccc2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
44273077 199110 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
44273316 199110 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL279022 199110 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL281361 199110 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 589 7 1 5 4.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C[C@@H](NCc3ccccc3)C1=O)C2 10.1016/0960-894X(94)00469-V
71720517 177883 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 177883 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
3514 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
5280343 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
DB04216 371491 78 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
44293777 371329 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1c(F)cccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL49824 371329 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 460 3 1 4 5.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1c(F)cccc1Cl 10.1016/s0960-894x(99)00279-6
10837633 203074 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1021/jm980179c
CHEMBL306970 203074 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1021/jm980179c
10719289 470460 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1Cl 10.1021/jm980179c
CHEMBL81755 470460 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 473 3 1 3 6.1 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1Cl 10.1021/jm980179c
44214518 238605 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 561 5 2 4 7.0 O=C(Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
CHEMBL349141 238605 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 561 5 2 4 7.0 O=C(Nc1ccc(C(=O)N2Cc3ccc(C(=O)O)n3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
10551037 469159 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL70981 469159 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
9954905 202019 3 None None None Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptorIn vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
CHEMBL300946 202019 3 None None None Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptorIn vitro inhibition of (P[3H]-AVP binding to isolated rat kidney medullary V2 receptor
ChEMBL 440 3 1 4 4.8 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1 10.1016/s0960-894x(99)00279-6
10837633 203074 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL306970 203074 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 459 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccc(F)cc1Cl 10.1016/s0960-894x(03)00388-3
10551037 469159 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL70981 469159 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 439 3 1 3 5.4 Cc1c(F)cccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10764664 469289 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71797 469289 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10231366 19293 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.7 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL104796 19293 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.7 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
9915472 327811 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL443498 327811 0 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
11422294 125044 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL177885 125044 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
10764664 469289 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
CHEMBL71797 469289 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 421 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1021/jm980179c
10495509 234114 1 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
CHEMBL334376 234114 1 None None None Human 8.4 pIC50 = 8.4 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 314 1 1 2 4.2 Cc1cc(N)ccc1C(=O)N1CCCCc2cc(Cl)ccc21 10.1021/jm000108p
10814200 328476 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 469 3 1 3 6.2 Cc1ccc(C)c(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/jm980179c
CHEMBL420216 328476 0 None None None Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 469 3 1 3 6.2 Cc1ccc(C)c(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/jm980179c
69940338 297286 0 None None None Human 8.4 pIC50 = 8.4 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cn(-c3ccccc3Cl)cn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3955416 297286 0 None None None Human 8.4 pIC50 = 8.4 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cn(-c3ccccc3Cl)cn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
44293778 201737 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 476 3 1 4 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL298911 201737 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 476 3 1 4 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Cl)ccc1Cl 10.1016/s0960-894x(99)00279-6
69939726 291767 0 None None None Human 8.4 pIC50 = 8.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 1 8 3.6 O=c1n(Cc2cn(-c3ccccc3Cl)nn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3911148 291767 0 None None None Human 8.4 pIC50 = 8.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 1 8 3.6 O=c1n(Cc2cn(-c3ccccc3Cl)nn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10742418 214204 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
CHEMBL310416 214204 0 None None None Rat 8.4 pIC50 = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 455 3 1 3 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/jm980179c
53379068 279520 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 551 7 2 6 5.4 O=C(O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
CHEMBL3889504 279520 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 551 7 2 6 5.4 O=C(O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
10527151 202265 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm980179c
CHEMBL302709 202265 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm980179c
132102856 462126 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 540 7 1 9 3.8 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1ccccc1Cl nan
CHEMBL6036527 462126 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 540 7 1 9 3.8 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1ccccc1Cl nan
86690918 298457 0 None None None Human 7.4 pIC50 = 7.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 547 6 1 6 6.4 O=c1n(Cc2ccc(-c3cccc(Cl)c3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3965329 298457 0 None None None Human 7.4 pIC50 = 7.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 547 6 1 6 6.4 O=c1n(Cc2ccc(-c3cccc(Cl)c3Cl)s2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
69940091 294609 0 None None None Human 6.4 pIC50 = 6.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2ccnc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3933604 294609 0 None None None Human 6.4 pIC50 = 6.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 508 6 1 6 5.1 O=c1n(Cc2ccnc(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10548204 26653 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 4 1 3 4.5 COc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
CHEMBL118562 26653 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 386 4 1 3 4.5 COc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
10762667 27081 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 385 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL118829 27081 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 385 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCN(C)c3ccccc32)cc1 10.1021/jm960133o
71720517 177883 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 177883 0 None None None Human 6.4 pIC50 = 6.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
1307424 26703 11 None None None Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 356 3 1 2 4.5 O=C(Nc1cccc(C(=O)N2CCCc3ccccc32)c1)c1ccccc1 10.1021/jm960133o
CHEMBL118595 26703 11 None None None Rat 4.4 pIC50 = 4.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 356 3 1 2 4.5 O=C(Nc1cccc(C(=O)N2CCCc3ccccc32)c1)c1ccccc1 10.1021/jm960133o
CHEMBL419793 488423 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)
ChEMBL 796 10 5 7 2.8 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10595449 24803 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 372 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOc3ccccc32)cc1 10.1021/jm960133o
CHEMBL116820 24803 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 372 3 1 3 4.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCOc3ccccc32)cc1 10.1021/jm960133o
44272960 145473 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 527 6 1 5 3.2 CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL20126 145473 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 527 6 1 5 3.2 CCNC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
11757133 235813 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 543 6 2 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)O)C1=O)C2 10.1021/jm00077a002
CHEMBL338548 235813 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 543 6 2 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)O)C1=O)C2 10.1021/jm00077a002
9889904 277633 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(C(F)(F)F)c1 10.1016/j.bmcl.2005.10.107
CHEMBL380733 277633 0 None None None Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccnn1-c1ccc(C(=O)N2Cc3cccnc3Nc3ccccc32)c(C(F)(F)F)c1 10.1016/j.bmcl.2005.10.107
44309820 469153 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 433 3 2 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Nc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL70949 469153 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 433 3 2 3 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Nc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
2981363 26791 5 None None None Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
CHEMBL118660 26791 5 None None None Rat 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 390 3 1 2 5.2 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1Cl 10.1021/jm960133o
10030231 42775 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 6 1 4 4.5 CC(C)CC1NC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
CHEMBL128489 42775 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 6 1 4 4.5 CC(C)CC1NC(=O)N([C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1021/jm00077a002
44352302 42815 0 None None None Human 6.4 pIC50 = 6.4 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 521 6 1 4 6.7 CN(C)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL128687 42815 0 None None None Human 6.4 pIC50 = 6.4 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 521 6 1 4 6.7 CN(C)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL1790938 484816 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 769 6 4 7 2.3 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
10693776 24460 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)cc1 10.1021/jm960133o
CHEMBL115853 24460 0 None None None Rat 7.4 pIC50 = 7.4 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 427 4 1 3 5.3 Cc1ccc(C(=O)Nc2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)cc2)cc1 10.1021/jm960133o
9935969 238831 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c(Cl)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL351453 238831 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c(Cl)[nH]c4cccc2c34)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
23598642 310825 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL400267 310825 0 None None None Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 541 6 2 3 7.1 CNCC1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
10460610 337143 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 567 6 1 7 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
CHEMBL449399 337143 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 567 6 1 7 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
14969548 465639 0 None None None Rat 4.4 pIC50 = 4.4 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 477 11 1 4 4.9 NCCCCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL60905 465639 0 None None None Rat 4.4 pIC50 = 4.4 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 477 11 1 4 4.9 NCCCCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
9937535 116561 1 None None None Rat 6.4 pIC50 = 6.4 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788221 116561 1 None None None Rat 6.4 pIC50 = 6.4 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 554 7 2 4 5.1 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3F)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
86690936 295803 0 None None None Human 7.4 pIC50 = 7.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 596 7 1 10 3.2 O=c1n(S(=O)(=O)c2ncnn2Cc2ccccc2C(F)(F)F)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
CHEMBL3943296 295803 0 None None None Human 7.4 pIC50 = 7.4 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 596 7 1 10 3.2 O=c1n(S(=O)(=O)c2ncnn2Cc2ccccc2C(F)(F)F)nc(-c2ccc(Cl)cc2)n1CC(O)C(F)(F)F nan
10461149 236130 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 596 7 4 8 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CNc3n[nH]c(N)n3)C1=O)C2 10.1021/jm00077a002
CHEMBL339524 236130 0 None None None Rat 6.4 pIC50 = 6.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 596 7 4 8 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CNc3n[nH]c(N)n3)C1=O)C2 10.1021/jm00077a002
44352413 45311 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1cccnc1)C2 10.1021/jm00077a002
CHEMBL131551 45311 0 None None None Rat 5.4 pIC50 = 5.4 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1cccnc1)C2 10.1021/jm00077a002
71720517 177883 0 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 177883 0 None None None Human 4.4 pIC50 = 4.4 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
132072820 354798 0 None None None Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human AVPR2 by PathHunter beta-arrestin assayAntagonist activity at human AVPR2 by PathHunter beta-arrestin assay
ChEMBL 610 8 0 7 5.4 COC(=O)[C@H]1[C@@H](OCc2cccc(OC)c2)CC[C@H]2CN3CC[C@@]4(C(=O)N(Cc5cccc(OC)c5)c5ccccc54)[C@@H]3C[C@@H]21 10.1016/j.bmc.2020.115546
CHEMBL4758081 354798 0 None None None Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human AVPR2 by PathHunter beta-arrestin assayAntagonist activity at human AVPR2 by PathHunter beta-arrestin assay
ChEMBL 610 8 0 7 5.4 COC(=O)[C@H]1[C@@H](OCc2cccc(OC)c2)CC[C@H]2CN3CC[C@@]4(C(=O)N(Cc5cccc(OC)c5)c5ccccc54)[C@@H]3C[C@@H]21 10.1016/j.bmc.2020.115546
10369423 327749 0 None None None Rat 4.3 pIC50 = 4.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 520 6 1 3 4.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccccc1)C2 10.1021/jm00077a002
CHEMBL435815 327749 0 None None None Rat 4.3 pIC50 = 4.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 520 6 1 3 4.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccccc1)C2 10.1021/jm00077a002
44352400 42764 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
CHEMBL128423 42764 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
9910527 157583 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 429 2 0 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4N(C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL205013 157583 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 429 2 0 5 5.2 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4N(C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
56848684 295096 0 None None None Human 7.3 pIC50 = 7.3 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 545 9 2 7 3.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(CCC(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3937650 295096 0 None None None Human 7.3 pIC50 = 7.3 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 545 9 2 7 3.9 NC(=O)OC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(CCC(F)(F)F)c1=O)c1ccccc1Cl nan
44294195 201445 1 None None None Rat 6.3 pIC50 = 6.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 519 4 1 5 6.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(-c2ccccn2)ccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL296619 201445 1 None None None Rat 6.3 pIC50 = 6.3 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 519 4 1 5 6.1 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(-c2ccccn2)ccc1Cl 10.1016/s0960-894x(99)00279-6
44352347 235693 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 540 6 4 7 2.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1n[nH]c(N)n1)C2 10.1021/jm00077a002
CHEMBL337853 235693 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 540 6 4 7 2.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1n[nH]c(N)n1)C2 10.1021/jm00077a002
44352184 235844 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 687 11 2 8 2.5 Cn1cnc(CC(=O)NC(CCS(C)(=O)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL338711 235844 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 687 11 2 8 2.5 Cn1cnc(CC(=O)NC(CCS(C)(=O)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
135177383 448267 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 419 6 0 7 3.7 COCc1nnc(N2CC(c3cccc4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5991970 448267 0 None None None Human 5.3 pIC50 = 5.3 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 419 6 0 7 3.7 COCc1nnc(N2CC(c3cccc4cc(F)ccc34)C2)n1-c1ccc(OC)nc1 nan
44352374 42388 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 529 7 3 5 3.0 CC(C)[C@H](N)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL127445 42388 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 529 7 3 5 3.0 CC(C)[C@H](N)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
9824954 155543 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL201889 155543 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 449 2 1 5 5.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmcl.2005.10.107
56848488 296236 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 609 10 3 8 3.3 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
CHEMBL3946734 296236 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 609 10 3 8 3.3 NC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
56848554 298481 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 595 10 3 8 2.3 CS(=O)(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3965460 298481 0 None None None Human 8.3 pIC50 = 8.3 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 595 10 3 8 2.3 CS(=O)(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
10503021 202796 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1021/jm980179c
CHEMBL304956 202796 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 435 3 1 3 5.6 Cc1cccc(C(=O)Nc2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)c1C 10.1021/jm980179c
172997 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
2238 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
CHEMBL49429 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
DB06666 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2007.09.059
54582950 125772 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788220 125772 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Evaluated for binding affinity towards vasopressin V2 receptor in ratEvaluated for binding affinity towards vasopressin V2 receptor in rat
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
10527151 202265 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(03)00388-3
CHEMBL302709 202265 0 None None None Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 441 3 1 3 5.6 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(03)00388-3
10642447 238065 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 362 3 1 2 5.4 CCNc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL343945 238065 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 362 3 1 2 5.4 CCNc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(Cl)c1 10.1021/jm000108p
172997 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
2238 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
CHEMBL49429 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
DB06666 4754 54 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
44335329 332598 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL430841 332598 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
21467167 123301 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
CHEMBL175813 123301 0 None None None Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 452 4 1 3 6.7 O=C(Nc1ccc(C(=O)N2CCCCc3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm00137a004
9851013 238896 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 570 7 1 5 6.7 COc1cc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
CHEMBL352150 238896 0 None None None Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 570 7 1 5 6.7 COc1cc(C(=O)N2Cc3ccc(CN(C)C)n3Cc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1016/s0960-894x(00)00095-0
67408780 298764 0 None None None Human 8.2 pIC50 = 8.2 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 550 7 2 6 4.8 NC(=O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
CHEMBL3967902 298764 0 None None None Human 8.2 pIC50 = 8.2 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 550 7 2 6 4.8 NC(=O)c1ccc(-c2ccccc2Cl)cc1Cn1nc(-c2ccc(Cl)cc2)n(CC(O)C(F)(F)F)c1=O nan
10831068 60875 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 340 4 1 2 4.9 C=CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
CHEMBL136644 60875 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 340 4 1 2 4.9 C=CCNc1ccc(C(=O)N2CCCCc3ccccc32)c(Cl)c1 10.1021/jm000108p
10765617 26721 0 None None None Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 441 6 2 3 5.7 CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118609 26721 0 None None None Rat 7.3 pIC50 = 7.3 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 441 6 2 3 5.7 CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
44377836 120328 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL166261 120328 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 505 4 2 2 7.3 O=C(Nc1ccc(C(=O)N2CCCc3c[nH]c4cccc2c34)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
11365307 124856 0 None None None Rat 7.3 pIC50 = 7.3 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL177556 124856 0 None None None Rat 7.3 pIC50 = 7.3 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
10840974 124530 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
CHEMBL177285 124530 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 579 7 1 6 5.8 CN1CCN(CCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccsc32)CC1 10.1021/jm030287l
11365307 124856 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
CHEMBL177556 124856 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 586 8 1 5 7.7 CN(CCc1cccnc1)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm00137a004
119369 5304 49 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
2197 5304 49 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
4004 5304 49 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
CHEMBL420762 5304 49 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm00137a004
15307972 469265 0 None None None Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 446 3 1 2 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71626 469265 0 None None None Rat 4.3 pIC50 = 4.3 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 446 3 1 2 6.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
71720517 177883 0 None None None Human 4.3 pIC50 = 4.3 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 177883 0 None None None Human 4.3 pIC50 = 4.3 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
10737785 61049 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 368 2 0 2 5.2 CC1CCN(c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)C1 10.1021/jm000108p
CHEMBL136790 61049 0 None None None Human 7.3 pIC50 = 7.3 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 368 2 0 2 5.2 CC1CCN(c2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)C1 10.1021/jm000108p
15298022 144263 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 370 2 0 3 5.4 O=C(c1ccc(-c2cccs2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL197616 144263 0 None None None Human 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 370 2 0 3 5.4 O=C(c1ccc(-c2cccs2)cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
71458039 155156 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 530 8 3 5 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00031a004
CHEMBL2112899 155156 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 530 8 3 5 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@@H](N)CCC(N)=O)C2 10.1021/jm00031a004
10075696 44357 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
10256467 44357 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL130742 44357 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL131650 44357 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
44352438 234204 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 6 3 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CCCNC1)C2 10.1021/jm00077a002
CHEMBL334610 234204 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 6 3 5 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CCCNC1)C2 10.1021/jm00077a002
44352412 234438 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccncc1)C2 10.1021/jm00077a002
CHEMBL335182 234438 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)Cc1ccncc1)C2 10.1021/jm00077a002
11269308 241186 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 390 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)cc1 10.1021/jm00137a004
CHEMBL360272 241186 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 390 3 1 3 5.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3sccc32)cc1 10.1021/jm00137a004
CHEMBL1790937 484815 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 755 6 5 7 1.9 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
9984805 235922 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 7 2 4 4.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCC1CCCNC1)C2 10.1021/jm00077a002
CHEMBL339155 235922 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 541 7 2 4 4.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCC1CCCNC1)C2 10.1021/jm00077a002
135177445 432683 0 None None None Human 4.3 pIC50 = 4.3 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 410 6 0 8 2.2 COCc1nnc(N2CC(N3CCc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5930186 432683 0 None None None Human 4.3 pIC50 = 4.3 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 410 6 0 8 2.2 COCc1nnc(N2CC(N3CCc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
11432362 194550 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 518 4 2 3 6.1 O=C(O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL249340 194550 0 None None None Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 518 4 2 3 6.1 O=C(O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
10621059 233281 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1[N+](=O)[O-] 10.1021/jm960133o
CHEMBL333055 233281 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1[N+](=O)[O-] 10.1021/jm960133o
44310140 469369 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 423 3 2 4 4.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1O 10.1016/s0960-894x(03)00388-3
CHEMBL72342 469369 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 423 3 2 4 4.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1O 10.1016/s0960-894x(03)00388-3
44352427 235700 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 637 10 4 6 3.2 CC(C)[C@H](NC(=O)Cc1c[nH]cn1)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL337889 235700 0 None None None Rat 6.3 pIC50 = 6.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 637 10 4 6 3.2 CC(C)[C@H](NC(=O)Cc1c[nH]cn1)C(=O)NC[C@@]1(O)C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
10258572 236926 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CC(CC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL340676 236926 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CC(CC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
14969539 332712 0 None None None Rat 4.3 pIC50 = 4.3 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 434 8 0 3 5.2 CCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL431723 332712 0 None None None Rat 4.3 pIC50 = 4.3 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 434 8 0 3 5.2 CCCCCCOc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
44273321 332274 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 542 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCN)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL429971 332274 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 542 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCN)C1=O)C2 10.1016/0960-894X(94)00469-V
44377521 238767 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 571 7 1 5 7.0 CCOC(=O)Cn1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
CHEMBL350792 238767 0 None None None Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 571 7 1 5 7.0 CCOC(=O)Cn1cc2c3c(cccc31)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccc(C)cc3)cc1)CCC2 10.1016/s0960-894x(02)01059-4
23598556 18714 0 None None None Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 454 3 1 2 6.4 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1F 10.1016/j.bmcl.2004.02.103
CHEMBL101157 18714 0 None None None Human 6.3 pIC50 = 6.3 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 454 3 1 2 6.4 O=C(Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1)c1ccccc1F 10.1016/j.bmcl.2004.02.103
10459923 235261 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 539 5 1 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL335944 235261 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 539 5 1 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
10480543 235438 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 485 4 1 4 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1CCC(N)C1=O)C2 10.1021/jm00077a002
CHEMBL336195 235438 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 485 4 1 4 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1CCC(N)C1=O)C2 10.1021/jm00077a002
44352490 236785 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 577 6 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CC(S(C)(=O)=O)CN1)C2 10.1021/jm00077a002
CHEMBL340362 236785 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 577 6 2 6 2.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C1CC(S(C)(=O)=O)CN1)C2 10.1021/jm00077a002
44352443 237270 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 539 7 3 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL341311 237270 0 None None None Rat 5.3 pIC50 = 5.3 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 539 7 3 5 2.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)Cc1c[nH]cn1)C2 10.1021/jm00077a002
71146879 292844 0 None None None Human 7.3 pIC50 = 7.3 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 2 7 3.8 O=c1n(Cc2nnc(-c3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3919631 292844 0 None None None Human 7.3 pIC50 = 7.3 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 2 7 3.8 O=c1n(Cc2nnc(-c3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10437668 155157 1 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 554 9 2 7 1.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@@H](N)CCS(C)(=O)=O)C3(C)C)CC1 10.1021/jm00031a004
CHEMBL2112903 155157 1 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidneyDisplacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
ChEMBL 554 9 2 7 1.5 Cc1ccccc1N1CCN(S(=O)(=O)C[C@]23CCC(C[C@@H]2NC(=O)[C@@H](N)CCS(C)(=O)=O)C3(C)C)CC1 10.1021/jm00031a004
10415322 332953 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 556 7 2 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCC(N)=O)C1=O)C2 10.1021/jm00077a002
CHEMBL433662 332953 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 556 7 2 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCC(N)=O)C1=O)C2 10.1021/jm00077a002
2249 4540 14 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
9872389 4540 14 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
CHEMBL1253853 4540 14 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat kidney V2 receptorInhibition of rat kidney V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
10789935 26091 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 455 4 1 5 5.0 CC(=O)O/N=C1\CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL118204 26091 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 455 4 1 5 5.0 CC(=O)O/N=C1\CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
22405322 144009 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 406 4 0 2 6.3 CCCc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
CHEMBL196737 144009 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 406 4 0 2 6.3 CCCc1ccc(-c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)cc2)cc1 10.1016/j.bmcl.2005.08.007
135177444 412436 0 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 440 7 0 9 2.4 CCOCc1nnc(N2CC(N3CCOc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5818544 412436 0 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 440 7 0 9 2.4 CCOCc1nnc(N2CC(N3CCOc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
135177938 462483 0 None None None Human 4.2 pIC50 = 4.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 440 6 0 9 1.6 COCc1nnc(N2CC(N3C(=O)COc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL6040264 462483 0 None None None Human 4.2 pIC50 = 4.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 440 6 0 9 1.6 COCc1nnc(N2CC(N3C(=O)COc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
9805201 119065 0 None None None Rat 8.2 pIC50 = 8.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 480 3 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
CHEMBL162748 119065 0 None None None Rat 8.2 pIC50 = 8.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 480 3 2 4 5.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)c(Cl)c1 10.1016/s0960-894x(00)00084-6
10279928 216982 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 527 4 1 3 7.0 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL317673 216982 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 527 4 1 3 7.0 O=C(Nc1ccc(C(=O)N2CC3C4CCC(CC4)N3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
11158261 257569 0 None None None Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL367323 257569 0 None None None Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
11490613 317266 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL413748 317266 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 636 9 1 6 6.6 CN1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
132102771 449661 0 None None None Human 8.2 pIC50 = 8.2 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 524 7 1 9 3.3 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(F)c1 nan
CHEMBL6006651 449661 0 None None None Human 8.2 pIC50 = 8.2 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 524 7 1 9 3.3 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(F)c1 nan
89707628 427871 0 None None None Human 8.2 pIC50 = 8.2 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 570 8 1 10 3.4 COC(=O)Cn1nc(-c2ccccc2Cl)nc1Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O nan
CHEMBL5881094 427871 0 None None None Human 8.2 pIC50 = 8.2 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 570 8 1 10 3.4 COC(=O)Cn1nc(-c2ccccc2Cl)nc1Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O nan
10390899 369987 0 None None None Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 490 3 1 3 6.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(99)00278-4
CHEMBL48867 369987 0 None None None Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 490 3 1 3 6.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2Cc3sccc3Cc3ccccc32)c(Cl)c1 10.1016/s0960-894x(99)00278-4
10578460 123198 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL175182 123198 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 544 6 1 5 7.1 O=C(Nc1ccc(C(=O)N2CCCN(Cc3cccnc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
11351397 123768 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
CHEMBL176264 123768 0 None None None Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 449 4 1 3 5.9 Cn1ccc2c1CCCCN2C(=O)c1ccc(NC(=O)c2ccccc2-c2ccccc2)cc1 10.1021/jm00137a004
10392781 237099 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 4.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)c1cccnc1)C2 10.1021/jm00077a002
CHEMBL340964 237099 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 7 2 5 4.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)c1cccnc1)C2 10.1021/jm00077a002
1513 468245 48 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 468245 48 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 468245 48 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
10620049 233131 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 5 1 2 4.9 O=C(CCc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL332757 233131 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 384 5 1 2 4.9 O=C(CCc1ccccc1)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
44352392 235739 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 567 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL338118 235739 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 567 6 2 5 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C1CN3CCC1CC3)C2 10.1021/jm00077a002
44273013 199670 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 543 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCO)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL283126 199670 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 543 7 2 6 2.2 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCCO)C1=O)C2 10.1016/0960-894X(94)00469-V
10394512 235879 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 652 11 3 7 2.3 Cn1cnc(CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL338921 235879 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 652 11 3 7 2.3 Cn1cnc(CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
44352114 45897 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 517 8 3 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCCO)C2 10.1021/jm00077a002
CHEMBL132165 45897 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 517 8 3 5 2.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCCO)C2 10.1021/jm00077a002
10393719 46153 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 595 8 2 5 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)CC1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL132391 46153 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 595 8 2 5 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CCNC(=O)CC1CN3CCC1CC3)C2 10.1021/jm00077a002
3514 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
5280343 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
DB04216 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
1513 468245 48 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 468245 48 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 468245 48 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
10790546 220172 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 470 5 2 4 4.9 CC(=O)Nc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL325819 220172 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 470 5 2 4 4.9 CC(=O)Nc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
2984025 27154 5 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 346 3 1 3 4.1 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccco1 10.1021/jm960133o
CHEMBL118892 27154 5 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 346 3 1 3 4.1 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccco1 10.1021/jm960133o
11764606 236211 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 630 9 0 7 3.3 Cn1cnc(CC(=O)N(CCS(C)(=O)=O)[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL339756 236211 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 630 9 0 7 3.3 Cn1cnc(CC(=O)N(CCS(C)(=O)=O)[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
2981862 232382 5 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc([N+](=O)[O-])cc1 10.1021/jm960133o
CHEMBL331647 232382 5 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccc([N+](=O)[O-])cc1 10.1021/jm960133o
10414380 234995 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
CHEMBL335634 234995 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 521 6 1 4 4.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)Cc1ccccn1)C2 10.1021/jm00077a002
44352124 235916 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 512 7 2 5 3.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCC#N)C2 10.1021/jm00077a002
CHEMBL339124 235916 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 512 7 2 5 3.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCC#N)C2 10.1021/jm00077a002
15340668 468757 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 407 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL68033 468757 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 407 3 1 3 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3-c3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10483586 44546 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 591 7 1 6 2.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCS(C)(=O)=O)C1=O)C2 10.1021/jm00077a002
CHEMBL130891 44546 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 591 7 1 6 2.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CCS(C)(=O)=O)C1=O)C2 10.1021/jm00077a002
11757440 235803 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 556 7 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CCC(=O)O)C1=O)C2 10.1021/jm00077a002
CHEMBL338503 235803 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 556 7 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(CCC(=O)O)C1=O)C2 10.1021/jm00077a002
53378840 296392 0 None None None Human 7.2 pIC50 = 7.2 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 532 6 1 7 5.3 O=c1n(Cc2cnc(-c3cccc(Cl)c3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3947893 296392 0 None None None Human 7.2 pIC50 = 7.2 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 532 6 1 7 5.3 O=c1n(Cc2cnc(-c3cccc(Cl)c3Cl)o2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
10322392 19033 0 None None None Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 468 3 1 2 6.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
CHEMBL103406 19033 0 None None None Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 468 3 1 2 6.7 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
135177583 407479 0 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 424 6 0 8 2.6 COCc1nnc(N2CC(N3CCCc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5765880 407479 0 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 424 6 0 8 2.6 COCc1nnc(N2CC(N3CCCc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
10393965 45889 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 610 7 3 8 2.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)Nc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
CHEMBL132157 45889 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 610 7 3 8 2.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)NC(CC(=O)Nc3nn[nH]n3)C1=O)C2 10.1021/jm00077a002
44352123 236918 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 566 8 3 6 1.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCS(N)(=O)=O)C2 10.1021/jm00077a002
CHEMBL340639 236918 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 566 8 3 6 1.6 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)C(N)CCS(N)(=O)=O)C2 10.1021/jm00077a002
135177410 406952 0 None None None Human 4.2 pIC50 = 4.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 426 6 0 9 2.0 COCc1nnc(N2CC(N3CCOc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
CHEMBL5760655 406952 0 None None None Human 4.2 pIC50 = 4.2 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 426 6 0 9 2.0 COCc1nnc(N2CC(N3CCOc4cc(F)ccc43)C2)n1-c1ccc(OC)nc1 nan
15307968 203104 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 432 3 1 2 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL307271 203104 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 432 3 1 2 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10619160 26119 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.8 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
CHEMBL118220 26119 0 None None None Rat 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.8 Cc1cccc(C(=O)Nc2ccc(C(=O)N3CCCc4ccccc43)cc2)c1 10.1021/jm960133o
44352453 42824 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1cccnc1)C2 10.1021/jm00077a002
CHEMBL128726 42824 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 535 6 2 5 3.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)c1cccnc1)C2 10.1021/jm00077a002
19699097 238699 0 None None None Rat 7.2 pIC50 = 7.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350090 238699 0 None None None Rat 7.2 pIC50 = 7.2 Binding
In vitro for its binding affinity to rat V2 receptorIn vitro for its binding affinity to rat V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL435021 488610 4 None None None Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 780 6 4 7 2.0 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CNCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
9871426 235876 0 None None None Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL338901 235876 0 None None None Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)CC1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44352757 237255 0 None None None Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL341173 237255 0 None None None Human 8.2 pIC50 = 8.2 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44378885 238792 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 625 7 1 6 6.4 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1Cc2ccc(CN3CCN(C)CC3)n2Cc2ccccc21 10.1016/s0960-894x(00)00095-0
CHEMBL351019 238792 0 None None None Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 625 7 1 6 6.4 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1Cc2ccc(CN3CCN(C)CC3)n2Cc2ccccc21 10.1016/s0960-894x(00)00095-0
18917534 469213 0 None None None Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 485 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Br 10.1016/s0960-894x(03)00388-3
CHEMBL71355 469213 0 None None None Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 485 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1)c1ccccc1Br 10.1016/s0960-894x(03)00388-3
10392505 218193 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
CHEMBL320416 218193 0 None None None Human 8.2 pIC50 = 8.2 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
11490514 258583 0 None None None Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL368354 258583 0 None None None Rat 8.2 pIC50 = 8.2 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 622 10 1 6 7.1 CN1CCN(CCCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
44294175 201946 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 520 3 1 4 5.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Br)ccc1Cl 10.1016/s0960-894x(99)00279-6
CHEMBL300433 201946 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 520 3 1 4 5.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1cc(Br)ccc1Cl 10.1016/s0960-894x(99)00279-6
9959838 330422 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 574 6 1 4 7.3 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
CHEMBL424163 330422 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 574 6 1 4 7.3 CN(C)Cc1ccc2n1Cc1ccccc1N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1Cl)C2 10.1016/s0960-894x(00)00095-0
10831734 237668 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 350 2 0 2 5.1 O=C(c1ccc(-n2cccc2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL342250 237668 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 350 2 0 2 5.1 O=C(c1ccc(-n2cccc2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
132088152 426372 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 538 7 0 9 4.0 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(CC(=O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 nan
CHEMBL5864081 426372 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 538 7 0 9 4.0 CC(=O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(CC(=O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 nan
67409800 293595 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cnn(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3925572 293595 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 497 6 1 7 4.2 O=c1n(Cc2cnn(-c3ccccc3Cl)c2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
56848491 299050 0 None None None Human 7.2 pIC50 = 7.2 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 651 9 3 8 4.7 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
CHEMBL3970631 299050 0 None None None Human 7.2 pIC50 = 7.2 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 651 9 3 8 4.7 CC(C)(C)OC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1C(F)(F)F nan
10595343 233440 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.9 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
CHEMBL333201 233440 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 370 3 1 2 4.9 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
44332273 333729 0 None None None Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 450 3 1 2 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
CHEMBL440147 333729 0 None None None Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptorIn vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
ChEMBL 450 3 1 2 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC3(C=CCCC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.02.103
10626339 256585 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL366790 256585 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
3514 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
5280343 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
DB04216 371491 78 None None None Human 5.2 pIC50 = 5.2 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
9981665 232117 5 None None None Rat 4.2 pIC50 = 4.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm00077a002
CHEMBL341339 232117 5 None None None Rat 4.2 pIC50 = 4.2 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm00077a002
11798122 233539 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 458 5 1 5 4.9 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3[N+](=O)[O-])cc2)c2ccccc21 10.1021/jm960133o
CHEMBL333597 233539 0 None None None Rat 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 458 5 1 5 4.9 CN(C)C1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3[N+](=O)[O-])cc2)c2ccccc21 10.1021/jm960133o
11238362 333545 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL438523 333545 0 None None None Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 562 6 2 4 6.5 CCOc1cc(C(=O)N2CC[C@]3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
19699097 238699 0 None None None Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
CHEMBL350090 238699 0 None None None Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity to human V2 receptorIn vitro binding affinity to human V2 receptor
ChEMBL 446 3 2 4 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCc3c[nH]nc3-c3sccc32)cc1 10.1016/s0960-894x(00)00084-6
977621 24390 10 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 322 4 1 2 4.0 CCCC(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL115434 24390 10 None None None Rat 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 322 4 1 2 4.0 CCCC(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
44273173 199254 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
44273417 199254 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL280202 199254 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL283317 199254 0 None None None Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
44335241 332743 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 575 4 1 3 8.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL432009 332743 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptorInhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
ChEMBL 575 4 1 3 8.0 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(CC5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL2112250 485098 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 766 6 4 7 2.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cccc3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
44273034 199276 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.3 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCC(=O)O)C1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL280356 199276 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 557 7 2 6 2.3 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CC(NCC(=O)O)C1=O)C2 10.1016/0960-894X(94)00469-V
14969534 332643 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 412 2 0 2 4.0 O=C(c1ccc(Br)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
CHEMBL431159 332643 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 412 2 0 2 4.0 O=C(c1ccc(Br)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
9986160 236217 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 608 7 2 6 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CC(=O)Nc3ncc[nH]3)C1=O)C2 10.1021/jm00077a002
CHEMBL339768 236217 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 608 7 2 6 3.1 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(CC(=O)Nc3ncc[nH]3)C1=O)C2 10.1021/jm00077a002
CHEMBL2112655 485105 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 707 8 4 7 1.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
44352146 236069 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 513 5 2 5 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CN1C(=O)CNC1=O)C2 10.1021/jm00077a002
CHEMBL339433 236069 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 513 5 2 5 2.5 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CN1C(=O)CNC1=O)C2 10.1021/jm00077a002
44352491 237052 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 8 2 5 2.7 C[S+]([O-])CCC(N)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL340915 237052 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 549 8 2 5 2.7 C[S+]([O-])CCC(N)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL2112651 485103 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)
ChEMBL 779 6 3 6 3.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
137484998 410615 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 532 5 0 7 4.6 O=C(OC(CF)CF)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL5798429 410615 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 532 5 0 7 4.6 O=C(OC(CF)CF)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137485239 410767 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 482 2 0 7 4.5 COC(=O)N1Cc2cc(Cl)ccc2-n2c(C3CC4(C3)CN(c3ncccc3F)C4)nnc2C1C nan
CHEMBL5800135 410767 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 482 2 0 7 4.5 COC(=O)N1Cc2cc(Cl)ccc2-n2c(C3CC4(C3)CN(c3ncccc3F)C4)nnc2C1C nan
137485093 412933 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 4 0 6 4.4 CC(CF)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
CHEMBL5824263 412933 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 4 0 6 4.4 CC(CF)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
137484946 424240 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 3 0 6 4.6 CC(C)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ncccc2F)C3)C1 nan
CHEMBL5840604 424240 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 452 3 0 6 4.6 CC(C)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ncccc2F)C3)C1 nan
137485171 443450 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 434 3 0 6 4.4 CC(C)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
CHEMBL5940399 443450 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 434 3 0 6 4.4 CC(C)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
137485007 444745 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 438 4 0 6 4.0 FCCN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
CHEMBL5953899 444745 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 438 4 0 6 4.0 FCCN1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccccn2)C3)C1 nan
137485282 445178 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 546 5 0 7 5.2 CC1c2nnc(C3CC4(C3)CN(c3ccc(F)cn3)C4)n2-c2ccc(Cl)cc2CN1C(=O)OC(CF)CF nan
CHEMBL5958710 445178 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 546 5 0 7 5.2 CC1c2nnc(C3CC4(C3)CN(c3ccc(F)cn3)C4)n2-c2ccc(Cl)cc2CN1C(=O)OC(CF)CF nan
137485195 463660 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 480 3 0 6 4.3 CC(C)C(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
CHEMBL6051766 463660 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 480 3 0 6 4.3 CC(C)C(=O)N1Cc2cc(Cl)ccc2-n2c(nnc2C2CC3(C2)CN(c2ccc(F)cn2)C3)C1 nan
137485448 463727 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 483 2 0 8 3.9 COC(=O)N1Cc2cc(Cl)ccc2-n2c(C3CC4(C3)CN(c3ncc(F)cn3)C4)nnc2C1C nan
CHEMBL6052527 463727 0 None None None Human 6.1 pIC50 = 6.1 Binding
Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.Vasopressin V2 Receptor Antagonist Assay: The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
ChEMBL 483 2 0 8 3.9 COC(=O)N1Cc2cc(Cl)ccc2-n2c(C3CC4(C3)CN(c3ncc(F)cn3)C4)nnc2C1C nan
10369550 237275 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 6 1 5 3.6 Cn1cncc1CC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL341338 237275 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 6 1 5 3.6 Cn1cncc1CC(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
44444760 308697 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL399288 308697 0 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 518 4 2 3 6.1 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3cc(F)ccc3Cl)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
10501216 222589 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc([N+](=O)[O-])c1 10.1021/jm960133o
CHEMBL331424 222589 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 401 4 1 4 4.4 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccc([N+](=O)[O-])c1 10.1021/jm960133o
10713341 27217 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 357 3 1 3 3.9 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccnc1 10.1021/jm960133o
CHEMBL118933 27217 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 357 3 1 3 3.9 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cccnc1 10.1021/jm960133o
10599369 233806 0 None None None Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 443 5 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
CHEMBL334082 233806 0 None None None Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 443 5 1 4 5.0 COc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(N(C)C)c3ccccc32)cc1 10.1021/jm960133o
21837089 213531 0 None None None Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 451 5 1 4 5.3 CCOc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL309096 213531 0 None None None Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 451 5 1 4 5.3 CCOc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
14969514 468340 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 368 2 0 2 3.9 O=C(c1ccc(Cl)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
CHEMBL64811 468340 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 368 2 0 2 3.9 O=C(c1ccc(Cl)cc1)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1021/jm00066a010
10548205 26974 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 386 3 1 3 5.3 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Oc1ccccc1 10.1021/jm960133o
CHEMBL118760 26974 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).Compound was tested for its ability to displace [3H]AVP from its specific binding sites in rat Kidney (AVP-V2 receptor).
ChEMBL 386 3 1 3 5.3 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)Oc1ccccc1 10.1021/jm960133o
10075696 44357 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
10256467 44357 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL130742 44357 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
CHEMBL131650 44357 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 530 8 3 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](N)CCC(N)=O)C2 10.1021/jm00077a002
1513 468245 48 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 468245 48 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 468245 48 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
9828129 235526 0 None None None Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
CHEMBL336825 235526 0 None None None Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 522 6 2 4 6.6 O=C(O)C[C@@H]1CCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc2S1 10.1016/j.bmcl.2003.08.051
44352783 235671 0 None None None Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL337725 235671 0 None None None Human 8.1 pIC50 = 8.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 508 6 2 4 6.5 O=C(Nc1ccc(C(=O)N2CCC(CCO)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
23598598 19306 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
CHEMBL104839 19306 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)Binding affinity measured by inhibition of 3[H] AVP binding to cloned human V2 receptor (Compound 7o)
ChEMBL 608 7 2 4 6.3 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCC3(C=C(C(=O)NCCN4CCCCC4)CC3)Cc3ccccc32)cc1 10.1016/j.bmcl.2004.04.016
54582950 125772 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
CHEMBL1788220 125772 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptorBinding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2004.04.016
56848555 298388 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 560 9 4 7 2.5 NC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
CHEMBL3964694 298388 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 560 9 4 7 2.5 NC(=O)NC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1ccccc1Cl nan
9848300 238748 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 487 4 2 3 6.1 O=C(Nc1ccc(C(=O)N2CCCC3C(=O)Nc4cccc2c43)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
CHEMBL350576 238748 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human V2 receptors expressed in HEK293 cellsDisplacement of [3H]AVP from human V2 receptors expressed in HEK293 cells
ChEMBL 487 4 2 3 6.1 O=C(Nc1ccc(C(=O)N2CCCC3C(=O)Nc4cccc2c43)cc1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)01059-4
10743659 470523 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 489 3 1 3 6.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL82376 470523 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 489 3 1 3 6.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1NC(=O)c1ccc(Cl)cc1Cl 10.1021/jm980179c
44444762 308702 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
CHEMBL399888 308702 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 612 8 2 4 6.6 CN(C)CCNC(=O)C1=C[C@@]2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
11262100 124526 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL177248 124526 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medullaInhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
11422294 125044 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL177885 125044 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 636 8 1 6 6.6 CN(C)C1CCN(C(=O)COc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
86690917 297073 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 555 8 2 9 2.7 NC(=O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
CHEMBL3953766 297073 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity: The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
ChEMBL 555 8 2 9 2.7 NC(=O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
86690917 297073 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 555 8 2 9 2.7 NC(=O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
CHEMBL3953766 297073 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 555 8 2 9 2.7 NC(=O)Cn1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nc1-c1ccccc1Cl nan
18917553 201585 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 484 4 1 4 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(99)00279-6
CHEMBL297705 201585 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of P[3H]-AVP from isolated rat kidney medullary V2 receptorDisplacement of P[3H]-AVP from isolated rat kidney medullary V2 receptor
ChEMBL 484 4 1 4 6.0 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)cn1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(99)00279-6
10673699 216346 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 527 3 1 3 6.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1cccc(C(F)(F)F)c1F 10.1021/jm980179c
CHEMBL314344 216346 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranesDisplacement of [3H]AVP from human V2 receptor expressed in murine fibroblast cell line (LV2) membranes
ChEMBL 527 3 1 3 6.8 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1cccc(C(F)(F)F)c1F 10.1021/jm980179c
10673295 214598 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
CHEMBL311230 214598 0 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
ChEMBL 509 3 1 3 6.9 O=C(Nc1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1)c1ccc(Cl)cc1Cl 10.1021/jm980179c
86690931 295709 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 543 6 1 7 5.1 O=c1n(Cc2cc(-c3cccc(Cl)c3Cl)ncn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3942564 295709 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 543 6 1 7 5.1 O=c1n(Cc2cc(-c3cccc(Cl)c3Cl)ncn2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
71146879 292844 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 2 7 3.8 O=c1n(Cc2nnc(-c3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
CHEMBL3919631 292844 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular In Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 498 6 2 7 3.8 O=c1n(Cc2nnc(-c3ccccc3Cl)[nH]2)nc(-c2ccc(Cl)cc2)n1C[C@H](O)C(F)(F)F nan
44378675 333301 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 671 6 1 5 7.4 CN(C)C1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
CHEMBL436241 333301 0 None None None Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranesDisplacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
ChEMBL 671 6 1 5 7.4 CN(C)C1CCN(C(=O)c2ccc3n2Cc2ccccc2N(C(=O)c2ccc(NC(=O)c4ccccc4-c4ccccc4)cc2Cl)C3)CC1 10.1016/s0960-894x(00)00095-0
10569977 64612 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 351 2 0 3 4.5 O=C(c1ccc(-n2cccn2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL139863 64612 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 351 2 0 3 4.5 O=C(c1ccc(-n2cccn2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
3537 8682 25 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
5311500 8682 25 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
CHEMBL363910 8682 25 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2005.10.107
11262100 124526 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL177248 124526 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 624 13 1 6 7.3 CN(C)CCN(C)CCCCOc1cc(C(=O)N2CCCCc3sccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm030287l
10626339 256585 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
CHEMBL366790 256585 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 543 6 1 4 7.7 O=C(Nc1ccc(C(=O)N2CCCN(Cc3ccccc3)c3sccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm030287l
10578000 333180 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
CHEMBL435331 333180 0 None None None Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 524 7 1 5 6.1 CN(C)CCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccsc21 10.1021/jm030287l
3537 8682 25 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2007.08.053
5311500 8682 25 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2007.08.053
CHEMBL363910 8682 25 None None None Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1016/j.bmcl.2007.08.053
1513 468245 48 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 468245 48 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 468245 48 None None None Human 6.1 pIC50 = 6.1 Binding
Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
14969540 200952 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 362 3 0 2 3.8 CCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL293184 200952 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 362 3 0 2 3.8 CCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL2112249 485097 2 None None None Rat 6.1 pIC50 = 6.1 Binding
Ability to inhibit AVP stimulation of adenylate cyclase activity in the rat kidney medulla (AVP-V2) receptorAbility to inhibit AVP stimulation of adenylate cyclase activity in the rat kidney medulla (AVP-V2) receptor
ChEMBL 766 6 4 7 2.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
11764710 235356 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL336082 235356 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 638 11 4 6 2.3 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)Cc1c[nH]cn1)C2 10.1021/jm00077a002
5099582 220037 8 None None None Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 322 3 1 2 3.9 CC(C)C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL324935 220037 8 None None None Rat 5.1 pIC50 = 5.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 322 3 1 2 3.9 CC(C)C(=O)Nc1ccc(C(=O)N2CCCc3ccccc32)cc1 10.1021/jm960133o
CHEMBL52813 489209 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 712 6 2 6 2.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/jm00099a019
10741034 28179 0 None None None Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cc(Cl)cc(Cl)c1 10.1021/jm960133o
CHEMBL119651 28179 0 None None None Rat 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 424 3 1 2 5.8 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1cc(Cl)cc(Cl)c1 10.1021/jm960133o
14969542 448058 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 390 5 0 2 4.6 CCCCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
CHEMBL59900 448058 0 None None None Rat 4.1 pIC50 = 4.1 Binding
Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
ChEMBL 390 5 0 2 4.6 CCCCc1ccc(C(=O)N2CCC(N3C(=O)CCc4ccccc43)CC2)cc1 10.1021/jm00066a010
44273173 199254 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
44273417 199254 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL280202 199254 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL283317 199254 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 555 7 0 5 4.0 CCN(CC)[C@@H]1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
10370127 42730 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 542 6 2 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CN1CC[C@H](N)C1=O)C2 10.1021/jm00077a002
CHEMBL128228 42730 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 542 6 2 5 2.2 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CN1CC[C@H](N)C1=O)C2 10.1021/jm00077a002
44352796 45323 0 None None None Human 7.1 pIC50 = 7.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 510 6 1 3 7.5 O=C(Nc1ccc(C(=O)N2CCC(CCF)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
CHEMBL131566 45323 0 None None None Human 7.1 pIC50 = 7.1 Binding
Ability to displace [3H]arginine vasopressin in cloned human V2 receptorAbility to displace [3H]arginine vasopressin in cloned human V2 receptor
ChEMBL 510 6 1 3 7.5 O=C(Nc1ccc(C(=O)N2CCC(CCF)Sc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2003.08.051
15307967 202377 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 432 3 1 2 6.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL303376 202377 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 432 3 1 2 6.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
15307988 469278 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 450 3 1 3 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Sc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
CHEMBL71712 469278 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
ChEMBL 450 3 1 3 6.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccccc3Sc3ccccc32)cc1 10.1016/s0960-894x(03)00388-3
10393977 333197 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 611 10 3 5 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)N(CCC(=O)O)CCc1c[nH]cn1)C2 10.1021/jm00077a002
CHEMBL435409 333197 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 611 10 3 5 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)N(CCC(=O)O)CCc1c[nH]cn1)C2 10.1021/jm00077a002
44273459 155610 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 482 4 0 4 3.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C=CC1=O)C2 10.1016/0960-894X(94)00469-V
CHEMBL20205 155610 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 482 4 0 4 3.4 CC1(C)C2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)C=CC1=O)C2 10.1016/0960-894X(94)00469-V
10030575 45952 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 5 2 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NC1CN3CCC1CC3)C2 10.1021/jm00077a002
CHEMBL132210 45952 0 None None None Rat 5.1 pIC50 = 5.1 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 5 2 4 3.9 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)NC1CN3CCC1CC3)C2 10.1021/jm00077a002
44273355 156615 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 587 8 0 6 3.9 CN(C)CCSC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
CHEMBL20319 156615 0 None None None Rat 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptorInhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
ChEMBL 587 8 0 6 3.9 CN(C)CCSC1CC(=O)N([C@H]2CC3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)C1=O 10.1016/0960-894X(94)00469-V
10043741 237004 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
CHEMBL340893 237004 0 None None None Human 8.1 pIC50 = 8.1 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm020133q
56848489 291625 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 637 11 3 8 4.0 CCNC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
CHEMBL3909988 291625 0 None None None Human 8.1 pIC50 = 8.1 Binding
Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.Cellular in Vitro Assay: On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
ChEMBL 637 11 3 8 4.0 CCNC(=O)OCC(CNC(=O)Cn1nc(-c2ccc(Cl)cc2)n(C[C@H](O)C(F)(F)F)c1=O)c1cccc(C(F)(F)F)c1 nan
15307998 201232 0 None None None Human 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccsc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
CHEMBL295014 201232 0 None None None Human 8.1 pIC50 = 8.1 Binding
In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)In vitro inhibition of [3H]AVP binding to human V2 receptor from murine fibroblast cell line (LV2)
ChEMBL 438 3 1 3 6.1 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2Cc3ccsc3Cc3ccccc32)cc1 10.1016/s0960-894x(99)00278-4
10043741 237004 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
CHEMBL340893 237004 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cellsInhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
ChEMBL 354 2 0 2 4.9 O=C(c1ccc(N2CCCC2)cc1Cl)N1CCCCc2ccccc21 10.1021/jm000108p
11158261 257569 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
CHEMBL367323 257569 0 None None None Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cellsInhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
ChEMBL 692 12 1 6 8.1 CCN(CC)C1CCN(C(=O)CCCOc2cc(C(=O)N3CCCCc4sccc43)ccc2NC(=O)c2ccccc2-c2ccccc2)CC1 10.1021/jm030287l
44376291 197414 0 None None None Pig 8.0 pIC50 = 8.0 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1115 19 14 17 -4.8 NC(=O)CC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](N)CSSSC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/S0960-894X(97)00050-4
CHEMBL267405 197414 0 None None None Pig 8.0 pIC50 = 8.0 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
ChEMBL 1115 19 14 17 -4.8 NC(=O)CC[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](N)CSSSC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1016/S0960-894X(97)00050-4
9888109 156030 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL202447 156030 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 415 2 1 5 5.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(Cl)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL2112249 485097 2 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
ChEMBL 766 6 4 7 2.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00099a019
135177589 445964 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 451 6 0 8 3.3 CCOCc1nnc(N2CC(N3CCCc4cc(F)ccc43)C2)n1-c1ccc2c(c1)OCO2 nan
CHEMBL5967011 445964 0 None None None Human 5.0 pIC50 = 5.0 Binding
Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)Inhibition Activity Assay: V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
ChEMBL 451 6 0 8 3.3 CCOCc1nnc(N2CC(N3CCCc4cc(F)ccc43)C2)n1-c1ccc2c(c1)OCO2 nan
11261339 308698 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
CHEMBL399289 308698 0 None None None Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cellsDisplacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 548 5 2 4 6.1 COc1cc(C(=O)N2CCC3(C=C(C(=O)O)CC3)Cc3ccccc32)ccc1NC(=O)c1cc(F)ccc1Cl 10.1016/j.bmcl.2007.09.059
44352371 45175 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 593 9 3 7 1.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C(N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
CHEMBL131388 45175 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 593 9 3 7 1.8 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CNC(=O)C(N)CCS(C)(=O)=O)C2 10.1021/jm00077a002
10345259 235827 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 484 4 0 3 4.5 CC1CCC(=O)N1[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
CHEMBL338635 235827 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 484 4 0 3 4.5 CC1CCC(=O)N1[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)C2(C)C 10.1021/jm00077a002
9887157 155625 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 399 2 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(F)c2)n1 10.1016/j.bmcl.2005.10.107
CHEMBL202106 155625 0 None None None Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]AVP from human V2 receptor transfected in LV2 cellsDisplacement of [3H]AVP from human V2 receptor transfected in LV2 cells
ChEMBL 399 2 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3Cc4cccnc4Nc4ccccc43)c(F)c2)n1 10.1016/j.bmcl.2005.10.107
10370697 237189 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
CHEMBL341049 237189 0 None None None Rat 6.0 pIC50 = 6.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 565 6 1 5 3.7 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](N1C(=O)CN(Cc3c[nH]cn3)C1=O)C2 10.1021/jm00077a002
10098332 46276 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 6 1 5 3.6 Cn1cnc(CC(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
CHEMBL132496 46276 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 524 6 1 5 3.6 Cn1cnc(CC(=O)N[C@H]2C[C@H]3CC[C@]2(CS(=O)(=O)N2CCC4(CCc5ccccc54)CC2)C3(C)C)c1 10.1021/jm00077a002
10599903 38476 0 None None None Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 456 4 3 3 4.7 CNC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
CHEMBL120449 38476 0 None None None Rat 7.0 pIC50 = 7.0 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 456 4 3 3 4.7 CNC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2)c2ccccc21 10.1021/jm960133o
22405327 277564 0 None None None Human 7.0 pIC50 = 7.0 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 409 3 0 4 5.3 O=C(c1ccc(-c2ccccc2[N+](=O)[O-])cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
CHEMBL380579 277564 0 None None None Human 7.0 pIC50 = 7.0 Binding
Inhibition of [3H]-AVP binding to human V2 receptorInhibition of [3H]-AVP binding to human V2 receptor
ChEMBL 409 3 0 4 5.3 O=C(c1ccc(-c2ccccc2[N+](=O)[O-])cc1)N1Cc2cccn2Cc2ccccc21 10.1016/j.bmcl.2005.08.007
10435004 42747 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 473 6 2 4 3.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCN)C2 10.1021/jm00077a002
CHEMBL128328 42747 0 None None None Rat 5.0 pIC50 = 5.0 Binding
Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissueInhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
ChEMBL 473 6 2 4 3.0 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(CCc4ccccc43)CC1)[C@@H](NC(=O)CCN)C2 10.1021/jm00077a002
11070458 37960 5 None None None Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
CHEMBL125878 37960 5 None None None Human 6.0 pIC50 = 6.0 Binding
Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determinedBinding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
ChEMBL 453 5 1 3 5.4 CC(C)NC(=O)C[C@@H]1CCCN(C(=O)c2ccc(N3CCCC3)cc2Cl)c2ccccc21 10.1021/jm020133q
10642000 233408 8 None None None Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
CHEMBL333139 233408 8 None None None Rat 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
ChEMBL 356 3 1 2 4.5 O=C(Nc1ccc(C(=O)N2CCCc3ccccc32)cc1)c1ccccc1 10.1021/jm960133o
71457081 163802 0 None None None Human 8.9 pKd = 8.9 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482251 163802 0 None None None Human 8.9 pKd = 8.9 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172289 163802 0 None None None Human 8.9 pKd = 8.9 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44386183 312019 0 None None None Bovine 8.9 pKd = 8.9 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1013 18 12 14 -3.5 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
CHEMBL406303 312019 0 None None None Bovine 8.9 pKd = 8.9 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1013 18 12 14 -3.5 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
146681949 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
2168 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
2810 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
644077 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
CHEMBL373742 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
DB00067 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
P01185 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
P01186 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
P35455 8624 35 None 1 3 Rat 8.8 pKd = 8.8 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/s0960-894x(99)00041-4
146681949 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
2168 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
2810 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
644077 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
CHEMBL373742 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
DB00067 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
P01185 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
P01186 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
P35455 8624 35 None -2 3 Bovine 8.8 pKd = 8.8 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm00028a008
CHEMBL265119 486148 0 None None None Bovine 8.0 pKd = 8 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1057 20 14 16 -5.9 CN(CC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
71461726 161164 0 None -489 2 Pig 7.0 pKd = 7 Binding
Binding affinity towards Vasopressin V2 receptor in LLCPK cellsBinding affinity towards Vasopressin V2 receptor in LLCPK cells
ChEMBL 1186 20 11 15 0.9 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)CSSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00079a020
CHEMBL2115369 161164 0 None -489 2 Pig 7.0 pKd = 7 Binding
Binding affinity towards Vasopressin V2 receptor in LLCPK cellsBinding affinity towards Vasopressin V2 receptor in LLCPK cells
ChEMBL 1186 20 11 15 0.9 COc1ccc(C[C@@H]2NC(=O)C3(CCCC3)CSSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00079a020
118718749 234351 0 None -8 3 Rat 6.0 pKd = 6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
118718752 234351 0 None -8 3 Rat 6.0 pKd = 6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350119 234351 0 None -8 3 Rat 6.0 pKd = 6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350124 234351 0 None -8 3 Rat 6.0 pKd = 6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
71451749 163801 0 None None None Human 8.0 pKd = 8.0 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL2172288 163801 0 None None None Human 8.0 pKd = 8.0 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL413706 488295 0 None None None Bovine 7.0 pKd = 7.0 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1055 20 13 15 -5.3 C[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
118718753 234353 0 None -43 3 Rat 5.9 pKd = 5.9 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1074 18 11 15 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00010a020
CHEMBL3350126 234353 0 None -43 3 Rat 5.9 pKd = 5.9 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1074 18 11 15 -1.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00010a020
44320759 316382 0 None -8 2 Bovine 6.9 pKd = 6.9 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1036 22 12 15 -4.4 CCOc1ccc(C[C@@H]2NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm00028a008
CHEMBL411420 316382 0 None -8 2 Bovine 6.9 pKd = 6.9 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1036 22 12 15 -4.4 CCOc1ccc(C[C@@H]2NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm00028a008
136961687 237390 0 None -77 3 Human 6.9 pKd = 6.9 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1053 21 7 12 6.4 O=C(CCCCCNC(=O)c1ccc(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c(C(=O)O)c1)NCCNC(=O)CCc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(Cl)cc2)cc1 10.1021/jm501395b
CHEMBL3416749 237390 0 None -77 3 Human 6.9 pKd = 6.9 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1053 21 7 12 6.4 O=C(CCCCCNC(=O)c1ccc(-c2c3ccc(=O)cc-3oc3cc(O)ccc23)c(C(=O)O)c1)NCCNC(=O)CCc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(Cl)cc2)cc1 10.1021/jm501395b
CHEMBL2370617 477411 0 None -3 3 Rat 7.8 pKd = 7.8 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00010a020
56678404 126039 0 None 1 2 Bovine 6.7 pKd = 6.7 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm00028a008
CHEMBL1793955 126039 0 None 1 2 Bovine 6.7 pKd = 6.7 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm00028a008
71455302 163803 0 None None None Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482380 163803 0 None None None Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172290 163803 0 None None None Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71462477 163804 0 None None None Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482382 163804 0 None None None Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172291 163804 0 None None None Human 8.6 pKd = 8.6 Binding
Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assayBinding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL269715 486308 0 None None None Bovine 7.7 pKd = 7.7 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1071 20 14 16 -5.5 C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
70693557 159925 0 None -6 2 Rat 5.6 pKd = 5.6 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL2110163 159925 0 None -6 2 Rat 5.6 pKd = 5.6 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
44320761 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
44321207 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
CHEMBL265264 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
CHEMBL384292 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
44320761 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
44321207 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
CHEMBL265264 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
CHEMBL384292 197170 0 None -1 2 Bovine 6.6 pKd = 6.6 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1110 20 13 15 -3.2 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
CHEMBL2370976 477420 13 None -3 3 Rat 7.6 pKd = 7.6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00010a020
118718750 234352 0 None -501 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1151 19 12 15 -2.3 CN1C(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
118718751 234352 0 None -501 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1151 19 12 15 -2.3 CN1C(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350120 234352 0 None -501 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1151 19 12 15 -2.3 CN1C(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350123 234352 0 None -501 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1151 19 12 15 -2.3 CN1C(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
44320718 333533 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1139 22 12 15 -2.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00028a008
CHEMBL438387 333533 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1139 22 12 15 -2.5 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00028a008
44373714 197048 0 None 1 2 Rat 8.5 pKd = 8.5 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1148 32 14 16 -3.1 CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(=O)oc2cc(OC)ccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O 10.1016/s0960-894x(99)00041-4
CHEMBL264208 197048 0 None 1 2 Rat 8.5 pKd = 8.5 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1148 32 14 16 -3.1 CC[C@H](C)[C@H](NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)c1cc(=O)oc2cc(OC)ccc12)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O 10.1016/s0960-894x(99)00041-4
136961688 237391 0 None -21 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1206 23 5 13 7.4 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCNC(=O)CCc2ccc(S(=O)(=O)N(CC(=O)N/N=C3\C(=O)Nc4ccccc43)c3ccc(Cl)cc3)cc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL3416750 237391 0 None -21 3 Human 7.5 pKd = 7.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1206 23 5 13 7.4 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCNC(=O)CCc2ccc(S(=O)(=O)N(CC(=O)N/N=C3\C(=O)Nc4ccccc43)c3ccc(Cl)cc3)cc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
44321133 317350 0 None -38 2 Bovine 6.5 pKd = 6.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL414582 317350 0 None -38 2 Bovine 6.5 pKd = 6.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1060 20 12 14 -3.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
118718383 234320 0 None -194 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1000 14 11 13 0.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
118718385 234320 0 None -194 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1000 14 11 13 0.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349464 234320 0 None -194 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1000 14 11 13 0.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349466 234320 0 None -194 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1000 14 11 13 0.2 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
118718384 234321 0 None -154 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1154 18 12 16 -0.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349465 234321 0 None -154 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1154 18 12 16 -0.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
10463677 234323 4 None -363 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 15 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349468 234323 4 None -363 3 Rat 5.5 pKd = 5.5 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 15 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
44386245 333451 0 None None None Bovine 7.5 pKd = 7.5 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1027 18 12 14 -3.1 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
CHEMBL437631 333451 0 None None None Bovine 7.5 pKd = 7.5 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1027 18 12 14 -3.1 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
44321188 317415 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1105 22 12 15 -2.7 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm00028a008
CHEMBL415230 317415 0 None -1 2 Bovine 7.5 pKd = 7.5 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1105 22 12 15 -2.7 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm00028a008
145947801 332482 0 None -190 2 Human 6.5 pKd = 6.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1381 42 2 22 7.7 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL4302530 332482 0 None -190 2 Human 6.5 pKd = 6.5 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1381 42 2 22 7.7 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
118718386 234322 0 None -186 3 Rat 5.4 pKd = 5.4 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 14 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
CHEMBL3349467 234322 0 None -186 3 Rat 5.4 pKd = 5.4 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 991 14 10 14 -0.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)N(C)C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm00010a020
44373744 104407 0 None -52 2 Rat 6.4 pKd = 6.4 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 993 20 12 14 -4.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL157988 104407 0 None -52 2 Rat 6.4 pKd = 6.4 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 993 20 12 14 -4.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
44320760 473352 0 None -52 2 Bovine 6.4 pKd = 6.4 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 992 20 12 14 -4.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL87636 473352 0 None -52 2 Bovine 6.4 pKd = 6.4 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 992 20 12 14 -4.8 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL410025 488093 0 None None None Bovine 7.4 pKd = 7.4 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1041 20 13 15 -5.6 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
118718749 234351 0 None -8 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
118718752 234351 0 None -8 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350119 234351 0 None -8 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
CHEMBL3350124 234351 0 None -8 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1136 18 11 14 -0.5 CCN1C(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]1Cc1ccc(O)cc1 10.1021/jm00010a020
44373715 311636 0 None -131 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1031 20 13 14 -4.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL405165 311636 0 None -131 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1031 20 13 14 -4.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)CCSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
145947419 332426 0 None -323 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1204 30 2 18 7.6 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
CHEMBL4301807 332426 0 None -323 2 Human 6.3 pKd = 6.3 Binding
Binding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assayBinding affinity to V2R (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 1204 30 2 18 7.6 CCN1/C(=C\C=C\C=C\C2=[N+](CC)c3cc(S(=O)(=O)[O-])ccc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCc2nnc(N3CC(Oc4ccc(F)cc4Cl)C3)n2-c2ccc(OC)nc2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm501395b
44385836 316323 0 None None None Bovine 7.3 pKd = 7.3 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1056 20 13 15 -4.5 C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
CHEMBL411357 316323 0 None None None Bovine 7.3 pKd = 7.3 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1056 20 13 15 -4.5 C[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)N(C)C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
70693566 159935 0 None -2 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
CHEMBL2110297 159935 0 None -2 2 Rat 5.3 pKd = 5.3 Binding
Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptorCompound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
ChEMBL 1018 18 12 14 -4.5 CC[C@H](C)[C@H]1NC(=O)[C@]2(CCc3ccccc3C2)NC(=O)CCSSC[C@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1016/s0960-894x(99)00041-4
10011419 197335 0 None -1 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
44294474 197335 0 None -1 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
CHEMBL266643 197335 0 None -1 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
CHEMBL3350125 197335 0 None -1 3 Rat 7.3 pKd = 7.3 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
10011419 197335 0 None -1 3 Rat 8.1 pKd = 8.1 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
44294474 197335 0 None -1 3 Rat 8.1 pKd = 8.1 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
CHEMBL266643 197335 0 None -1 3 Rat 8.1 pKd = 8.1 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
CHEMBL3350125 197335 0 None -1 3 Rat 8.1 pKd = 8.1 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL 1092 17 11 13 -1.0 CC(C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)CC2(CCCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm00010a020
44386247 317221 0 None None None Bovine 8.1 pKd = 8.1 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1042 20 13 15 -4.9 CN(CC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
CHEMBL413249 317221 0 None None None Bovine 8.1 pKd = 8.1 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1042 20 13 15 -4.9 CN(CC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00151a016
44321134 222042 0 None -45 2 Bovine 6.1 pKd = 6.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 963 16 9 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@H]2C(=O)N(C)CC(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL330022 222042 0 None -45 2 Bovine 6.1 pKd = 6.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 963 16 9 14 -3.3 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@H]2C(=O)N(C)CC(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm00028a008
CHEMBL2371674 477422 0 None None None Bovine 8.0 pKd = 8.0 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1027 18 12 14 -3.1 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
CHEMBL217517 485223 0 None None None Bovine 8.0 pKd = 8.0 Binding
Binding affinity against plasma membrane from bovine kidney inner medullaBinding affinity against plasma membrane from bovine kidney inner medulla
ChEMBL 1028 18 13 15 -4.5 CC(C)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N(C)CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00151a016
44321206 197129 0 None -13 2 Bovine 7.0 pKd = 7.0 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1094 20 12 14 -2.9 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
CHEMBL265017 197129 0 None -13 2 Bovine 7.0 pKd = 7.0 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
ChEMBL 1094 20 12 14 -2.9 CN(CC(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)C(=O)[C@@H]1CSSC2(CCCCC2)CC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm00028a008
44419039 274799 0 None -1 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
CHEMBL375324 274799 0 None -1 8 Rat 9.7 pKi = 9.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
44419025 175267 18 None -1 8 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44419026 175267 18 None -1 8 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
74992363 175267 18 None -1 8 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL221436 175267 18 None -1 8 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL435323 175267 18 None -1 8 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL6015151 175267 18 None -1 8 Rat 9.6 pKi = 9.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44419025 175267 18 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44419026 175267 18 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
74992363 175267 18 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL221436 175267 18 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL435323 175267 18 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL6015151 175267 18 None -1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
5311065 484177 30 None 1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
817 484177 30 None 1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL1429 484177 30 None 1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
DB00035 484177 30 None 1 8 Rat 9.5 pKi = 9.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
151171 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
2203 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
732 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1755 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
DB00872 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2010.04.068
44520886 371999 0 None None None Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 628 7 2 4 7.4 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL506235 371999 0 None None None Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 628 7 2 4 7.4 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
216237 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
2226 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
4110 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
CHEMBL344159 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
DB06212 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/jm000108p
146681949 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
2168 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
2810 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
644077 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
CHEMBL373742 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
DB00067 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
P01185 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
P01186 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
P35455 8624 35 None -2 8 Rat 9.4 pKi = 9.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm060928n
CHEMBL2371605 477703 0 None None None Human 9.3 pKi = 9.3 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1138 22 13 14 -1.1 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
178297789 465801 0 None -4 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 479 2 0 8 3.0 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5OCC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6101825 465801 0 None -4 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 479 2 0 8 3.0 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5OCC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
10411308 462175 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
CHEMBL603708 462175 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.8b00697
10411308 462175 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
CHEMBL603708 462175 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
10411308 462175 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
CHEMBL603708 462175 0 None 2 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm901084f
151171 2408 36 None 2 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.ejmech.2024.117069
2203 2408 36 None 2 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.ejmech.2024.117069
732 2408 36 None 2 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.ejmech.2024.117069
CHEMBL1755 2408 36 None 2 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.ejmech.2024.117069
DB00872 2408 36 None 2 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1016/j.ejmech.2024.117069
121301508 350186 8 None 1 4 Human 9.2 pKi = 9.2 Binding
Radiometric AVPR2 binding assay (Eurofins #287610)Radiometric AVPR2 binding assay (Eurofins #287610)
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
CHEMBL4594444 350186 8 None 1 4 Human 9.2 pKi = 9.2 Binding
Radiometric AVPR2 binding assay (Eurofins #287610)Radiometric AVPR2 binding assay (Eurofins #287610)
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
DB16279 350186 8 None 1 4 Human 9.2 pKi = 9.2 Binding
Radiometric AVPR2 binding assay (Eurofins #287610)Radiometric AVPR2 binding assay (Eurofins #287610)
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
135413562 4496 12 None -1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 624 14 3 7 1.1 CN(CCCNC(=O)CCc1ccc(cc1)S(=O)(=O)N(c1ccc(cc1)Cl)CC(=O)NNC1=c2ccccc2=NC1=O)C 10.1021/jm901812z
2194 4496 12 None -1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 624 14 3 7 1.1 CN(CCCNC(=O)CCc1ccc(cc1)S(=O)(=O)N(c1ccc(cc1)Cl)CC(=O)NNC1=c2ccccc2=NC1=O)C 10.1021/jm901812z
CHEMBL445816 4496 12 None -1 5 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 624 14 3 7 1.1 CN(CCCNC(=O)CCc1ccc(cc1)S(=O)(=O)N(c1ccc(cc1)Cl)CC(=O)NNC1=c2ccccc2=NC1=O)C 10.1021/jm901812z
CHEMBL2371604 477702 0 None None None Human 9.2 pKi = 9.2 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1152 22 13 14 -0.9 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
178314842 465884 0 None -1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 465 2 0 7 3.7 Cc1cccc(N2CCN(c3nnc4n3-c3ccc(Cl)cc3CC3(C4)OCCO3)CC2)c1C 10.1016/j.ejmech.2024.117069
CHEMBL6103295 465884 0 None -1 3 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 465 2 0 7 3.7 Cc1cccc(N2CCN(c3nnc4n3-c3ccc(Cl)cc3CC3(C4)OCCO3)CC2)c1C 10.1016/j.ejmech.2024.117069
178299500 466420 0 None -3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.1 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(c5cccc6c5OCC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6145092 466420 0 None -3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.1 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(c5cccc6c5OCC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
2205 8924 8 None -3 5 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
9810140 8924 8 None -3 5 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
CHEMBL307483 8924 8 None -3 5 Rat 9.1 pKi = 9.1 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
178314843 465885 0 None -3 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 481 2 0 9 2.8 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5OCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6103298 465885 0 None -3 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 481 2 0 9 2.8 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5OCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
5311065 484177 30 None 1 8 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
817 484177 30 None 1 8 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL1429 484177 30 None 1 8 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
DB00035 484177 30 None 1 8 Rat 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
71462477 163804 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482382 163804 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172291 163804 0 None None None Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
178298703 465822 0 None -4 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 480 2 0 8 3.9 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(c5cccc6c5OCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6102315 465822 0 None -4 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 480 2 0 8 3.9 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(c5cccc6c5OCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
2198 6959 2 None 46 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
9807249 6959 2 None 46 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1192593 6959 2 None 46 2 Human 9.1 pKi = 9.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 10.1016/j.bmcl.2004.03.083
44382498 196831 0 None None None Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL262482 196831 0 None None None Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
44294575 163541 0 None 8 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
44335358 163541 0 None 8 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
44375638 163541 0 None 8 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL216606 163541 0 None 8 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL406184 163541 0 None 8 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL438014 163541 0 None 8 2 Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL3084974 477843 0 None None None Human 9.0 pKi = 9 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1150 19 11 14 -0.3 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
216237 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
2226 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
4110 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
CHEMBL344159 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
DB06212 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
216237 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1016/j.ejmech.2024.117069
2226 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1016/j.ejmech.2024.117069
4110 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1016/j.ejmech.2024.117069
CHEMBL344159 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1016/j.ejmech.2024.117069
DB06212 8365 53 None 2 7 Human 9.0 pKi = 9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1016/j.ejmech.2024.117069
122322 2781 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00124a025
2217 2781 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00124a025
44294542 2781 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00124a025
44382370 2781 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00124a025
CHEMBL262423 2781 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00124a025
CHEMBL384776 2781 0 None -3 4 Human 9.0 pKi = 9.0 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00124a025
178297835 465526 0 None -2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 491 2 0 7 4.1 Clc1ccc2c(c1)CC1(CCOCC1)Cc1nnc(N3CCN(c4cccc5c4OCC5)CC3)n1-2 10.1016/j.ejmech.2024.117069
CHEMBL6083042 465526 0 None -2 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 491 2 0 7 4.1 Clc1ccc2c(c1)CC1(CCOCC1)Cc1nnc(N3CCN(c4cccc5c4OCC5)CC3)n1-2 10.1016/j.ejmech.2024.117069
2205 8924 8 None -3 5 Human 8.9 pKi = 8.9 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
9810140 8924 8 None -3 5 Human 8.9 pKi = 8.9 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
CHEMBL307483 8924 8 None -3 5 Human 8.9 pKi = 8.9 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1021/jm010544r
2205 8924 8 None -3 5 Rat 8.9 pKi = 8.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1016/s0960-894x(01)00723-5
9810140 8924 8 None -3 5 Rat 8.9 pKi = 8.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1016/s0960-894x(01)00723-5
CHEMBL307483 8924 8 None -3 5 Rat 8.9 pKi = 8.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 10.1016/s0960-894x(01)00723-5
44419025 175267 18 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
44419026 175267 18 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
74992363 175267 18 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL221436 175267 18 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL435323 175267 18 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL6015151 175267 18 None -4 8 Human 8.9 pKi = 8.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1039 17 13 14 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
146681949 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
2168 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
2810 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
644077 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
CHEMBL373742 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
DB00067 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
P01185 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
P01186 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
P35455 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm1016208
155753095 466331 0 None -4 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 472 2 0 8 3.1 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5ncccc5Cl)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6142775 466331 0 None -4 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 472 2 0 8 3.1 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5ncccc5Cl)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL408474 488015 0 None None None Pig 8.9 pKi = 8.9 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1056 19 13 16 -3.7 NCCCC[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(=O)O 10.1021/jm00150a003
146681949 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
2168 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
2810 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
644077 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
CHEMBL373742 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
DB00067 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
P01185 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
P01186 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
P35455 8624 35 None -5 8 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assayDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
44325703 220906 0 None 75 2 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327242 220906 0 None 75 2 Human 8.9 pKi = 8.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(O)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
146681949 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
2168 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
2810 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
644077 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
CHEMBL373742 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
DB00067 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
P01185 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
P01186 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
P35455 8624 35 None -5 8 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1021/jm3006146
CHEMBL2369831 477593 1 None -1 4 Human 8.8 pKi = 8.8 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1041 17 13 15 -4.2 C[C@@H](O)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
44351500 236319 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339943 236319 0 None 1 2 Human 8.8 pKi = 8.8 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
155753084 465588 0 None -39 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 464 1 0 7 3.8 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC5(CC4)OCc4ccccc45)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6087371 465588 0 None -39 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 464 1 0 7 3.8 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC5(CC4)OCc4ccccc45)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
44297505 330720 0 None -7 3 Rat 8.8 pKi = 8.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL424905 330720 0 None -7 3 Rat 8.8 pKi = 8.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
216237 8365 53 None 2 7 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
2226 8365 53 None 2 7 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
4110 8365 53 None 2 7 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
CHEMBL344159 8365 53 None 2 7 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
DB06212 8365 53 None 2 7 Human 8.8 pKi = 8.8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00011
16109443 278920 0 None -9 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1040 18 14 15 -4.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL385739 278920 0 None -9 4 Rat 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1040 18 14 15 -4.0 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44325362 474244 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93603 474244 0 None 354 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
71455302 163803 0 None 194 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482380 163803 0 None 194 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172290 163803 0 None 194 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assayDisplacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44520857 353353 0 None 3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 562 5 2 6 5.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL474072 353353 0 None 3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 562 5 2 6 5.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
167184780 374249 0 None None None Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 566 8 2 4 7.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCc3ccncc3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5189068 374249 0 None None None Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 566 8 2 4 7.3 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCc3ccncc3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
168295452 375401 0 None None None Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 10 1 4 7.2 CCN(CC)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL5207405 375401 0 None None None Human 8.0 pKi = 8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 10 1 4 7.2 CCN(CC)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL2370641 477668 0 None -1 2 Pig 8.0 pKi = 8 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1007 15 8 12 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL2371440 477687 0 None None None Pig 8.0 pKi = 8 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL 1023 17 11 13 -2.7 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
44325732 330307 0 None None None Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
CHEMBL423868 330307 0 None None None Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
44325543 474189 0 None None None Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3cccc(Cl)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93195 474189 0 None None None Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3cccc(Cl)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325731 474192 0 None None None Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(F)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93205 474192 0 None None None Human 8.0 pKi = 8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(F)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44297449 333859 0 None -22 3 Rat 8.0 pKi = 8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL441195 333859 0 None -22 3 Rat 8.0 pKi = 8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
145976546 328610 0 None 7 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 381 2 1 4 4.3 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4204008 328610 0 None 7 2 Human 7.0 pKi = 7 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 381 2 1 4 4.3 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
44419030 317154 22 None -630 4 Rat 7.0 pKi = 7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1025 18 11 14 -1.5 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL412972 317154 22 None -630 4 Rat 7.0 pKi = 7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1025 18 11 14 -1.5 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
177382709 391149 0 None None None Human 6.0 pKi = 6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1175 34 15 13 -1.1 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5564165 391149 0 None None None Human 6.0 pKi = 6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1175 34 15 13 -1.1 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
10303620 473255 0 None -954 4 Rat 6.0 pKi = 6 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
CHEMBL86949 473255 0 None -954 4 Rat 6.0 pKi = 6 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
11092056 216690 0 None -354 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 481 9 0 6 5.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL315524 216690 0 None -354 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 481 9 0 6 5.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCN1CCN(C)CC1 10.1021/jm010544r
44321415 221802 0 None -269 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 467 8 0 6 4.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL329209 221802 0 None -269 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 467 8 0 6 4.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCN1CCN(C)CC1 10.1021/jm010544r
46890484 21357 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084822 21357 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
16109439 274647 0 None -104 4 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1023 15 11 14 -1.7 NC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL375187 274647 0 None -104 4 Rat 6.0 pKi = 6.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1023 15 11 14 -1.7 NC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
46890486 21359 0 None -28 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1084824 21359 0 None -28 2 Human 6.0 pKi = 6.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL2369847 477604 0 None -112 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1087 18 12 14 -2.4 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890528 21360 0 None -199 2 Human 7.0 pKi = 7.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1084825 21360 0 None -199 2 Human 7.0 pKi = 7.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
168294940 375418 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 576 7 1 5 5.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1Br 10.1021/acs.jmedchem.2c00567
CHEMBL5207597 375418 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 576 7 1 5 5.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1Br 10.1021/acs.jmedchem.2c00567
CHEMBL5081323 478923 0 None -2691 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 390 3 1 6 3.5 Cc1ccc2c(c1)CC(O)Cc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
CHEMBL2369835 477595 0 None -7 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1069 19 13 15 -3.7 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
178306359 465585 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 437 2 1 7 2.6 OC1Cc2cc(Cl)ccc2-n2c(nnc2N2CCN(c3cccc4c3OCC4)CC2)C1 10.1016/j.ejmech.2024.117069
CHEMBL6087333 465585 0 None -7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 437 2 1 7 2.6 OC1Cc2cc(Cl)ccc2-n2c(nnc2N2CCN(c3cccc4c3OCC4)CC2)C1 10.1016/j.ejmech.2024.117069
178315333 465982 0 None -64 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 466 3 0 7 3.9 COC1(c2ccccc2)CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
CHEMBL6108984 465982 0 None -64 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 466 3 0 7 3.9 COC1(c2ccccc2)CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
44520864 337150 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 603 5 1 6 6.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5s4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL449517 337150 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 603 5 1 6 6.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5s4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520858 348469 0 None 4 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 590 6 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N(C)C)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL455279 348469 0 None 4 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 590 6 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(N(C)C)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520863 355695 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 553 5 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nccs4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL477868 355695 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 553 5 1 6 5.7 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nccs4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520862 372729 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL514772 372729 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520871 385165 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 513 5 2 5 3.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL521597 385165 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 513 5 2 5 3.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520875 26742 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 609 6 1 5 7.0 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(-c4ccccc4)n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186237 26742 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 609 6 1 5 7.0 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(-c4ccccc4)n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44520883 26961 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187505 26961 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 564 5 1 4 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
164946750 373223 1 None None None Human 8.0 pKi = 8.0 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5173331 373223 1 None None None Human 8.0 pKi = 8.0 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 574 8 2 5 6.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44351384 235863 0 None None None Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 980 18 10 13 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCNC(N)C=N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL338798 235863 0 None None None Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 980 18 10 13 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCNC(N)C=N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351279 316986 0 None None None Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3cccc(CN)c3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL412732 316986 0 None None None Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3cccc(CN)c3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44325689 473065 0 None 44 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL90657 473065 0 None 44 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325505 474335 0 None 562 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL94133 474335 0 None 562 2 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1790551 484809 0 None -229 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 795 8 2 9 2.1 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2C[C@@H](CN(C)C)C=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
44361403 67461 1 None -457 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 491 5 0 5 4.1 CC(=O)N1CCCC(COc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)C1 10.1021/jm00023a002
CHEMBL142324 67461 1 None -457 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 491 5 0 5 4.1 CC(=O)N1CCCC(COc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)C1 10.1021/jm00023a002
44361387 238172 0 None -724 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 505 6 0 5 4.6 CC(=O)N1CCCCC1CCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
CHEMBL344752 238172 0 None -724 5 Rat 5.0 pKi = 5.0 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 505 6 0 5 4.6 CC(=O)N1CCCCC1CCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
10863737 473582 0 None -1202 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 477 11 0 6 6.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCn1ccnc1 10.1021/jm010544r
CHEMBL89177 473582 0 None -1202 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 477 11 0 6 6.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCn1ccnc1 10.1021/jm010544r
CHEMBL2369837 477597 0 None -6165 4 Human 5.0 pKi = 5.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 20 13 15 -3.5 NCCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
11366713 274628 0 None -2511 8 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1054 19 13 15 -3.9 NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL375096 274628 0 None -2511 8 Human 6.0 pKi = 6.0 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1054 19 13 15 -3.9 NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
145974638 329526 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 347 2 1 4 3.7 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4215696 329526 0 None -7 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 347 2 1 4 3.7 Cc1ccn(-c2ccc(C(=O)N3CCCC(O)c4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL2369830 477592 0 None -275 4 Human 6.9 pKi = 6.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 19 12 14 -2.4 CCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
46890572 21678 0 None -1148 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 4.8 CNC(=O)c1cccc(-c2ccc(C(=O)N3C[C@]4(C)C[C@H]3CC(C)(C)C4)cc2OC)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086294 21678 0 None -1148 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 4.8 CNC(=O)c1cccc(-c2ccc(C(=O)N3C[C@]4(C)C[C@H]3CC(C)(C)C4)cc2OC)c1 10.1016/j.bmcl.2010.04.068
154638544 391765 0 None -1659 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 451 5 1 6 4.9 CC(C)N[C@@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.3c01868
CHEMBL5574495 391765 0 None -1659 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 451 5 1 6 4.9 CC(C)N[C@@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.3c01868
10208389 160148 0 None -8128 4 Rat 4.9 pKi = 4.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL2112339 160148 0 None -8128 4 Rat 4.9 pKi = 4.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
44520865 372282 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 586 5 2 5 6.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5[nH]4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL510500 372282 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 586 5 2 5 6.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4nc5ccccc5[nH]4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
167183380 373662 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 587 8 2 5 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCN(C)CC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5180200 373662 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 587 8 2 5 5.9 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCN(C)CC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
10674616 374498 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 572 8 1 4 7.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5192961 374498 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 572 8 1 4 7.3 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
168290973 374929 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCN(CCCN2CCOCC2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL5199628 374929 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CCCN(CCCN2CCOCC2)c2ccccc21 10.1021/acs.jmedchem.2c00567
122322 2781 0 None -8 4 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
2217 2781 0 None -8 4 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
44294542 2781 0 None -8 4 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
44382370 2781 0 None -8 4 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
CHEMBL262423 2781 0 None -8 4 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
CHEMBL384776 2781 0 None -8 4 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
44294575 163541 0 None -8 2 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44335358 163541 0 None -8 2 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44375638 163541 0 None -8 2 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL216606 163541 0 None -8 2 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL406184 163541 0 None -8 2 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL438014 163541 0 None -8 2 Pig 7.9 pKi = 7.9 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
71460754 163814 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1141 17 2 11 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)N4CCN(CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)CC4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172392 163814 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1141 17 2 11 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)N4CCN(CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)CC4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
44419028 197233 21 None -10 8 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
CHEMBL265858 197233 21 None -10 8 Rat 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm060928n
10615 1182 36 None -1949 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
46200932 1182 36 None -1949 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
CHEMBL4297183 1182 36 None -1949 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
DB14823 1182 36 None -1949 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.1c00863
46890529 21064 0 None -47 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@@]2(C)C[C@@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1083730 21064 0 None -47 2 Human 5.9 pKi = 5.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(-c2ccccc2C)c(Cl)cc1C(=O)N1C[C@@]2(C)C[C@@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
145976648 328808 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 293 3 0 1 4.6 CCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL4206482 328808 0 None -1 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 293 3 0 1 4.6 CCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
172441826 387419 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccccc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5395776 387419 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccccc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
46890152 21082 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1083765 21082 0 None -3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
10164478 473633 0 None -1174 4 Rat 5.9 pKi = 5.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL89552 473633 0 None -1174 4 Rat 5.9 pKi = 5.9 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
118734336 237398 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416770 237398 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
11569194 144330 0 None -63 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 479 7 2 3 3.5 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc(F)cc1 10.1021/jm901812z
11619939 144330 0 None -63 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 479 7 2 3 3.5 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc(F)cc1 10.1021/jm901812z
CHEMBL197793 144330 0 None -63 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 479 7 2 3 3.5 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc(F)cc1 10.1021/jm901812z
CHEMBL427353 144330 0 None -63 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 479 7 2 3 3.5 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc(F)cc1 10.1021/jm901812z
25212177 348862 6 None -2818 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to vasopressin V2 receptor by filtration assayBinding affinity to vasopressin V2 receptor by filtration assay
ChEMBL 463 7 0 7 3.9 COc1ccc(N(Cc2ccc(-c3ccccc3C)cn2)S(=O)(=O)c2cn(C)c(C)n2)cn1 10.1016/j.bmcl.2008.11.018
CHEMBL456263 348862 6 None -2818 4 Human 4.9 pKi = 4.9 Binding
Binding affinity to vasopressin V2 receptor by filtration assayBinding affinity to vasopressin V2 receptor by filtration assay
ChEMBL 463 7 0 7 3.9 COc1ccc(N(Cc2ccc(-c3ccccc3C)cn2)S(=O)(=O)c2cn(C)c(C)n2)cn1 10.1016/j.bmcl.2008.11.018
178306361 465586 0 None -51 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 505 2 0 7 3.4 O=C1c2ccccc2CCN1C1CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
CHEMBL6087335 465586 0 None -51 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 505 2 0 7 3.4 O=C1c2ccccc2CCN1C1CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
138687887 465655 0 None -19 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 450 3 1 6 3.1 Cc1cccc(N2CCN(c3nnc4n3-c3ccc(Cl)cc3CC(C(N)=O)C4)CC2)c1C 10.1016/j.ejmech.2024.117069
CHEMBL6091822 465655 0 None -19 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 450 3 1 6 3.1 Cc1cccc(N2CCN(c3nnc4n3-c3ccc(Cl)cc3CC(C(N)=O)C4)CC2)c1C 10.1016/j.ejmech.2024.117069
44520849 461472 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 503 5 2 4 4.4 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL606464 461472 0 None -1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 503 5 2 4 4.4 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
168289573 374890 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5198918 374890 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 572 8 2 4 7.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCN3CCCCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
168286187 374549 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 587 8 1 5 6.1 CN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
CHEMBL5193621 374549 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 587 8 1 5 6.1 CN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
44335329 332598 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL430841 332598 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 561 4 1 3 7.6 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@@H]4C5CCC(C5)N4Cc4cc(Cl)ccc43)cc2)cc1 10.1016/s0960-894x(02)00649-2
44325704 221794 0 None 64 2 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329141 221794 0 None 64 2 Human 7.9 pKi = 7.9 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1cc(O)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44316235 316115 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1011 16 12 14 -3.6 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL411148 316115 0 None -2 4 Human 7.9 pKi = 7.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1011 16 12 14 -3.6 C[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
9938406 184110 1 None -181 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Vasopressin V2 receptor by using functional assayBinding affinity towards cloned human Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
CHEMBL24526 184110 1 None -181 6 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Vasopressin V2 receptor by using functional assayBinding affinity towards cloned human Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
46890101 21623 0 None -181 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2cccnc12 10.1016/j.bmcl.2010.04.068
CHEMBL1086070 21623 0 None -181 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2cccnc12 10.1016/j.bmcl.2010.04.068
53349471 237401 0 None -22 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416774 237401 0 None -22 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
44351328 43245 0 None None None Pig 6.9 pKi = 6.9 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 909 10 7 11 2.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL129274 43245 0 None None None Pig 6.9 pKi = 6.9 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 909 10 7 11 2.3 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44419039 274799 0 None -1023 8 Human 6.9 pKi = 6.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
CHEMBL375324 274799 0 None -1023 8 Human 6.9 pKi = 6.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1096 20 14 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890187 21574 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085851 21574 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
172452353 388772 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1cccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5424001 388772 0 None None None Human 6.9 pKi = 6.9 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1cccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/acs.jmedchem.2c01625
168272611 373476 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5177490 373476 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(-c2ccccc2)cc1 10.1021/acs.jmedchem.2c00567
44314081 469834 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2cccc(C(=O)N3CCC(N4CCCCC4)CC3)c2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL76498 469834 0 None -2 2 Rat 5.9 pKi = 5.9 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2cccc(C(=O)N3CCC(N4CCCCC4)CC3)c2)cc1 10.1016/s0960-894x(01)00723-5
44275104 197597 0 None -1737 4 Human 6.9 pKi = 6.9 Binding
Compound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorCompound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1127 32 14 14 -3.9 CN(C(=O)Cc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
CHEMBL269012 197597 0 None -1737 4 Human 6.9 pKi = 6.9 Binding
Compound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorCompound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1127 32 14 14 -3.9 CN(C(=O)Cc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
CHEMBL2369836 477596 0 None -2630 4 Human 5.9 pKi = 5.9 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1110 21 14 15 -4.2 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCCN=C(N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
44520860 353511 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cnccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL474274 353511 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cnccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520880 26845 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1186825 26845 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.0 CC1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
44520882 26849 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186831 26849 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44520852 432986 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 537 5 2 4 4.7 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL593325 432986 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 537 5 2 4 4.7 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
44520851 443439 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 503 5 2 4 4.4 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL594026 443439 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 503 5 2 4 4.4 C[C@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2009.10.038
71453576 163807 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172294 163807 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
71462477 163804 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482382 163804 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172291 163804 0 None None None Human 7.9 pKi = 7.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1573 42 5 20 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
56665480 125919 0 None -91 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790544 125919 0 None -91 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
137637867 312145 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4064556 312145 0 None -50 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
70685417 155339 0 None -141 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C/I)c2)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017867 155339 0 None -141 3 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C/I)c2)CC1 10.1016/j.bmc.2012.02.019
177382707 391734 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1163 36 15 14 -2.0 CCOc1ccc(C[C@H](NC(=O)[C@@H](Cc2ccc(OCC)cc2)NC(=O)CC)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5573762 391734 0 None None None Human 5.9 pKi = 5.9 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1163 36 15 14 -2.0 CCOc1ccc(C[C@H](NC(=O)[C@@H](Cc2ccc(OCC)cc2)NC(=O)CC)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
10929819 216600 0 None -371 2 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 565 15 0 6 7.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL314908 216600 0 None -371 2 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 565 15 0 6 7.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
10208389 160148 0 None -10000 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL2112339 160148 0 None -10000 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 11 0 6 6.4 Cc1cccc(OCCCCCCN2CCN(C)CC2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
46890707 21056 0 None -19 2 Human 7.8 pKi = 7.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1083703 21056 0 None -19 2 Human 7.8 pKi = 7.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 419 3 0 3 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1csc2ccccc12 10.1016/j.bmcl.2010.04.068
9807250 155107 0 None 58 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL2110044 155107 0 None 58 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.1 O=C(Nc1ccc(C(=O)N2C[C@@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325733 474193 0 None None None Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 549 5 1 5 6.2 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
CHEMBL93209 474193 0 None None None Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 549 5 1 5 6.2 COc1cc(NC(=O)c2ccccc2-c2ccccc2)ccc1C(=O)N1CC2CSCCN2Cc2ccccc21 10.1016/j.bmcl.2004.03.083
9938406 184110 1 None -213 6 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards rat kidney Vasopressin V2 receptor by using functional assayBinding affinity towards rat kidney Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
CHEMBL24526 184110 1 None -213 6 Rat 6.8 pKi = 6.8 Binding
Binding affinity towards rat kidney Vasopressin V2 receptor by using functional assayBinding affinity towards rat kidney Vasopressin V2 receptor by using functional assay
ChEMBL 589 7 0 6 4.7 CC(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)c(OCC(F)(F)F)c2)CC1 10.1016/s0960-894x(99)00181-x
CHEMBL1790548 484807 0 None -50 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 742 6 4 8 1.3 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCNN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
CHEMBL1790548 484807 0 None -50 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 742 6 4 8 1.3 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCNN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
2042 8014 41 None -1905 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm501395b
2176 8014 41 None -1905 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm501395b
439302 8014 41 None -1905 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm501395b
CHEMBL395429 8014 41 None -1905 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm501395b
54585227 123947 0 None -912 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1042 18 12 15 -1.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765669 123947 0 None -912 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1042 18 12 15 -1.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
177382710 391682 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1185 34 15 13 -1.3 CCOc1ccc(C[C@@H](NC(=O)c2ccccc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5572965 391682 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1185 34 15 13 -1.3 CCOc1ccc(C[C@@H](NC(=O)c2ccccc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
44520856 372186 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 577 6 1 6 5.6 COc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
CHEMBL509183 372186 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 577 6 1 6 5.6 COc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
44520881 26846 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1186826 26846 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 550 5 1 4 6.1 CC1CCCN1c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
44520850 442440 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 537 5 2 4 4.7 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
CHEMBL594488 442440 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 537 5 2 4 4.7 C[C@@H]1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)C1 10.1016/j.bmc.2009.10.038
71455306 163815 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1204 26 3 13 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172393 163815 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1204 26 3 13 9.7 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
132822146 313145 0 None -23 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4076436 313145 0 None -23 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
47177173 329382 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 377 1 0 1 4.3 O=C(c1ccc(I)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4213812 329382 0 None -3 3 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 377 1 0 1 4.3 O=C(c1ccc(I)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
44335356 19563 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL106229 19563 0 None 5 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 385 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCNc3ccccc32)cc1 10.1016/s0960-894x(02)00649-2
CHEMBL1790542 484804 0 None -346 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 754 6 3 8 1.3 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC(=O)NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
10615 1182 36 None -1949 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.3c01868
46200932 1182 36 None -1949 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.3c01868
CHEMBL4297183 1182 36 None -1949 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.3c01868
DB14823 1182 36 None -1949 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 10.1021/acs.jmedchem.3c01868
177382708 391144 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1133 34 15 13 -2.1 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5564111 391144 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1133 34 15 13 -2.1 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(C)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL339118 487010 0 None -19 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 740 6 2 6 3.1 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
44297525 197135 0 None -89125 3 Rat 4.8 pKi = 4.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL265048 197135 0 None -89125 3 Rat 4.8 pKi = 4.8 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1329 38 15 16 -1.8 CN(C(=O)CCc1cccc(N=[N+]=[N-])c1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
178313968 465662 0 None -1258 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 451 4 1 6 3.3 COC1(c2ccccc2)CCN(c2nnc3n2-c2ccc(Cl)cc2CC(C(N)=O)C3)CC1 10.1016/j.ejmech.2024.117069
CHEMBL6092017 465662 0 None -1258 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 451 4 1 6 3.3 COC1(c2ccccc2)CCN(c2nnc3n2-c2ccc(Cl)cc2CC(C(N)=O)C3)CC1 10.1016/j.ejmech.2024.117069
10444 4740 20 None -7 3 Human 5.8 pKi = 5.8 Binding
Displacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assayDisplacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
145711714 4740 20 None -7 3 Human 5.8 pKi = 5.8 Binding
Displacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assayDisplacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
CHEMBL4204210 4740 20 None -7 3 Human 5.8 pKi = 5.8 Binding
Displacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assayDisplacement of DY647 from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells by TR-FRET assay
ChEMBL 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 10.1021/acs.jmedchem.8b00697
53239961 138909 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 491 2 3 5 5.1 Nc1nc(-c2ccc3c(c2)C(=Cc2cc(Br)c(O)c(Br)c2)C(=O)N3)cs1 10.1016/s0960-894x(01)00723-5
CHEMBL1852697 138909 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 491 2 3 5 5.1 Nc1nc(-c2ccc3c(c2)C(=Cc2cc(Br)c(O)c(Br)c2)C(=O)N3)cs1 10.1016/s0960-894x(01)00723-5
172452804 389050 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 458 3 0 4 7.2 Cc1ccc(F)cc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5430804 389050 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 458 3 0 4 7.2 Cc1ccc(F)cc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
44325377 221084 0 None None None Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2)c(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL328227 221084 0 None None None Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2)c(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
132822145 315382 0 None -26 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4102459 315382 0 None -26 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
44520885 26718 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 565 5 1 5 4.9 CN1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)CC1 10.1016/j.bmc.2008.09.039
CHEMBL1186071 26718 0 None None None Human 6.8 pKi = 6.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 565 5 1 5 4.9 CN1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)CC1 10.1016/j.bmc.2008.09.039
46890154 21180 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 423 2 0 2 7.3 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1084070 21180 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 423 2 0 2 7.3 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
46890214 21420 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 417 2 0 1 7.2 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085123 21420 0 None -1 2 Human 6.8 pKi = 6.8 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 417 2 0 1 7.2 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
3482 8039 36 None -229 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
60943 8039 36 None -229 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
CHEMBL419667 8039 36 None -229 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
10164478 473633 0 None -1698 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL89552 473633 0 None -1698 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 509 11 0 6 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCN(C)CC1 10.1021/jm010544r
137648906 313282 0 None -22 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4078185 313282 0 None -22 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
44520868 355865 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 498 5 1 4 5.4 CCCNC(=O)/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(C)n3)cc2Cl)CCC1(F)F 10.1016/j.bmc.2009.03.001
CHEMBL478083 355865 0 None -1 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 498 5 1 4 5.4 CCCNC(=O)/C=C1/c2ccccc2N(C(=O)c2ccc(-n3ccc(C)n3)cc2Cl)CCC1(F)F 10.1016/j.bmc.2009.03.001
44520874 26943 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 575 6 1 5 6.4 CC(C)c1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL1187362 26943 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 575 6 1 5 6.4 CC(C)c1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
168277203 373724 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCN(CCCN4CCOCC4)c4ccccc43)cc2)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5181318 373724 0 None None None Human 7.8 pKi = 7.8 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 8 1 5 6.5 Cc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3CCCN(CCCN4CCOCC4)c4ccccc43)cc2)cc1 10.1021/acs.jmedchem.2c00567
44325545 474047 0 None None None Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.5 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)c(F)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL92187 474047 0 None None None Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 555 4 1 4 6.5 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)c(F)c32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44335386 217633 0 None 14 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
CHEMBL319433 217633 0 None 14 2 Human 6.8 pKi = 6.8 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 489 3 1 3 5.7 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1F 10.1016/s0960-894x(02)00649-2
57519948 155341 4 None -112 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2017869 155341 4 None -112 3 Human 5.8 pKi = 5.8 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmcl.2013.07.045
118734334 237395 0 None -10 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416767 237395 0 None -10 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
57519948 155341 4 None -112 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017869 155341 4 None -112 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 587 9 0 6 3.4 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OCCF)c2)CC1 10.1016/j.bmc.2012.02.019
14310031 391512 9 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
177382701 391512 9 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5570228 391512 9 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5573809 391512 9 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
177382703 391805 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1169 34 15 13 -1.2 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5575105 391805 0 None None None Human 5.8 pKi = 5.8 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1169 34 15 13 -1.2 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL52176 489105 0 None -229 2 Rat 5.8 pKi = 5.8 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 755 6 5 7 1.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCCCN2C(=O)[C@@H]2CCCCN2C1=O 10.1021/jm00169a001
10483105 174420 1 None -34 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1016/j.bmcl.2012.10.116
CHEMBL2391300 174420 1 None -34 4 Human 6.7 pKi = 6.7 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 568 10 2 7 1.8 CN[C@@H](CCS(C)(=O)=O)C(=O)N[C@H]1C[C@H]2CC[C@]1(CS(=O)(=O)N1CCN(c3ccccc3C)CC1)C2(C)C 10.1016/j.bmcl.2012.10.116
46890614 21002 0 None -416 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 397 3 0 2 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083443 21002 0 None -416 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 397 3 0 2 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1 10.1016/j.bmcl.2010.04.068
118734334 237395 0 None -10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416767 237395 0 None -10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
10304617 473211 0 None -1819 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL86667 473211 0 None -1819 4 Rat 5.7 pKi = 5.7 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
71451750 163805 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6C)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172292 163805 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)[O-])cc3S(=O)(=O)NCCOCCOCCOCCn3cc(CNC(=O)CCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6C)cc5)c5ccccc54)nn3)c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
46890569 21617 0 None -74 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 439 4 0 2 7.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1086052 21617 0 None -74 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 439 4 0 2 7.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.04.068
46890099 21621 0 None -331 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cnc2ccccc2c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086068 21621 0 None -331 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cnc2ccccc2c1 10.1016/j.bmcl.2010.04.068
44520854 374978 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 546 5 1 4 6.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL520040 374978 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 546 5 1 4 6.2 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
9959174 386967 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL528996 386967 0 None -3 3 Rat 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
44294532 311694 0 None None None Pig 7.7 pKi = 7.7 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL405818 311694 0 None None None Pig 7.7 pKi = 7.7 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
10304617 473211 0 None -1905 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL86667 473211 0 None -1905 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 625 8 0 6 7.9 Cc1cccc(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
178315364 466598 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 467 3 0 8 3.1 COc1ccccc1N1CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
CHEMBL6149769 466598 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 467 3 0 8 3.1 COc1ccccc1N1CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
CHEMBL2369829 477591 0 None -1 4 Human 8.7 pKi = 8.7 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1025 17 12 14 -3.2 CC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
178295831 466158 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 479 2 0 8 3.0 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5CCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6120797 466158 0 None -5 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 479 2 0 8 3.0 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5CCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
172997 4754 54 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
2238 4754 54 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
CHEMBL49429 4754 54 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
DB06666 4754 54 None 64 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/j.bmcl.2004.03.083
216237 8365 53 None 2 7 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
2226 8365 53 None 2 7 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
4110 8365 53 None 2 7 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
CHEMBL344159 8365 53 None 2 7 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
DB06212 8365 53 None 2 7 Human 8.6 pKi = 8.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.2c00567
11740743 38028 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
CHEMBL119793 38028 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
178315745 466655 0 None -5 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 479 2 0 8 3.1 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5COC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6151152 466655 0 None -5 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 479 2 0 8 3.1 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5cccc6c5COC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
44325345 221059 0 None 75 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL328079 221059 0 None 75 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 493 3 1 4 4.9 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
44325607 221643 0 None 660 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL329026 221643 0 None 660 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)cc1 10.1016/j.bmcl.2004.03.083
44351500 236319 0 None -1 2 Pig 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339943 236319 0 None -1 2 Pig 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 995 16 10 12 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
155753136 466621 0 None -199 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 453 3 0 8 3.2 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(Oc5ccccn5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6150478 466621 0 None -199 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 453 3 0 8 3.2 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(Oc5ccccn5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
44520853 368809 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL486268 368809 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccncc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520878 26717 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 583 5 1 5 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cc4ccccc4n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186070 26717 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 583 5 1 5 6.5 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cc4ccccc4n3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
44563579 348637 0 None None None Human 6.7 pKi = 6.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL455699 348637 0 None None None Human 6.7 pKi = 6.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 449 4 2 2 5.6 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)Nc1c(F)cccc1F 10.1021/jm8008162
CHEMBL5070075 478437 0 None -660 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 410 3 1 6 3.9 O[C@@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
44520884 26720 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 579 6 1 5 5.3 CN(C)C1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
CHEMBL1186088 26720 0 None None None Human 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 579 6 1 5 5.3 CN(C)C1CCN(c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)C1 10.1016/j.bmc.2008.09.039
2249 4540 14 None -54 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
9872389 4540 14 None -54 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
CHEMBL1253853 4540 14 None -54 7 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
10298385 350829 38 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
25178787 350829 38 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL461520 350829 38 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
CHEMBL518043 350829 38 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
DB11734 350829 38 None None None Human 5.7 pKi = 5.7 Binding
Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assayBinding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
ChEMBL 462 4 1 3 3.7 Cc1cc(C(=O)N2CCCCc3ccccc32)ccc1CNC(=O)N1CCC[C@@H]1C(=O)N(C)C 10.1021/jm8008162
46890438 20916 0 None -4073 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083094 20916 0 None -4073 2 Human 6.7 pKi = 6.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
44314342 203135 0 None -6 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 604 7 1 5 6.9 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2-c2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL307487 203135 0 None -6 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 604 7 1 5 6.9 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2-c2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
46890054 21248 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 443 4 0 3 6.6 COc1ccc2cc(-c3ccc(C(=O)N4C[C@]5(C)C[C@H]4CC(C)(C)C5)cc3OC)ccc2c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084386 21248 0 None -19 2 Human 5.7 pKi = 5.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 443 4 0 3 6.6 COc1ccc2cc(-c3ccc(C(=O)N4C[C@]5(C)C[C@H]4CC(C)(C)C5)cc3OC)ccc2c1 10.1016/j.bmcl.2010.04.068
46890185 21523 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 549 3 0 2 10.1 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4csc5ccccc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085624 21523 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 549 3 0 2 10.1 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4csc5ccccc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
19608069 237394 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 402 3 1 3 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416766 237394 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 402 3 1 3 5.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
178316307 466195 0 None -74 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 9 3.2 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5nccc6ccoc56)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6132850 466195 0 None -74 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 9 3.2 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5nccc6ccoc56)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
10119966 368679 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL486064 368679 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnc4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520873 26963 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 6 1 5 5.9 CCc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL1187511 26963 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 6 1 5 5.9 CCc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
16109440 317156 0 None -831 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 997 16 11 14 -2.3 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL412973 317156 0 None -831 4 Rat 6.7 pKi = 6.7 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 997 16 11 14 -2.3 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
172458738 389343 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N/c2cccc(-c3ccccc3)c2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5437303 389343 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N/c2cccc(-c3ccccc3)c2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
154638688 391903 0 None -2187 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 451 5 1 6 4.9 CC(C)NC1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.3c01868
CHEMBL5579703 391903 0 None -2187 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as inhibition constant by Cheng-Prusoff equation analysis
ChEMBL 451 5 1 6 4.9 CC(C)NC1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.3c01868
44520870 370210 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 514 5 2 5 4.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL490249 370210 0 None 10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 514 5 2 5 4.1 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCC(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44520879 27000 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1187728 27000 0 None None None Human 7.7 pKi = 7.7 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 536 5 1 4 5.7 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(N3CCCC3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1790549 484808 0 None -18 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 758 6 4 9 1.4 CC[C@@H](C)[C@H]1C(=O)N2NCCC[C@@H]2C(=O)N2NCCC[C@H]2C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N2CCC[C@H]2C(=O)N[C@H](Cc2ccccc2)C(=O)N1O 10.1021/jm00171a003
14310031 391512 9 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
177382701 391512 9 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5570228 391512 9 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5573809 391512 9 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1119 34 15 13 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
177382706 392163 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1149 35 15 14 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5591604 392163 0 None None None Human 5.7 pKi = 5.7 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1149 35 15 14 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(OC)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
54584267 123945 0 None -35481 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1154 25 12 15 0.2 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765667 123945 0 None -35481 4 Human 4.7 pKi = 4.7 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1154 25 12 15 0.2 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
44314536 469867 0 None -1 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2ccccc2C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL76763 469867 0 None -1 2 Rat 5.7 pKi = 5.7 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 620 8 1 6 7.0 Cc1occc1C(=O)Nc1ccc(C(=O)N(C)c2ccccc2Oc2ccccc2C(=O)N2CCC(N3CCCCC3)CC2)cc1 10.1016/s0960-894x(01)00723-5
168277882 373600 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 9 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5179440 373600 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 588 9 1 5 6.6 O=C(Nc1ccc(C(=O)N2CCCN(CCCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
5311065 484177 30 None -7 8 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
817 484177 30 None -7 8 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
CHEMBL1429 484177 30 None -7 8 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
DB00035 484177 30 None -7 8 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
46890153 21179 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1084069 21179 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 457 2 0 2 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3csc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
145975166 328759 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 328 2 0 2 4.7 O=C(c1ccc(-c2cccnc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4205970 328759 0 None -3 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 328 2 0 2 4.7 O=C(c1ccc(-c2cccnc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
46890053 21185 0 None -141 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084112 21185 0 None -141 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2010.04.068
178315169 465430 0 None -29 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 507 2 0 8 3.8 CC1(C)Cc2cccc(N3CCN(c4nnc5n4-c4ccc(Cl)cc4CC4(C5)OCCO4)CC3)c2O1 10.1016/j.ejmech.2024.117069
CHEMBL6078057 465430 0 None -29 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 507 2 0 8 3.8 CC1(C)Cc2cccc(N3CCN(c4nnc5n4-c4ccc(Cl)cc4CC4(C5)OCCO4)CC3)c2O1 10.1016/j.ejmech.2024.117069
CHEMBL2369845 477603 0 None -30 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1039 18 12 14 -2.8 CCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL2369838 477598 0 None -12 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1027 17 13 15 -4.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
16109446 274035 0 None -630 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 983 15 11 14 -2.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL373968 274035 0 None -630 4 Rat 6.6 pKi = 6.6 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 983 15 11 14 -2.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44297632 202117 0 None -57 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 780 6 3 6 2.9 CC[C@@H](C)[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)N2CCN(CC2)C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
CHEMBL301708 202117 0 None -57 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 780 6 3 6 2.9 CC[C@@H](C)[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)N2CCN(CC2)C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
44316241 197234 0 None -6165 8 Human 6.6 pKi = 6.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
44419029 197234 0 None -6165 8 Human 6.6 pKi = 6.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL265859 197234 0 None -6165 8 Human 6.6 pKi = 6.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL268306 197234 0 None -6165 8 Human 6.6 pKi = 6.6 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
5034737 473315 9 None -20 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 341 4 0 4 4.9 COc1ccccc1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL87351 473315 9 None -20 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 341 4 0 4 4.9 COc1ccccc1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
10142915 473387 0 None -549 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 12 0 6 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL87887 473387 0 None -549 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 12 0 6 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
46890055 20781 0 None -2290 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 398 3 0 3 5.5 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccnc1Cl 10.1016/j.bmcl.2010.04.068
CHEMBL1082493 20781 0 None -2290 2 Human 5.6 pKi = 5.6 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 398 3 0 3 5.5 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccnc1Cl 10.1016/j.bmcl.2010.04.068
42629368 366052 0 None 251 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478902 366052 0 None 251 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 457 3 1 4 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44325895 473118 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96731 473118 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
71460752 163812 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1001 14 2 9 10.1 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172390 163812 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1001 14 2 9 10.1 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2372926 485914 0 None -5 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 784 8 2 7 3.5 CCOc1ccc(C[C@H]2NC(=O)[C@@H]3CCCN3C(=O)[C@@H](Cc3ccccc3)N(C)C(=O)[C@@H]3CCCCN3C(=O)[C@H]3CCCCN3C(=O)[C@H]([C@@H](C)CC)NC2=O)cc1 10.1021/jm00169a001
1103817 40884 7 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cellsDisplacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cells
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm050645f
CHEMBL1254117 40884 7 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cellsDisplacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cells
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm050645f
1103817 40884 7 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm901812z
CHEMBL1254117 40884 7 None -602 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 492 8 2 6 3.1 CCOc1ccc(S(=O)(=O)N(CC(=O)N/N=C2\C(=O)Nc3ccccc32)c2ccc(C)cc2)cc1 10.1021/jm901812z
42611262 354432 0 None -251 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assayDisplacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assay
ChEMBL 349 6 0 2 4.7 Cc1cc(C(=O)N(CC2CC2)CC2CCCO2)ccc1-c1ccccc1 10.1016/j.bmcl.2008.11.064
CHEMBL475395 354432 0 None -251 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assayDisplacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assay
ChEMBL 349 6 0 2 4.7 Cc1cc(C(=O)N(CC2CC2)CC2CCCO2)ccc1-c1ccccc1 10.1016/j.bmcl.2008.11.064
138688095 466218 0 None -33 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 456 3 1 6 3.1 NC(=O)C1Cc2cc(Cl)ccc2-n2c(nnc2N2CCN(c3cccc(Cl)c3)CC2)C1 10.1016/j.ejmech.2024.117069
CHEMBL6133355 466218 0 None -33 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 456 3 1 6 3.1 NC(=O)C1Cc2cc(Cl)ccc2-n2c(nnc2N2CCN(c3cccc(Cl)c3)CC2)C1 10.1016/j.ejmech.2024.117069
178309678 465664 0 None -87 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.1 Clc1ccc2c(c1)CC1(Cc3nnc(C4CCN(c5cccc6c5CCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6092084 465664 0 None -87 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.1 Clc1ccc2c(c1)CC1(Cc3nnc(C4CCN(c5cccc6c5CCO6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
178299938 466223 0 None -125 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.2 Clc1ccc2c(c1)CC1(Cc3nnc(C4CCN(c5cccc6c5COC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6133453 466223 0 None -125 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.2 Clc1ccc2c(c1)CC1(Cc3nnc(C4CCN(c5cccc6c5COC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
168270081 373151 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5172250 373151 0 None None None Human 7.6 pKi = 7.6 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 560 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
44294573 317597 0 None -3 2 Pig 7.6 pKi = 7.6 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL416114 317597 0 None -3 2 Pig 7.6 pKi = 7.6 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
71451749 163801 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL2172288 163801 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1205 25 7 15 9.2 O=C(CCC(=O)NC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21)NCc1cn(CCOCCOCCOCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)nn1 10.1021/jm3006146
CHEMBL300642 486409 0 None -32 2 Rat 6.6 pKi = 6.6 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 779 6 3 6 3.6 CC[C@H](C)[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
177382704 392396 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1131 31 14 13 -2.2 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N2Cc3ccccc3C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5595563 392396 0 None None None Human 5.6 pKi = 5.6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1131 31 14 13 -2.2 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N2Cc3ccccc3C[C@H]2C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
44520866 355487 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 536 5 1 5 5.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccco4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL477456 355487 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 536 5 1 5 5.8 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccco4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44351385 235905 0 None None None Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 910 14 8 11 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339073 235905 0 None None None Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 910 14 8 11 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
172451749 388304 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N/c2ccccc2-c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5414365 388304 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N/c2ccccc2-c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
44351440 333457 0 None None None Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1036 17 8 12 3.0 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL437674 333457 0 None None None Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1036 17 8 12 3.0 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351357 311650 0 None None None Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3ccc(CN)cc3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL405308 311650 0 None None None Pig 7.6 pKi = 7.6 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1055 14 8 12 3.1 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCc3ccc(CN)cc3)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
2253 4548 22 None -37153 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
5311202 4548 22 None -37153 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
CHEMBL306645 4548 22 None -37153 6 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
167312309 388853 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c01625
CHEMBL5425852 388853 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c01625
CHEMBL5427331 388853 0 None None None Human 6.6 pKi = 6.6 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c01625
145978570 328785 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 331 2 0 3 4.2 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4206233 328785 0 None -8 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 331 2 0 3 4.2 Cc1ccn(-c2ccc(C(=O)N3CCCCc4ccccc43)cc2)n1 10.1021/acs.jmedchem.8b00697
44275447 196766 0 None -354 4 Human 6.6 pKi = 6.6 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1111 32 13 13 -3.6 CN(C(=O)Cc1ccccc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
CHEMBL262035 196766 0 None -354 4 Human 6.6 pKi = 6.6 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1111 32 13 13 -3.6 CN(C(=O)Cc1ccccc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm9804782
3482 8039 36 None -371 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
60943 8039 36 None -371 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
CHEMBL419667 8039 36 None -371 4 Rat 6.5 pKi = 6.5 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10.1021/jm010544r
172449149 387959 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 444 3 0 4 6.9 O=C(c1ccc(/N=N\c2ccc(F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5407121 387959 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 444 3 0 4 6.9 O=C(c1ccc(/N=N\c2ccc(F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
172442489 388486 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 426 3 0 4 6.8 O=C(c1ccc(/N=N/c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5417656 388486 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 426 3 0 4 6.8 O=C(c1ccc(/N=N/c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
135916070 450839 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL601931 450839 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
135916070 450839 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/jm901084f
CHEMBL601931 450839 0 None -1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 418 2 1 6 4.5 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)c(Cl)c2)n1 10.1021/jm901084f
2202 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
9895468 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
CHEMBL582857 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
DB12643 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2011.03.012
9981665 232117 5 None -77 6 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
CHEMBL341339 232117 5 None -77 6 Rat 4.5 pKi = 4.5 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
46890615 21003 0 None -128 2 Human 6.5 pKi = 6.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1083444 21003 0 None -128 2 Human 6.5 pKi = 6.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 411 3 0 2 6.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(Cl)cc1C 10.1016/j.bmcl.2010.04.068
44297517 311660 0 None -20 3 Rat 8.5 pKi = 8.5 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1343 39 15 16 -1.4 CN(C(=O)CCCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL405440 311660 0 None -20 3 Rat 8.5 pKi = 8.5 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1343 39 15 16 -1.4 CN(C(=O)CCCc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
151171 2408 36 None -5 5 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
2203 2408 36 None -5 5 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
732 2408 36 None -5 5 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
CHEMBL1755 2408 36 None -5 5 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
DB00872 2408 36 None -5 5 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
ChEMBL 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 10.1021/acs.jmedchem.8b00697
44316241 197234 0 None -77 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44419029 197234 0 None -77 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL265859 197234 0 None -77 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL268306 197234 0 None -77 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 18 13 14 -2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
16109448 278813 0 None -5 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 14 15 -3.7 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL385068 278813 0 None -5 4 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 14 15 -3.7 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44325579 221415 0 None 33 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 535 4 2 5 5.9 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(O)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL328791 221415 0 None 33 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 535 4 2 5 5.9 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(O)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
10414302 222004 0 None 50 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL329903 222004 0 None 50 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44294573 317597 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL416114 317597 0 None 3 2 Human 8.5 pKi = 8.5 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
11366713 274628 0 None -7 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 13 15 -3.9 NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL375096 274628 0 None -7 8 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1054 19 13 15 -3.9 NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
44520861 354687 0 None 12 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL475684 354687 0 None 12 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 548 5 1 6 5.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccnn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL2370646 477669 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 1093 17 10 13 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351441 197204 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL265591 197204 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44325691 27259 0 None 239 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL1189693 27259 0 None 239 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 1 4 6.8 O=C(Nc1ccc(C(=O)N2C[C@H]3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325766 222039 0 None 109 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL330005 222039 0 None 109 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1ccc(F)cc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325695 332751 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL432043 332751 0 None 1230 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1cccc(-c2ccccc2C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c1 10.1016/j.bmcl.2004.03.083
44325332 474287 0 None None None Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL93861 474287 0 None None None Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 503 4 1 4 5.5 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
16109442 274800 0 None -6 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 20 14 15 -3.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL375325 274800 0 None -6 4 Rat 8.4 pKi = 8.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1068 20 14 15 -3.3 N=C(N)NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
163408867 375393 6 None None None Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 7 2 5 5.5 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCC(=O)N3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5207224 375393 6 None None None Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 7 2 5 5.5 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCC(=O)N3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
122322 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00162a001
2217 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00162a001
44294542 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00162a001
44382370 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00162a001
CHEMBL262423 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00162a001
CHEMBL384776 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00162a001
122322 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
2217 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
44294542 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
44382370 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
CHEMBL262423 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
CHEMBL384776 2781 0 None -8 4 Pig 8.4 pKi = 8.4 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 10.1021/jm00150a003
46890612 21233 0 None -81 2 Human 7.5 pKi = 7.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 5.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(NC(C)=O)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1084325 21233 0 None -81 2 Human 7.5 pKi = 7.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 420 4 1 3 5.4 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(NC(C)=O)c1 10.1016/j.bmcl.2010.04.068
11757222 217626 0 None None None Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL319418 217626 0 None None None Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
44294592 197085 0 None None None Pig 7.5 pKi = 7.5 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL264540 197085 0 None None None Pig 7.5 pKi = 7.5 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
56679085 125920 0 None None None Rat 4.5 pKi = 4.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 724 6 2 8 2.7 CC[C@@H](C)[C@@H]1NC[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790550 125920 0 None None None Rat 4.5 pKi = 4.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 724 6 2 8 2.7 CC[C@@H](C)[C@@H]1NC[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
167184706 373086 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 9 2 5 6.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5171014 373086 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 588 9 2 5 6.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
167184778 373148 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 10 2 4 7.0 CCN(CC)CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21 10.1021/acs.jmedchem.2c00011
CHEMBL5172177 373148 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 10 2 4 7.0 CCN(CC)CCCNC1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3C)cc2C)c2ccc(Cl)cc21 10.1021/acs.jmedchem.2c00011
53349471 237401 0 None -22 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416774 237401 0 None -22 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL1790552 484810 0 None -1 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 770 6 2 8 2.0 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCN(C)N2C(=O)[C@H]2CCCN(C)N2C1=O 10.1021/jm00171a003
54582318 123946 0 None -8317 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1210 29 12 15 1.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765668 123946 0 None -8317 4 Human 4.5 pKi = 4.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1210 29 12 15 1.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
11465834 275790 0 None -263 4 Human 6.5 pKi = 6.5 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm060073e
CHEMBL377414 275790 0 None -263 4 Human 6.5 pKi = 6.5 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm060073e
146681949 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
2168 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
2810 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
644077 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
CHEMBL373742 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
DB00067 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
P01185 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
P01186 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
P35455 8624 35 None -5 8 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting methodDisplacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
ChEMBL 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10.1016/j.bmc.2018.03.019
44335345 19510 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL105961 19510 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 505 3 1 3 6.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
177382705 391829 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1137 34 15 13 -2.2 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5575489 391829 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1137 34 15 13 -2.2 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL2372927 485915 0 None -199 2 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 766 6 4 7 2.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCCCN2C(=O)[C@@H]2CCCCN2C1=O 10.1021/jm00169a001
2202 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
9895468 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
CHEMBL582857 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
DB12643 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptorDisplacement of [3H]AVP from human vasopressin V2 receptor
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2010.12.081
2202 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
9895468 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
CHEMBL582857 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
DB12643 5638 34 None -489 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counterDisplacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
ChEMBL 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 10.1016/j.bmcl.2009.09.050
151426084 465521 0 None -154 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 449 2 1 6 3.1 NC(=O)C1Cc2cc(Cl)ccc2-n2c(nnc2N2CCC3(CC2)OCc2ccccc23)C1 10.1016/j.ejmech.2024.117069
CHEMBL6082986 465521 0 None -154 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 449 2 1 6 3.1 NC(=O)C1Cc2cc(Cl)ccc2-n2c(nnc2N2CCC3(CC2)OCc2ccccc23)C1 10.1016/j.ejmech.2024.117069
44520867 355863 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 456 3 1 4 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478082 355863 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 456 3 1 4 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(N)=O)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
44314134 214501 0 None -331 2 Rat 7.5 pKi = 7.5 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 576 5 1 5 5.5 Cc1occc1C(=O)Nc1ccc(C(=O)N2CCC(F)(F)/C(=C/C(=O)N3CCC(N(C)C)CC3)c3ccccc32)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL310921 214501 0 None -331 2 Rat 7.5 pKi = 7.5 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 576 5 1 5 5.5 Cc1occc1C(=O)Nc1ccc(C(=O)N2CCC(F)(F)/C(=C/C(=O)N3CCC(N(C)C)CC3)c3ccccc32)cc1 10.1016/s0960-894x(01)00723-5
2213 1072 37 None -87 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1016/j.bmcl.2007.11.008
3008 1072 37 None -87 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1016/j.bmcl.2007.11.008
5311010 1072 37 None -87 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1016/j.bmcl.2007.11.008
68613 1072 37 None -87 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1016/j.bmcl.2007.11.008
CHEMBL378642 1072 37 None -87 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1016/j.bmcl.2007.11.008
CHEMBL382301 1072 37 None -87 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1016/j.bmcl.2007.11.008
DB09059 1072 37 None -87 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 10.1016/j.bmcl.2007.11.008
CHEMBL52813 489209 0 None -23 2 Rat 4.5 pKi = 4.5 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 712 6 2 6 2.3 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCN2C1=O 10.1021/jm00169a001
145966126 329096 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 3 0 4 4.9 Cc1ccn(-c2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4210158 329096 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 3 0 4 4.9 Cc1ccn(-c2ccc(C(=O)N3CCCC(N(C)C)c4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
145964296 329079 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 2 0 3 4.1 O=C(c1ccc(-c2ncccn2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4209952 329079 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 2 0 3 4.1 O=C(c1ccc(-c2ncccn2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
46890439 20917 1 None -51 2 Human 5.5 pKi = 5.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083095 20917 1 None -51 2 Human 5.5 pKi = 5.5 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 347 2 0 1 5.7 Cc1ccccc1-c1ccc(C(=O)N2C[C@@]3(C)C[C@@H]2CC(C)(C)C3)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1790549 484808 0 None -18 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 758 6 4 9 1.4 CC[C@@H](C)[C@H]1C(=O)N2NCCC[C@@H]2C(=O)N2NCCC[C@H]2C(=O)N(C)[C@H](Cc2ccccc2)C(=O)N2CCC[C@H]2C(=O)N[C@H](Cc2ccccc2)C(=O)N1O 10.1021/jm00171a003
45103785 429849 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 584 4 1 5 4.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
CHEMBL590175 429849 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 584 4 1 5 4.6 Cc1cc(C(=O)N2Cc3cccn3Cc3ccccc32)ccc1CNC(=O)N1CCC[C@H]1C(=S)N1CCCN(C)CC1 10.1021/jm901084f
168281863 374113 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 608 8 1 5 6.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5187046 374113 0 None None None Human 7.5 pKi = 7.5 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 608 8 1 5 6.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccc(Cl)cc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
2042 8014 41 None -1905 6 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm010526+
2176 8014 41 None -1905 6 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm010526+
439302 8014 41 None -1905 6 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm010526+
CHEMBL395429 8014 41 None -1905 6 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm010526+
44361522 240294 0 None -6165 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 477 4 0 5 3.8 CC(=O)N1CCC(Oc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)CC1 10.1021/jm00023a002
CHEMBL358793 240294 0 None -6165 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from ratsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
ChEMBL 477 4 0 5 3.8 CC(=O)N1CCC(Oc2ccc(C(=O)N3CCC(N4C(=O)OCc5ccccc54)CC3)cc2)CC1 10.1021/jm00023a002
44361406 78503 0 None -1122 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.
ChEMBL 451 7 1 5 3.4 CC(=O)NCCCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
CHEMBL143304 78503 0 None -1122 5 Rat 4.5 pKi = 4.5 Binding
Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.
ChEMBL 451 7 1 5 3.4 CC(=O)NCCCOc1ccc(C(=O)N2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm00023a002
172452353 388431 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1cccc(/N=N/c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5416738 388431 0 None None None Human 6.5 pKi = 6.5 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1cccc(/N=N/c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/acs.jmedchem.2c01625
46890184 20865 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 453 3 0 3 7.3 COc1cc(-c2csc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1082835 20865 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 453 3 0 3 7.3 COc1cc(-c2csc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL2369841 477601 0 None -10 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1026 17 13 15 -4.6 NC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
118734334 237395 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416767 237395 0 None -10 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
178294922 465815 0 None -2570 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 438 4 1 7 2.6 NC(=O)C1Cc2cc(Cl)ccc2-n2c(nnc2N2CCC(Oc3ccccn3)CC2)C1 10.1016/j.ejmech.2024.117069
CHEMBL6102091 465815 0 None -2570 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 438 4 1 7 2.6 NC(=O)C1Cc2cc(Cl)ccc2-n2c(nnc2N2CCC(Oc3ccccn3)CC2)C1 10.1016/j.ejmech.2024.117069
10187283 473198 0 None -120 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
CHEMBL86577 473198 0 None -120 4 Rat 6.4 pKi = 6.4 Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidneyBinding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
44325905 329225 0 None 275 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL421180 329225 0 None 275 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 571 4 1 4 7.0 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1)c1cc(F)ccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44294507 196832 0 None None None Pig 7.4 pKi = 7.4 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL262499 196832 0 None None None Pig 7.4 pKi = 7.4 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL54443 489222 0 None -70 2 Rat 6.4 pKi = 6.4 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 756 6 6 8 0.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]2CCCN2C(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCCCN2C(=O)[C@@H]2CCNCN2C1=O 10.1021/jm00169a001
57520031 155346 0 None -131 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 555 7 0 6 3.0 COc1cc(OC2CCN(S(C)(=O)=O)CC2)ccc1CC(=O)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017979 155346 0 None -131 3 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 555 7 0 6 3.0 COc1cc(OC2CCN(S(C)(=O)=O)CC2)ccc1CC(=O)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmc.2012.02.019
2252 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity towards human kidney Vasopressin V2 receptor by using functional assayBinding affinity towards human kidney Vasopressin V2 receptor by using functional assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1016/s0960-894x(99)00181-x
6918320 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity towards human kidney Vasopressin V2 receptor by using functional assayBinding affinity towards human kidney Vasopressin V2 receptor by using functional assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1016/s0960-894x(99)00181-x
CHEMBL24781 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity towards human kidney Vasopressin V2 receptor by using functional assayBinding affinity towards human kidney Vasopressin V2 receptor by using functional assay
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1016/s0960-894x(99)00181-x
2252 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donorsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm00023a002
6918320 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donorsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm00023a002
CHEMBL24781 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donorsBinding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm00023a002
2252 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901812z
6918320 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901812z
CHEMBL24781 4546 39 None -10000 5 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 507 5 0 6 3.8 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)C(=O)C 10.1021/jm901812z
145976595 328683 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
CHEMBL4205046 328683 0 None 6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 408 2 1 4 4.9 Cc1ccn(C(=O)Nc2ccc(C(=O)N3CCCCc4ccccc43)c(Cl)c2)n1 10.1021/acs.jmedchem.8b00697
2204 8913 7 None -1258 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranesDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes
ChEMBL 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 10.1021/acs.jmedchem.8b00697
9917025 8913 7 None -1258 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranesDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes
ChEMBL 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 10.1021/acs.jmedchem.8b00697
CHEMBL3307200 8913 7 None -1258 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranesDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes
ChEMBL 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 10.1021/acs.jmedchem.8b00697
177382713 391555 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1305 46 15 13 2.4 CCCCCCCCCCCCCCC(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C 10.1021/acs.jmedchem.4c00217
CHEMBL5570833 391555 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1305 46 15 13 2.4 CCCCCCCCCCCCCCC(=O)N[C@H](Cc1ccc(OCC)cc1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C 10.1021/acs.jmedchem.4c00217
168282087 373837 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 602 10 2 5 6.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5182998 373837 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 602 10 2 5 6.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCCCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
46890215 21475 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 447 3 0 2 7.2 COc1cc(-c2cccc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
CHEMBL1085378 21475 0 None 3 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 447 3 0 2 7.2 COc1cc(-c2cccc3ccccc23)c(Cl)cc1C(=O)N1C[C@]2(C)C[C@H]1CC(C)(C)C2 10.1016/j.bmcl.2010.04.068
11465834 275790 0 None -263 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm201287w
CHEMBL377414 275790 0 None -263 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 483 6 1 3 3.3 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N(C)C)c1ccc(F)cc1F 10.1021/jm201287w
3537 8682 25 None 3 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to V2 receptor (unknown origin)Binding affinity to V2 receptor (unknown origin)
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
5311500 8682 25 None 3 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to V2 receptor (unknown origin)Binding affinity to V2 receptor (unknown origin)
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL363910 8682 25 None 3 3 Human 7.4 pKi = 7.4 Binding
Binding affinity to V2 receptor (unknown origin)Binding affinity to V2 receptor (unknown origin)
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL1790547 484806 0 None -57 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 736 6 2 8 2.0 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2C=CC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790543 484805 0 None -61 2 Rat 5.4 pKi = 5.4 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 756 6 4 8 0.8 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC(=O)NN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
177382702 391767 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1105 33 15 13 -2.3 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)c2ccccc2)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5574509 391767 0 None None None Human 5.4 pKi = 5.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1105 33 15 13 -2.3 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)c2ccccc2)cc1 10.1021/acs.jmedchem.4c00217
11634973 157006 17 None -31622 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 518 6 1 5 2.8 CC[C@H](C)[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N1CCOCC1)c1ccc(C)nc1C 10.1021/jm201287w
CHEMBL2037511 157006 17 None -31622 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 518 6 1 5 2.8 CC[C@H](C)[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N1CCOCC1)c1ccc(C)nc1C 10.1021/jm201287w
DB11934 157006 17 None -31622 2 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 518 6 1 5 2.8 CC[C@H](C)[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)N1CCOCC1)c1ccc(C)nc1C 10.1021/jm201287w
71462479 163808 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172295 163808 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1357 31 4 17 9.0 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7-c7ccccc7)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
178295806 466512 0 None -19 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.1 Clc1ccc2c(c1)CC1(Cc3nnc(C4CCN(c5cccc6c5OCC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6147507 466512 0 None -19 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 478 2 0 7 4.1 Clc1ccc2c(c1)CC1(Cc3nnc(C4CCN(c5cccc6c5OCC6)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL2370640 477667 0 None 1 2 Human 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 1150 19 11 14 -0.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44325363 216275 0 None 281 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
CHEMBL314290 216275 0 None 281 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 567 5 1 5 6.1 COc1ccc(C(=O)Nc2ccc(C(=O)N3C[C@H]4COCCN4Cc4ccccc43)c(Cl)c2)c(-c2ccccc2)c1 10.1016/j.bmcl.2004.03.083
44325538 222041 0 None 616 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
CHEMBL330016 222041 0 None 616 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccc(O)cc1 10.1016/j.bmcl.2004.03.083
168294659 375432 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5207885 375432 0 None None None Human 8.4 pKi = 8.4 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 574 8 1 5 6.2 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL2370646 477669 0 None -1 2 Pig 8.4 pKi = 8.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1093 17 10 13 0.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL408474 488015 0 None None None Pig 8.3 pKi = 8.3 Binding
Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
ChEMBL 1056 19 13 16 -3.7 NCCCC[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](N)C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(=O)O 10.1021/jm00150a003
138688092 466322 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 438 2 0 8 2.5 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5ccccn5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6142653 466322 0 None -7 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 438 2 0 8 2.5 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5ccccn5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
73348509 180260 0 None 1 2 Pig 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL2370642 180260 0 None 1 2 Pig 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
9959174 386967 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL528996 386967 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
9959174 386967 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL528996 386967 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
73348509 180260 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL2370642 180260 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 979 13 8 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
15416417 308834 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4104877 308834 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
44382498 196831 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
CHEMBL262482 196831 0 None None None Human 8.3 pKi = 8.3 Binding
Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
ChEMBL 1093 17 10 13 0.6 CCOc1ccc(C[C@@H]2NC(=O)CC3(CCC(C)CC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00124a025
46890288 21745 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 528 3 0 2 8.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1086574 21745 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 528 3 0 2 8.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
155753110 392355 5 None -131 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as dissociation constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as dissociation constant by Cheng-Prusoff equation analysis
ChEMBL 452 3 0 7 4.3 Clc1ccc2c(c1)CC1(Cc3nnc([C@H]4CC[C@H](Oc5ccccn5)CC4)n3-2)OCCO1 10.1021/acs.jmedchem.3c01868
CHEMBL5594994 392355 5 None -131 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]AVP from human Vasopressin V2 receptor assessed as dissociation constant by Cheng-Prusoff equation analysisDisplacement of [3H]AVP from human Vasopressin V2 receptor assessed as dissociation constant by Cheng-Prusoff equation analysis
ChEMBL 452 3 0 7 4.3 Clc1ccc2c(c1)CC1(Cc3nnc([C@H]4CC[C@H](Oc5ccccn5)CC4)n3-2)OCCO1 10.1021/acs.jmedchem.3c01868
155753110 392355 5 None -131 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 452 3 0 7 4.3 Clc1ccc2c(c1)CC1(Cc3nnc([C@H]4CC[C@H](Oc5ccccn5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL5594994 392355 5 None -131 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 452 3 0 7 4.3 Clc1ccc2c(c1)CC1(Cc3nnc([C@H]4CC[C@H](Oc5ccccn5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
167312309 388853 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c01625
CHEMBL5425852 388853 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c01625
CHEMBL5427331 388853 0 None None None Human 7.4 pKi = 7.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)cc1 10.1021/acs.jmedchem.2c01625
44314382 203044 0 None -14 2 Rat 7.4 pKi = 7.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 9 1 6 7.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL306718 203044 0 None -14 2 Rat 7.4 pKi = 7.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 648 9 1 6 7.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCc2ccc(C(=O)N3CCC(N4CCCCC4)CC3)cc2)c1 10.1016/s0960-894x(01)00723-5
44351409 196955 0 None None None Pig 7.4 pKi = 7.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1050 18 8 12 3.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL263432 196955 0 None None None Pig 7.4 pKi = 7.4 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 1050 18 8 12 3.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
46890290 21326 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 544 3 0 2 9.4 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1084717 21326 0 None -58 2 Human 6.4 pKi = 6.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 544 3 0 2 9.4 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
16109445 274649 0 None -1659 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1011 17 11 14 -1.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL375188 274649 0 None -1659 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1011 17 11 14 -1.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
46890289 21746 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 558 4 0 3 8.9 COc1cc(-c2cccc3cccnc23)c(Cl)cc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086575 21746 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 558 4 0 3 8.9 COc1cc(-c2cccc3cccnc23)c(Cl)cc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
172441826 387840 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccccc1/N=N/c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5404703 387840 0 None None None Human 6.4 pKi = 6.4 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccccc1/N=N/c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL2369848 477605 0 None -912 4 Human 5.4 pKi = 5.4 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1093 18 12 15 -2.3 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2cccs2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
11016093 332791 0 None -2089 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 466 9 1 5 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCC1CCNCC1 10.1021/jm010544r
CHEMBL432375 332791 0 None -2089 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 466 9 1 5 6.5 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCC1CCNCC1 10.1021/jm010544r
44313913 469720 0 None -58 2 Rat 6.4 pKi = 6.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 670 10 1 7 6.2 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCc2ccc(C(=O)N3CCN(C)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL75489 469720 0 None -58 2 Rat 6.4 pKi = 6.4 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 670 10 1 7 6.2 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCc2ccc(C(=O)N3CCN(C)CC3)cc2)cc1 10.1016/s0960-894x(01)00723-5
16109438 196913 0 None -147 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1051 17 11 14 -1.0 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL263090 196913 0 None -147 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1051 17 11 14 -1.0 NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
16109444 316992 0 None -562 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1037 16 11 14 -1.3 NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL412742 316992 0 None -562 4 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1037 16 11 14 -1.3 NCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL297725 486403 0 None -31 2 Rat 5.4 pKi = 5.4 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 726 6 3 6 2.7 CC[C@H](C)[C@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
54584268 123948 0 None -5370 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1226 29 13 16 0.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765671 123948 0 None -5370 4 Human 4.4 pKi = 4.4 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1226 29 13 16 0.7 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)C(O)CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCCCCCCCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
137652605 314697 0 None -22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4094707 314697 0 None -22 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3c(C)cccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL2371439 477686 0 None None None Pig 7.3 pKi = 7.3 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL 1092 18 11 13 -1.1 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CC(C2CCCC2)SSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
26434734 328489 8 None -5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 294 2 0 2 3.7 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL4202525 328489 8 None -5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 294 2 0 2 3.7 CN(C)c1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL5070261 478440 0 None -1548 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 410 3 1 6 3.9 OC1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
53349364 331503 0 None -8 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
CHEMBL4282161 331503 0 None -8 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
46890485 21358 0 None -7943 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1084823 21358 0 None -7943 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 361 2 0 1 6.0 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)cc1C 10.1016/j.bmcl.2010.04.068
CHEMBL300103 486408 0 None -81 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 741 6 3 7 1.8 CC[C@H](C)[C@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCCN2C(=O)[C@H]2CCNCN2C1=O 10.1021/jm00169a001
10278394 473170 0 None -1202 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 495 10 0 6 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL86384 473170 0 None -1202 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 495 10 0 6 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCN1CCN(C)CC1 10.1021/jm010544r
44351337 336247 0 None None None Pig 6.3 pKi = 6.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 840 10 7 10 2.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL446683 336247 0 None None None Pig 6.3 pKi = 6.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 840 10 7 10 2.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
54584266 123943 0 None -7585 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1145 20 12 15 0.2 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)c2ccccc2N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765664 123943 0 None -7585 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1145 20 12 15 0.2 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)c2ccccc2N)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
5311065 484177 30 None -7 8 Human 8.3 pKi = 8.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
817 484177 30 None -7 8 Human 8.3 pKi = 8.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
CHEMBL1429 484177 30 None -7 8 Human 8.3 pKi = 8.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
DB00035 484177 30 None -7 8 Human 8.3 pKi = 8.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm030611c
9849525 220928 0 None 61 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL327365 220928 0 None 61 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 519 4 1 4 6.2 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
44325558 222049 0 None 1096 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330094 222049 0 None 1096 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 553 4 2 5 5.8 O=C(Nc1ccc(C(=O)N2C[C@H]3COCCN3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1cccc(O)c1 10.1016/j.bmcl.2004.03.083
178296207 466188 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 477 2 0 7 3.8 Clc1ccc2c(c1)CC1(CCCO1)Cc1nnc(N3CCN(c4cccc5c4OCC5)CC3)n1-2 10.1016/j.ejmech.2024.117069
CHEMBL6132657 466188 0 None -3 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 477 2 0 7 3.8 Clc1ccc2c(c1)CC1(CCCO1)Cc1nnc(N3CCN(c4cccc5c4OCC5)CC3)n1-2 10.1016/j.ejmech.2024.117069
44317966 311591 0 None None None Pig 8.3 pKi = 8.3 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1124 21 11 14 -0.7 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL404820 311591 0 None None None Pig 8.3 pKi = 8.3 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1124 21 11 14 -0.7 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
44520855 353265 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 561 5 1 5 5.9 Cc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
CHEMBL473872 353265 0 None 5 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 561 5 1 5 5.9 Cc1cccc(CNC(=O)/C=C2/c3ccccc3N(C(=O)c3ccc(-n4ccc(C)n4)cc3Cl)CCC2(F)F)n1 10.1016/j.bmc.2009.03.001
CHEMBL2370640 477667 0 None -1 2 Pig 8.3 pKi = 8.3 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1150 19 11 14 -0.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
71457081 163802 0 None 31 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482251 163802 0 None 31 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172289 163802 0 None 31 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1309 24 5 14 10.2 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44294573 317597 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL416114 317597 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44294573 317597 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL416114 317597 0 None -3 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 953 16 9 12 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL2369839 477599 0 None -33 4 Human 7.3 pKi = 7.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1054 18 13 15 -4.7 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
3537 8682 25 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
5311500 8682 25 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
CHEMBL363910 8682 25 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/acs.jmedchem.8b00697
3537 8682 25 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
5311500 8682 25 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
CHEMBL363910 8682 25 None 3 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 10.1021/jm901084f
44243143 40903 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 372 5 0 6 4.3 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cn1 10.1021/jm901812z
CHEMBL1254297 40903 0 None -8 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 372 5 0 6 4.3 COc1ccc(-n2c(C)nnc2-c2ccc(-c3ccccc3OC)cc2)cn1 10.1021/jm901812z
CHEMBL2372928 485916 0 None -10 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 782 9 5 7 2.4 CC[C@@H](C)[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCN)NC(=O)[C@H]2CCCCN2C1=O 10.1021/jm00169a001
11488952 159212 0 None -2511 3 Human 5.3 pKi = 5.3 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 501 7 2 4 4.2 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc2occc2c1 10.1021/jm060073e
CHEMBL208787 159212 0 None -2511 3 Human 5.3 pKi = 5.3 Binding
Displacement of vasopressin from human V2RDisplacement of vasopressin from human V2R
ChEMBL 501 7 2 4 4.2 CC(C)C[C@@H]1C(=O)N[C@H](C2Cc3ccccc3C2)C(=O)N1[C@@H](C(=O)NC(C)C)c1ccc2occc2c1 10.1021/jm060073e
5306925 329034 10 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 285 1 0 1 4.3 O=C(c1ccc(Cl)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4209421 329034 10 None 1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 285 1 0 1 4.3 O=C(c1ccc(Cl)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
16109441 274798 0 None -114 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1026 19 12 15 -2.8 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL375323 274798 0 None -114 4 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1026 19 12 15 -2.8 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
177382711 391712 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1213 35 15 13 -1.1 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5573307 391712 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1213 35 15 13 -1.1 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
168288721 374458 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 532 8 1 4 6.4 CN(C)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
CHEMBL5192496 374458 0 None None None Human 7.3 pKi = 7.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 532 8 1 4 6.4 CN(C)CCCN1CCCN(C(=O)c2ccc(NC(=O)c3ccccc3-c3ccccc3)cc2)c2ccccc21 10.1021/acs.jmedchem.2c00567
145970757 329707 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 307 4 0 1 5.0 CCCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
CHEMBL4218211 329707 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 307 4 0 1 5.0 CCCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
44335343 217096 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
CHEMBL318392 217096 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 519 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(CC4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1Cl 10.1016/s0960-894x(02)00649-2
54581307 123944 0 None -4073 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1097 21 12 15 -1.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765666 123944 0 None -4073 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1097 21 12 15 -1.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCNC(=O)CCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
172464381 389286 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 494 3 0 4 7.8 O=C(c1ccc(/N=N\c2ccc(C(F)(F)F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5435956 389286 0 None None None Human 5.3 pKi = 5.3 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 494 3 0 4 7.8 O=C(c1ccc(/N=N\c2ccc(C(F)(F)F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
44520869 370191 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 527 6 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCN(C)C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL490049 370191 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 527 6 1 5 4.6 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCN(C)C)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
46890440 21671 0 None -173 2 Human 7.3 pKi = 7.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086272 21671 0 None -173 2 Human 7.3 pKi = 7.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 381 2 0 1 6.4 Cc1ccccc1-c1ccc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)c(Cl)c1 10.1016/j.bmcl.2010.04.068
137642420 313941 0 None -11 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4086079 313941 0 None -11 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 414 3 2 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@H](O)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.7b00422
71451752 163806 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7C)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172293 163806 0 None 9 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1295 30 4 17 7.6 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCOCCOCCOCCn4cc(CNC(=O)CCC(=O)NC5CCCN(C(=O)c6ccc(NC(=O)c7ccccc7C)cc6)c6ccccc65)nn4)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL1790546 484183 0 None -85 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 738 6 2 8 2.3 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
2241 4522 5 None -208 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00169a001
9810632 4522 5 None -208 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00169a001
CHEMBL127686 4522 5 None -208 4 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00169a001
168280173 373862 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5183482 373862 0 None None None Human 6.3 pKi = 6.3 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(F)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL1790551 484809 0 None -229 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 795 8 2 9 2.1 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2C[C@@H](CN(C)C)C=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL292579 486388 0 None -32 2 Rat 6.3 pKi = 6.3 Binding
Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptorInhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
ChEMBL 744 9 5 8 0.7 CC[C@@H](C)[C@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@H](CCCN)NC(=O)[C@H]2CCNCN2C1=O 10.1021/jm00169a001
44316236 470360 0 None -23 4 Human 6.3 pKi = 6.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 997 16 12 14 -4.0 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H]1CCCN1C(=O)[C@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
CHEMBL80877 470360 0 None -23 4 Human 6.3 pKi = 6.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 997 16 12 14 -4.0 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H]1CCCN1C(=O)[C@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccccc2)C(=O)NCC(=O)N[C@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890654 21453 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(C)cc1 10.1016/j.bmcl.2010.04.068
CHEMBL1085299 21453 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccc(C)cc1 10.1016/j.bmcl.2010.04.068
162676461 366849 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
CHEMBL4799793 366849 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
162676461 366849 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assayDisplacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
CHEMBL4799793 366849 0 None -707 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assayDisplacement of [3H]AVP from human V2a receptor expressed in 1132N1 cells assessed as dissociation constant by radioligand binding assay
ChEMBL 394 3 0 5 4.9 Clc1ccc2c(c1)CCCc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1016/j.bmcl.2020.127417
9981665 232117 5 None -15 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
CHEMBL341339 232117 5 None -15 6 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 459 5 2 4 3.4 CC1(C)[C@@H]2CC[C@@]1(CS(=O)(=O)N1CCC3(C=Cc4ccccc43)CC1)[C@@](O)(CC(=O)O)C2 10.1021/jm901812z
CHEMBL2369834 477594 0 None -43 4 Human 6.3 pKi = 6.3 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1040 18 13 15 -4.3 NCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm030611c
172452804 388444 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 458 3 0 4 7.2 Cc1ccc(F)cc1/N=N/c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5416967 388444 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 458 3 0 4 7.2 Cc1ccc(F)cc1/N=N/c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL1790547 484806 0 None -57 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 736 6 2 8 2.0 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2C=CC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
57519947 155340 0 None -100 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C\I)c2)CC1 10.1016/j.bmc.2012.02.019
CHEMBL2017868 155340 0 None -100 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation countingDisplacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
ChEMBL 707 9 0 6 4.3 CS(=O)(=O)N1CCC(Oc2ccc(CC(=O)N3CCC(N4C(=O)CCc5ccccc54)CC3)c(OC/C=C\I)c2)CC1 10.1016/j.bmc.2012.02.019
10187283 473198 0 None -194 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
CHEMBL86577 473198 0 None -194 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 543 7 0 6 5.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCc1ccc(C(=O)N2CCN(C)CC2)cc1 10.1021/jm010544r
172464381 388910 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 494 3 0 4 7.8 O=C(c1ccc(/N=N/c2ccc(C(F)(F)F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5427253 388910 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 494 3 0 4 7.8 O=C(c1ccc(/N=N/c2ccc(C(F)(F)F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
2249 4540 14 None -162 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
9872389 4540 14 None -162 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
CHEMBL1253853 4540 14 None -162 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to human V2 receptorBinding affinity to human V2 receptor
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1016/j.bmcl.2012.10.116
2249 4540 14 None -162 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
9872389 4540 14 None -162 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
CHEMBL1253853 4540 14 None -162 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
ChEMBL 554 9 2 7 1.5 O=C([C@H](CCS(=O)(=O)C)N)N[C@H]1C[C@@H]2C([C@]1(CC2)CS(=O)(=O)N1CCN(CC1)c1ccccc1C)(C)C 10.1021/jm901812z
44520877 26879 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccnn1-c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
CHEMBL1186990 26879 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 547 5 1 5 5.6 Cc1ccnn1-c1ccc(C(=O)N2CCC(F)(F)/C(=C\C(=O)NCc3ccccn3)c3ccccc32)c(Cl)c1 10.1016/j.bmc.2008.09.039
44351441 197204 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL265591 197204 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1050 16 9 12 1.5 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCN=C(N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
171391764 391803 3 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1255 35 15 13 -0.1 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5575063 391803 3 None 31 2 Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1255 35 15 13 -0.1 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C(C)(C)C)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
44294575 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
44335358 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
44375638 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL216606 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL406184 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL438014 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
135916059 451719 0 None 5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 513 4 2 5 6.6 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm901084f
CHEMBL602872 451719 0 None 5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 513 4 2 5 6.6 Cc1cc(C(=O)N2Cc3cnn(C)c3Nc3ccccc32)ccc1NC(=O)c1ccccc1-c1ccccc1 10.1021/jm901084f
44294575 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44335358 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44375638 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL216606 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL406184 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL438014 163541 0 None -8 2 Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1136 19 11 14 -0.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
178298564 465981 0 None -45 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 494 2 0 9 3.7 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5nccc6ccsc56)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6108956 465981 0 None -45 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 494 2 0 9 3.7 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCN(c5nccc6ccsc56)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
177382714 392295 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1267 35 15 13 -0.4 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5594237 392295 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1267 35 15 13 -0.4 CCOc1ccc(C[C@@H](NC(=O)Cc2ccc(C(F)(F)F)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
44351278 236132 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339532 236132 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44351278 236132 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL339532 236132 0 None -1 2 Pig 8.2 pKi = 8.2 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
ChEMBL 924 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44294532 311694 0 None None None Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL405818 311694 0 None None None Pig 8.2 pKi = 8.2 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 910 15 8 11 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
168268939 373017 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 7 2 5 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
CHEMBL5169868 373017 0 None None None Human 8.2 pKi = 8.2 Binding
Displacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assayDisplacement of conivaptan-red from SNAP-tagged V2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition constant measured after 2 hrs by HTRF assay
ChEMBL 560 7 2 5 5.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(NCCN3CCOCC3)c3cc(Cl)ccc32)c(C)c1 10.1021/acs.jmedchem.2c00011
44325915 222215 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
CHEMBL330494 222215 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 509 3 1 4 5.6 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccccc32)c(Cl)c1 10.1016/j.bmcl.2004.03.083
46890186 21573 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1085850 21573 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cccc4ccccc34)c(Cl)c2Cl)C1 10.1016/j.bmcl.2010.04.068
46890709 21166 0 None -6025 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 402 3 1 2 5.9 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1c[nH]c2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1084008 21166 0 None -6025 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 402 3 1 2 5.9 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1c[nH]c2ccccc12 10.1016/j.bmcl.2010.04.068
16109437 175275 0 None -316 4 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1065 18 11 14 -0.6 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL221485 175275 0 None -316 4 Rat 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1065 18 11 14 -0.6 NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
2042 8014 41 None -60 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
2176 8014 41 None -60 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
439302 8014 41 None -60 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
CHEMBL395429 8014 41 None -60 6 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
168281109 374215 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 512 7 1 5 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5188374 374215 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 512 7 1 5 4.8 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
54584476 125111 0 None -478 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 630 8 1 10 2.3 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cccnc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
CHEMBL1779400 125111 0 None -478 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 630 8 1 10 2.3 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cccnc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
177382700 391785 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1216 35 15 14 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5574765 391785 0 None None None Human 5.2 pKi = 5.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1216 35 15 14 -2.4 CCOc1ccc(C[C@@H](NC(=O)CC)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL2369842 477602 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1103 18 13 15 -2.7 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
46890052 21184 0 None -11 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1084111 21184 0 None -11 2 Human 7.2 pKi = 7.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 413 3 0 2 6.6 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ccccc12 10.1016/j.bmcl.2010.04.068
2239 2222 0 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]oxytocin from human V2 vasopressin receptorDisplacement of [3H]oxytocin from human V2 vasopressin receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm050557v
6918854 2222 0 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]oxytocin from human V2 vasopressin receptorDisplacement of [3H]oxytocin from human V2 vasopressin receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm050557v
CHEMBL196478 2222 0 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]oxytocin from human V2 vasopressin receptorDisplacement of [3H]oxytocin from human V2 vasopressin receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm050557v
2239 2222 0 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm901812z
6918854 2222 0 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm901812z
CHEMBL196478 2222 0 None -501 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptorDisplacement of [3H]vasopressin from human vasopressin V2 receptor
ChEMBL 497 7 2 3 3.7 CC(C[C@@H]1C(=O)N[C@@H](C(=O)N1[C@H](c1ccc(cc1F)F)C(=O)NC(C)C)C1Cc2c(C1)cccc2)C 10.1021/jm901812z
54585429 125115 0 None -112 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 661 9 1 12 1.7 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cnc(OC)nc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
CHEMBL1779404 125115 0 None -112 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
ChEMBL 661 9 1 12 1.7 COc1ccc(S(=O)(=O)N2C(=O)[C@@](c3cnc(OC)nc3OC)(N3C[C@H](O)C[C@H]3C(=O)N(C)C)c3cc(Cl)ccc32)c(OC)c1 10.1016/j.bmcl.2011.03.012
168277442 373598 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.2c00567
CHEMBL5179419 373598 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)c(Cl)c1 10.1021/acs.jmedchem.2c00567
168271930 373181 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 530 7 1 5 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
CHEMBL5172734 373181 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 530 7 1 5 5.0 Cc1ccc(F)cc1C(=O)Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1 10.1021/acs.jmedchem.2c00567
53349364 331503 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
CHEMBL4282161 331503 0 None -8 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 minsDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHO cell membranes after 60 mins
ChEMBL 427 3 1 3 4.6 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC(=O)N(C)c3cccc(C)c32)cc1 10.1039/C8MD00033F
168282729 374131 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1F 10.1021/acs.jmedchem.2c00567
CHEMBL5187312 374131 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 516 7 1 5 4.7 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1F 10.1021/acs.jmedchem.2c00567
44325896 474681 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL96255 474681 0 None 27 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 551 4 1 5 4.9 O=C(Nc1ccc(C(=O)N2CC3CS(=O)(=O)CCN3Cc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
168287130 374636 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 498 7 1 5 4.5 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5195053 374636 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 498 7 1 5 4.5 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccccc1 10.1021/acs.jmedchem.2c00567
172458738 388824 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N\c2cccc(-c3ccccc3)c2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5425257 388824 0 None None None Human 6.2 pKi = 6.2 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N\c2cccc(-c3ccccc3)c2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
10907482 473254 0 None -724 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 10 0 6 5.6 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCC(=O)N1CCN(C)CC1 10.1021/jm010544r
CHEMBL86936 473254 0 None -724 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 523 10 0 6 5.6 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCC(=O)N1CCN(C)CC1 10.1021/jm010544r
100915923 373729 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 558 8 1 4 6.9 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
CHEMBL5181341 373729 0 None None None Human 7.2 pKi = 7.2 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 558 8 1 4 6.9 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCCC3)c3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.2c00567
54584265 123942 0 None -12882 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1026 18 11 14 -0.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
CHEMBL1765663 123942 0 None -12882 4 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
ChEMBL 1026 18 11 14 -0.9 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm1016208
46890656 21457 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 403 3 0 3 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1coc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1085301 21457 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 403 3 0 3 6.1 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1coc2ccccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1790542 484804 0 None -346 2 Rat 5.2 pKi = 5.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 754 6 3 8 1.3 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC(=O)NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
44419027 317307 6 None 1 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 19 13 15 -4.4 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2cccnc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
CHEMBL414074 317307 6 None 1 3 Rat 7.2 pKi = 7.2 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1053 19 13 15 -4.4 N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2cccnc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O 10.1021/jm060928n
10206901 473329 0 None -501 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 494 11 0 5 7.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCCCC1 10.1021/jm010544r
CHEMBL87455 473329 0 None -501 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 494 11 0 5 7.3 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCCCC1 10.1021/jm010544r
11740743 38028 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
CHEMBL119793 38028 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 384 3 1 2 5.2 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/jm3006146
44294592 197085 0 None None None Pig 8.1 pKi = 8.1 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL264540 197085 0 None None None Pig 8.1 pKi = 8.1 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1007 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@@H]3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
44520859 336161 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 572 5 1 6 5.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(C#N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL446566 336161 0 None 2 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 572 5 1 6 5.5 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4cccc(C#N)n4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
10411308 462175 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
CHEMBL603708 462175 0 None 2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 446 4 1 2 6.6 O=C(Nc1ccc(C(=O)N2CCCCc3ccccc32)cc1)c1ccccc1-c1ccccc1 10.1021/jm3006146
10715974 26196 2 None -4 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL118271 26196 2 None -4 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCC(O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
71449932 163813 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1100 19 3 10 10.4 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2172391 163813 0 None None None Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1100 19 3 10 10.4 CCN(CC)c1ccc2c(-c3ccc(S(=O)(=O)NCCCCC(=O)NC4CCCN(C(=O)c5ccc(NC(=O)c6ccccc6-c6ccccc6)cc5)c5ccccc54)cc3S(=O)(=O)[O-])c3ccc(=[N+](CC)CC)cc-3oc2c1 10.1021/jm3006146
CHEMBL2370641 477668 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of human kidney
ChEMBL 1007 15 8 12 2.2 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)NCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
56665480 125919 0 None -91 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL1790544 125919 0 None -91 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 754 6 2 8 3.5 CC[C@@H](C)[C@@H]1/N=C(\S)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
CHEMBL2371441 485716 0 None None None Pig 5.2 pKi = 5.2 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL 959 17 11 11 -3.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
46890571 21677 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(C)c1 10.1016/j.bmcl.2010.04.068
CHEMBL1086293 21677 0 None -177 2 Human 6.2 pKi = 6.2 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc(C)c1 10.1016/j.bmcl.2010.04.068
47177176 329750 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 1 0 1 4.4 O=C(c1ccc(Br)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4218739 329750 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 329 1 0 1 4.4 O=C(c1ccc(Br)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
44314222 469645 0 None -8 2 Rat 7.1 pKi = 7.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 560 11 1 6 5.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCN(C)CC2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL74593 469645 0 None -8 2 Rat 7.1 pKi = 7.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 560 11 1 6 5.1 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCN(C)CC2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL1790546 484183 0 None -85 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 738 6 2 8 2.3 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC=NN2C(=O)[C@H]2CCC=NN2C1=O 10.1021/jm00171a003
11144861 216648 0 None -954 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 452 8 1 5 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCC1CCNCC1 10.1021/jm010544r
CHEMBL315232 216648 0 None -954 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 452 8 1 5 6.1 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCC1CCNCC1 10.1021/jm010544r
CHEMBL1790552 484810 0 None -1 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL 770 6 2 8 2.0 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCCN(C)N2C(=O)[C@H]2CCCN(C)N2C1=O 10.1021/jm00171a003
44419028 197233 21 None -630 8 Human 6.1 pKi = 6.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
CHEMBL265858 197233 21 None -630 8 Human 6.1 pKi = 6.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1093 18 12 14 -1.6 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CC2CCCCC2)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
44275525 387710 0 None -107151 4 Human 5.1 pKi = 5.1 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1525 36 12 20 1.8 CN(C)c1ccc2c(c1)Oc1cc(N(C)C)ccc1C21OC(=O)c2cc(C(=O)N(C(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccc(O)cc3)N(C)C(=O)CCc3ccc(O)cc3)[C@@H](CCCCN)C(N)=O)ccc21 10.1021/jm9804782
91931055 387710 0 None -107151 4 Human 5.1 pKi = 5.1 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1525 36 12 20 1.8 CN(C)c1ccc2c(c1)Oc1cc(N(C)C)ccc1C21OC(=O)c2cc(C(=O)N(C(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccc(O)cc3)N(C)C(=O)CCc3ccc(O)cc3)[C@@H](CCCCN)C(N)=O)ccc21 10.1021/jm9804782
CHEMBL540192 387710 0 None -107151 4 Human 5.1 pKi = 5.1 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1525 36 12 20 1.8 CN(C)c1ccc2c(c1)Oc1cc(N(C)C)ccc1C21OC(=O)c2cc(C(=O)N(C(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccc(O)cc3)N(C)C(=O)CCc3ccc(O)cc3)[C@@H](CCCCN)C(N)=O)ccc21 10.1021/jm9804782
16109447 164761 0 None -83 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1012 18 12 15 -3.2 NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
CHEMBL219272 164761 0 None -83 4 Rat 7.1 pKi = 7.1 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
ChEMBL 1012 18 12 15 -3.2 NCCC[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm060928n
46890100 21622 0 None -33 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ncccc12 10.1016/j.bmcl.2010.04.068
CHEMBL1086069 21622 0 None -33 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 414 3 0 3 6.0 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1cccc2ncccc12 10.1016/j.bmcl.2010.04.068
67839485 329150 0 None -33 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 327 2 0 1 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
CHEMBL4210854 329150 0 None -33 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 327 2 0 1 5.3 O=C(c1ccc(-c2ccccc2)cc1)N1CCCCc2ccccc21 10.1021/acs.jmedchem.8b00697
44520848 444355 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 534 5 2 5 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmc.2009.10.038
CHEMBL594953 444355 0 None 2 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 534 5 2 5 4.4 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(C(F)(F)F)c2)n1 10.1016/j.bmc.2009.10.038
CHEMBL1790543 484805 0 None -61 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 756 6 4 8 0.8 CC[C@@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](Cc2ccccc2)N(C)C(=O)[C@@H]2CCC(=O)NN2C(=O)[C@H]2CCCNN2C1=O 10.1021/jm00171a003
44314343 203102 0 None -134 2 Rat 6.1 pKi = 6.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 650 13 1 7 6.0 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCCCCCC(=O)N2CCN(C)CC2)cc1 10.1016/s0960-894x(01)00723-5
CHEMBL307269 203102 0 None -134 2 Rat 6.1 pKi = 6.1 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 650 13 1 7 6.0 CCc1nccn1-c1ccccc1C(=O)Nc1ccc(C(=O)N(C)c2ccc(C)cc2OCCCCCC(=O)N2CCN(C)CC2)cc1 10.1016/s0960-894x(01)00723-5
172451749 388816 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N\c2ccccc2-c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5425077 388816 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 502 4 0 4 8.4 O=C(c1ccc(/N=N\c2ccccc2-c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
44325804 474213 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
CHEMBL93366 474213 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 533 4 1 4 6.5 Cc1ccc2c(c1)N(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)CC1CSCCN1C2 10.1016/j.bmcl.2004.03.083
44297516 316841 0 None -33 3 Rat 8.1 pKi = 8.1 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
CHEMBL412192 316841 0 None -33 3 Rat 8.1 pKi = 8.1 Binding
Tested for inhibition constant at V2 receptor of rat kidney membraneTested for inhibition constant at V2 receptor of rat kidney membrane
ChEMBL 1315 37 15 16 -2.2 CN(C(=O)Cc1ccc(N=[N+]=[N-])cc1)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm00038a013
15416418 308794 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
CHEMBL4075127 308794 0 None -8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting methodDisplacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
ChEMBL 400 3 2 3 4.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[C@@H](O)c3ccccc32)cc1 10.1021/acs.jmedchem.7b00422
44351439 314882 0 None None None Pig 8.1 pKi = 8.1 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1022 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
CHEMBL409667 314882 0 None None None Pig 8.1 pKi = 8.1 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1022 16 8 12 2.6 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCCC3C(=O)NCCCCCN)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44317762 316865 0 None None None Pig 8.1 pKi = 8.1 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1067 19 10 13 0.2 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL412392 316865 0 None None None Pig 8.1 pKi = 8.1 Binding
Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
ChEMBL 1067 19 10 13 0.2 CCOc1ccc(C[C@H]2NC(=O)CC(CC)(CC)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCN=C(N)N)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00162a001
CHEMBL2369840 477600 0 None -10 4 Human 7.1 pKi = 7.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1126 18 13 14 -1.9 NC(=O)CNC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(N)=O)C(=O)N1 10.1021/jm030611c
177382712 392133 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1257 35 15 13 -0.0 CCOc1ccc(C[C@@H](NC(=O)CC23CC4CC(CC(C4)C2)C3)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
CHEMBL5591095 392133 0 None None None Human 7.1 pKi = 7.1 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition constant measured every 1 min for 1 hr by HTRF assay
ChEMBL 1257 35 15 13 -0.0 CCOc1ccc(C[C@@H](NC(=O)CC23CC4CC(CC(C4)C2)C3)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C(C)C)cc1 10.1021/acs.jmedchem.4c00217
10873853 216650 0 None -147 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 438 7 1 5 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCC1CCNCC1 10.1021/jm010544r
CHEMBL315251 216650 0 None -147 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 438 7 1 5 5.7 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCC1CCNCC1 10.1021/jm010544r
46890262 21015 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cc(Cl)c(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1083480 21015 0 None -1 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3cc(Cl)c(-c4cccc5cccnc45)cc3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
46890487 21227 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1C 10.1016/j.bmcl.2010.04.068
CHEMBL1084307 21227 0 None -4 2 Human 7.1 pKi = 7.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 377 3 0 2 5.7 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1C 10.1016/j.bmcl.2010.04.068
2241 4522 5 None -208 4 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligandBinding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00099a019
9810632 4522 5 None -208 4 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligandBinding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00099a019
CHEMBL127686 4522 5 None -208 4 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligandBinding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand
ChEMBL 738 6 2 8 2.3 CC[C@@H]([C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](N(C(=O)[C@H]2N(C(=O)[C@@H]3N(C1=O)N=CCC3)N=CCC2)C)Cc1ccccc1)C 10.1021/jm00099a019
118734336 237398 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416770 237398 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S@@+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
46890531 21066 0 None -38 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 455 5 0 3 7.2 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2010.04.068
CHEMBL1083732 21066 0 None -38 2 Human 6.1 pKi = 6.1 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 455 5 0 3 7.2 COc1cc(C(=O)N2C[C@]3(C)C[C@H]2CC(C)(C)C3)ccc1-c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2010.04.068
172449149 389255 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 444 3 0 4 6.9 O=C(c1ccc(/N=N/c2ccc(F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5435397 389255 0 None None None Human 6.1 pKi = 6.1 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 435 nm and further incubated for 1 hr by HTRF assay
ChEMBL 444 3 0 4 6.9 O=C(c1ccc(/N=N/c2ccc(F)cc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
10144208 216771 0 None -1047 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 557 7 0 6 6.2 Cc1cccc(OCc2ccc(C(=O)N3CCN(C)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
CHEMBL316093 216771 0 None -1047 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 557 7 0 6 6.2 Cc1cccc(OCc2ccc(C(=O)N3CCN(C)CC3)cc2)c1-n1c(C)nnc1-c1ccc(-c2ccccc2)cc1 10.1021/jm010544r
19607875 237397 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416769 237397 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 418 3 1 3 4.4 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCC[S+]([O-])c3ccccc32)cc1 10.1021/acs.jmedchem.5b00289
73350823 202597 0 None -575 9 Human 5.1 pKi = 5.1 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 202597 0 None -575 9 Human 5.1 pKi = 5.1 Binding
Binding affinity to human V2R by competitive binding assayBinding affinity to human V2R by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
2042 8014 41 None -60 6 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
2176 8014 41 None -60 6 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
439302 8014 41 None -60 6 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
CHEMBL395429 8014 41 None -60 6 Rat 7.1 pKi = 7.1 Binding
Binding affinity against Vasopressin receptor in rat kidney medullaBinding affinity against Vasopressin receptor in rat kidney medulla
ChEMBL 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 10.1021/jm00171a003
118734335 237396 0 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3c(C)cccc32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416768 237396 0 None -18 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 416 3 1 3 5.7 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCSc3c(C)cccc32)cc1 10.1021/acs.jmedchem.5b00289
10165683 215809 0 None -676 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 537 13 0 6 6.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
CHEMBL313451 215809 0 None -676 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 537 13 0 6 6.9 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCCCN1CCN(C)CC1 10.1021/jm010544r
178292835 465440 0 None -25 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 493 3 1 7 3.5 Cc1ccccc1C(=O)NC1CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
CHEMBL6078167 465440 0 None -25 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 493 3 1 7 3.5 Cc1ccccc1C(=O)NC1CCN(c2nnc3n2-c2ccc(Cl)cc2CC2(C3)OCCO2)CC1 10.1016/j.ejmech.2024.117069
168294720 375496 0 None 16 2 Human 8.1 pKi = 8.1 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
CHEMBL5208751 375496 0 None 16 2 Human 8.1 pKi = 8.1 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 601 9 1 5 6.5 CCN1CCN(CCCN2CCCN(C(=O)c3ccc(NC(=O)c4ccccc4-c4ccccc4)cc3)c3ccccc32)CC1 10.1021/acs.jmedchem.2c00567
10392505 218193 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
CHEMBL320416 218193 0 None 4 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 539 3 1 3 6.6 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3cc(Cl)ccc32)cc1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00649-2
9915472 327811 0 None 14 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
CHEMBL443498 327811 0 None 14 2 Human 8.1 pKi = 8.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 547 4 1 3 7.3 O=C(Nc1ccc(C(=O)N2C[C@@H]3C4CCC(C4)N3Cc3ccccc32)c(Cl)c1)c1ccccc1-c1ccccc1 10.1016/s0960-894x(02)00649-2
44325531 474093 0 None None None Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
CHEMBL92470 474093 0 None None None Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptorInhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
ChEMBL 537 4 1 4 6.3 O=C(Nc1ccc(C(=O)N2CC3CSCCN3Cc3ccc(F)cc32)cc1)c1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.03.083
71455302 163803 0 None 194 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
71482380 163803 0 None 194 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
CHEMBL2172290 163803 0 None 194 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 minsDisplacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
ChEMBL 1441 33 5 17 10.3 CCN1/C(=C/C=C/C=C/C2=[N+](CC)c3ccc(S(=O)(=O)[O-])cc3C2(C)C)C(C)(CCCC(=O)NCCOCCOCCOCCn2cc(CNC(=O)CCC(=O)NC3CCCN(C(=O)c4ccc(NC(=O)c5ccccc5-c5ccccc5)cc4)c4ccccc43)nn2)c2cc(S(=O)(=O)O)ccc21 10.1021/jm3006146
44520876 26709 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 5 1 5 5.9 Cc1cc(C)n(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
CHEMBL1185998 26709 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 561 5 1 5 5.9 Cc1cc(C)n(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCc4ccccn4)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2008.09.039
46890261 21014 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c(Cl)c3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
CHEMBL1083479 21014 0 None 3 2 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 562 3 0 2 9.6 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2ccc(-c3ccc(-c4cccc5cccnc45)c(Cl)c3Cl)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
44520872 26878 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL1186989 26878 0 None None None Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 533 5 1 5 5.3 O=C(/C=C1/c2ccccc2N(C(=O)c2ccc(-n3cccn3)cc2Cl)CCC1(F)F)NCc1ccccn1 10.1016/j.bmc.2008.09.039
CHEMBL3037878 477824 0 None None None Pig 8.0 pKi = 8.0 Binding
Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidneyInhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney
ChEMBL 1065 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SCSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00122a017
44294507 196832 0 None None None Pig 8.0 pKi = 8.0 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
CHEMBL262499 196832 0 None None None Pig 8.0 pKi = 8.0 Binding
Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
ChEMBL 1051 17 9 13 1.4 CCOc1ccc(C[C@H]2NC(=O)CC3(CCCCC3)SSC[C@H](C(=O)N3CCC[C@H]3C(=O)N[C@H](CCCCN)C(N)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm00150a003
119369 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
2197 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
4004 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
CHEMBL420762 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm000108p
119369 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
2197 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
4004 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
CHEMBL420762 5304 49 None 1 6 Human 8.0 pKi = 8.0 Binding
Binding affinity to vasopressin V2 receptorBinding affinity to vasopressin V2 receptor
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1021/jm3006146
42629369 356021 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
CHEMBL478283 356021 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human V2 receptor expressed in CHO cellsDisplacement of [3H]vasopressin from human V2 receptor expressed in CHO cells
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.03.001
42629369 356021 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
CHEMBL478283 356021 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation countingDisplacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells by microplate scintillation counting
ChEMBL 500 5 2 5 4.0 Cc1ccn(-c2ccc(C(=O)N3CCC(F)(F)/C(=C\C(=O)NCCO)c4ccccc43)c(Cl)c2)n1 10.1016/j.bmc.2009.10.038
56682530 125921 0 None -23 4 Human 8.0 pKi = 8 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 12 14 -2.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL1790575 125921 0 None -23 4 Human 8.0 pKi = 8 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
ChEMBL 1053 18 12 14 -2.6 CC[C@H](C)[C@@H]1NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)CCSSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
172997 4754 54 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
2238 4754 54 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
CHEMBL49429 4754 54 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
DB06666 4754 54 None 64 2 Human 7.1 pKi = 7.1 Binding
Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cellsInhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
ChEMBL 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 10.1016/s0960-894x(02)00649-2
CHEMBL5074709 478528 0 None -2951 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 410 3 1 6 3.9 O[C@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
2173 6017 25 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
3038506 6017 25 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
CHEMBL332447 6017 25 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
DB05838 6017 25 None 8 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting methodDisplacement of [3H]-AVP from human V2 receptor expressed in human HeLa cell membranes incubated for 2 hrs by scintillation counting method
ChEMBL 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10.1021/acs.jmedchem.8b00697
136961690 237392 0 None -87 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 412 3 1 6 4.2 Cc1ccn(Cc2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm501395b
CHEMBL3416757 237392 0 None -87 3 Human 6.0 pKi = 6.0 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL 412 3 1 6 4.2 Cc1ccn(Cc2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm501395b
135916069 463841 0 None -51 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 398 2 1 6 4.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm901084f
CHEMBL605373 463841 0 None -51 3 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cellsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
ChEMBL 398 2 1 6 4.1 Cc1ccn(-c2ccc(C(=O)N3Cc4cnn(C)c4Nc4ccccc43)cc2C)n1 10.1021/jm901084f
CHEMBL2371442 485717 0 None None None Pig 5.0 pKi = 5.0 Binding
Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparationInhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
ChEMBL 959 17 11 11 -3.3 CC(C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm00399a009
44275524 316842 0 None -53703 4 Human 5.0 pKi = 5.0 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1471 34 14 20 1.1 CN(C(=O)CCc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N(C(=O)c1ccc2c(c1)C(=O)OC21c2ccc(O)cc2Oc2cc(O)ccc21)[C@@H](CCCCN)C(N)=O 10.1021/jm9804782
91931053 316842 0 None -53703 4 Human 5.0 pKi = 5.0 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1471 34 14 20 1.1 CN(C(=O)CCc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N(C(=O)c1ccc2c(c1)C(=O)OC21c2ccc(O)cc2Oc2cc(O)ccc21)[C@@H](CCCCN)C(N)=O 10.1021/jm9804782
CHEMBL412210 316842 0 None -53703 4 Human 5.0 pKi = 5.0 Binding
The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptorThe inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
ChEMBL 1471 34 14 20 1.1 CN(C(=O)CCc1ccc(O)cc1)[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N(C(=O)c1ccc2c(c1)C(=O)OC21c2ccc(O)cc2Oc2cc(O)ccc21)[C@@H](CCCCN)C(N)=O 10.1021/jm9804782
172442489 387876 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 426 3 0 4 6.8 O=C(c1ccc(/N=N\c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
CHEMBL5405357 387876 0 None None None Human 7.0 pKi = 7.0 Binding
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 426 3 0 4 6.8 O=C(c1ccc(/N=N\c2ccccc2)cc1Cl)N1Cc2cccn2Cc2ccccc21 10.1021/acs.jmedchem.2c01625
56678446 125925 0 None -4466 3 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1125 16 13 16 -0.3 CC[C@@H](C)[C@H]1NC(=O)[C@@](C)(c2ccc(O)cc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@H](C(N)=O)c2ccc(O)cc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H]([C@@H](C)O)NC1=O 10.1021/jm010526+
CHEMBL1790712 125925 0 None -4466 3 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL 1125 16 13 16 -0.3 CC[C@@H](C)[C@H]1NC(=O)[C@@](C)(c2ccc(O)cc2)NC(=O)CC2(CCCCC2)SSC[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](CCCN)C(=O)N[C@H](C(N)=O)c2ccc(O)cc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H]([C@@H](C)O)NC1=O 10.1021/jm010526+
15953022 237440 0 None -4677 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assayDisplacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
ChEMBL 436 3 0 3 5.7 Cc1c(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccccc2n1Cc1ccccc1 10.1021/jm501745f
CHEMBL3416860 237440 0 None -4677 3 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assayDisplacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
ChEMBL 436 3 0 3 5.7 Cc1c(C(=O)N2CCC3(CC2)OCc2ccccc23)c2ccccc2n1Cc1ccccc1 10.1021/jm501745f
44314552 469916 0 None -18 2 Rat 7.0 pKi = 7.0 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 628 12 1 6 6.8 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCC(N3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00723-5
CHEMBL77105 469916 0 None -18 2 Rat 7.0 pKi = 7.0 Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 628 12 1 6 6.8 Cc1ccc(N(C)C(=O)c2ccc(NC(=O)c3ccoc3C)cc2)c(OCCCCCC(=O)N2CCC(N3CCCCC3)CC2)c1 10.1016/s0960-894x(01)00723-5
11340891 6755 33 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
8403 6755 33 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
CHEMBL429736 6755 33 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
DB11818 6755 33 None -891 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL 494 6 1 6 2.0 CC[C@@H]([C@@H]1C(=O)N[C@@H](C(=O)N1[C@@H](C(=O)N1CCOCC1)c1coc(n1)C)C1Cc2c(C1)cccc2)C 10.1016/j.bmcl.2007.11.008
2253 4548 22 None -12882 6 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
5311202 4548 22 None -12882 6 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
CHEMBL306645 4548 22 None -12882 6 Rat 5.0 pKi = 5.0 Binding
Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissueDisplacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
ChEMBL 586 7 0 7 4.4 COc1cc(ccc1C(=O)N1CCC(CC1)N1C(=O)OCc2c1cccc2)OC1CCN(CC1)Cc1ccc[n+](c1C)[O-] 10.1021/jm901812z
10303620 473255 0 None -933 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
CHEMBL86949 473255 0 None -933 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligandBinding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
ChEMBL 577 12 0 6 7.8 Cc1nnc(-c2ccc(-c3ccccc3)cc2)n1-c1ccccc1OCCCCCCN1CCC(N2CCCCC2)CC1 10.1021/jm010544r
53349471 237401 0 None -22 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
CHEMBL3416774 237401 0 None -22 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranesDisplacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
ChEMBL 413 3 1 3 5.0 Cc1ccccc1C(=O)Nc1ccc(C(=O)N2CCCN(C)c3cccc(C)c32)cc1 10.1021/acs.jmedchem.5b00289
168297437 375392 0 None None None Human 7.0 pKi = 7 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.2c00567
CHEMBL5207214 375392 0 None None None Human 7.0 pKi = 7 Binding
Displacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assayDisplacement of conivaptan-red from SNAP-tagged human V2 receptor expressed in HEK293 cells measured after 1 hr by HTRF assay
ChEMBL 566 7 1 5 5.8 O=C(Nc1ccc(C(=O)N2CCCN(CCCN3CCOCC3)c3ccccc32)cc1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.2c00567
155753091 465451 0 None -489 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 443 2 0 7 3.2 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(N5CCCCC5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
CHEMBL6078453 465451 0 None -489 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constantDisplacement of [3H]AVP from human vasopressin V2 receptor expressed in human 1321N1 cells assessed as inhibition constant
ChEMBL 443 2 0 7 3.2 Clc1ccc2c(c1)CC1(Cc3nnc(N4CCC(N5CCCCC5)CC4)n3-2)OCCO1 10.1016/j.ejmech.2024.117069
119369 5304 49 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 5304 49 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 5304 49 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 5304 49 None None None Rat 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidneyDisplacement of [3H]-AVP from its AVP-V2 receptor binding site in rat kidney
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
146681949 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2168 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2810 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
644077 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
CHEMBL373742 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
DB00067 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01185 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01186 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P35455 8624 35 None None None Pig 8.1 pIC50 = 8.1 Binding
Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cellsTested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
146681949 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2168 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2810 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
644077 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
CHEMBL373742 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
DB00067 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01185 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01186 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P35455 8624 35 None -2 3 Bovine 8.1 pKd = 8.1 Binding
Inhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membraneInhibition of radioligand [3H]AVP binding to V2 receptor in bovine kidney inner medulla membrane
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
10615 1182 36 None -3715352 3 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
46200932 1182 36 None -3715352 3 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
CHEMBL4297183 1182 36 None -3715352 3 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
DB14823 1182 36 None -3715352 3 Human 5.0 pKd = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 3 0 6 4.4 CN1Cc2cc(Cl)ccc2n2c(C1)nnc2[C@@H]1CC[C@H](CC1)Oc1ccccn1 31951127
2228 7911 0 None None None Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2964362
3817 7914 0 None None None Human 8.6 pKd = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
158348 8062 0 None None None Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)C1(CCC(CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
158348 8062 0 None None None Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)C1(CCC(CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
2234 8062 0 None None None Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)C1(CCC(CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
2234 8062 0 None None None Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)C1(CCC(CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
CHEMBL1628660 8062 0 None None None Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)C1(CCC(CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
CHEMBL1628660 8062 0 None None None Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)C1(CCC(CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
10124389 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 10780976
10124389 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9459574
10124389 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9792651
10124389 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9864265
10124389 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9884074
2175 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 10780976
2175 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9459574
2175 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9792651
2175 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9864265
2175 7880 0 None -3 5 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9884074
2042 8014 41 None -512 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
2176 8014 41 None -512 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
439302 8014 41 None -512 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
CHEMBL395429 8014 41 None -512 4 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
10124389 7880 0 None -3 5 Rat 8.8 pKd None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9792651
2175 7880 0 None -3 5 Rat 8.8 pKd None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1085 31 16 16 -5.9 NC(=O)CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)NCC(N)=O 9792651
2232 7642 0 None -1 2 Human 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2233 7643 0 None -1 2 Human 9.1 pKd None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2231 7640 0 None None None Rat 9.2 pKd None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2232 7642 0 None 1 2 Rat 9.3 pKd None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2233 7643 0 None 1 2 Rat 9.4 pKd None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2230 7639 0 None None None Rat 9.5 pKd None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
11169 1650 39 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C None
165708555 1650 39 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C None
16681432 1650 39 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C None
495 1650 39 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C None
CHEMBL3301668 1650 39 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C None
DB01282 1650 39 None -1 2 Human 8.3 pKi = 8.3 Binding
vasopressin V2 receptors expressed in COS-7 cellsvasopressin V2 receptors expressed in COS-7 cells
Drug Central 987 18 10 13 -2.5 CC[C@@H]([C@@H]1NC(=O)[C@@H](NC(=O)CCCSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)Cc1ccc(cc1)OC)C None
2213 1072 37 None -87 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C None
3008 1072 37 None -87 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C None
5311010 1072 37 None -87 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C None
68613 1072 37 None -87 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C None
CHEMBL378642 1072 37 None -87 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C None
CHEMBL382301 1072 37 None -87 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C None
DB09059 1072 37 None -87 5 Human 8.2 pKi = 8.2 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
Drug Central 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C None
2042 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
2174 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
439302 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
CHEMBL395429 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
DB00107 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
P01178 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
P01179 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
P35454 6074 0 None -2 7 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C None
119369 5304 49 None 1 6 Human 8.1 pKi = 8.1 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 5304 49 None 1 6 Human 8.1 pKi = 8.1 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 5304 49 None 1 6 Human 8.1 pKi = 8.1 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 5304 49 None 1 6 Human 8.1 pKi = 8.1 Binding
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
Drug Central 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
5311065 484177 30 None -7 8 Human 8.1 pKi = 8.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
817 484177 30 None -7 8 Human 8.1 pKi = 8.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
CHEMBL1429 484177 30 None -7 8 Human 8.1 pKi = 8.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
DB00035 484177 30 None -7 8 Human 8.1 pKi = 8.1 Binding
Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptorsBinding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
151171 2408 36 None -5 5 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 2408 36 None -5 5 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 2408 36 None -5 5 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 2408 36 None -5 5 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 2408 36 None -5 5 Rat 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting methodDisplacement of [3H]AVP from V2 receptor in Wistar rat kidney membranes incubated for 60 mins by microplate scintillation counting method
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216237 8365 53 None -2 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 8365 53 None -2 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 8365 53 None -2 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 8365 53 None -2 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 8365 53 None -2 7 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
146681949 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2168 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2810 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
644077 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
CHEMBL373742 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
DB00067 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01185 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01186 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P35455 8624 35 None -5 8 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 minsDisplacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
216237 8365 53 None 2 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 8365 53 None 2 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 8365 53 None 2 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 8365 53 None 2 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 8365 53 None 2 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
5311065 484177 30 None 1 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
817 484177 30 None 1 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
CHEMBL1429 484177 30 None 1 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
DB00035 484177 30 None 1 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1068 19 14 15 -4.1 N=C(N)NCCC[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1)C(=O)NCC(N)=O None
146681949 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2168 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
2810 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
644077 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
CHEMBL373742 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
DB00067 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01185 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P01186 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
P35455 8624 35 None -2 8 Rat 8.0 pKi = 8.0 Binding
Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranesDisplacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
Drug Central 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N None
151171 2408 36 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 2408 36 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 2408 36 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 2408 36 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 2408 36 None 2 5 Human 8.0 pKi = 8.0 Binding
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
Drug Central 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
10444 4740 20 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Guide to Pharmacology 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 30199637
145711714 4740 20 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Guide to Pharmacology 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 30199637
CHEMBL4204210 4740 20 None -7 3 Human 5.8 pKi = 5.8 Binding
Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V<sub>2</sub> receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
Guide to Pharmacology 531 4 2 6 4.2 Cc1c(ccc(c1)C(=O)N1Cc2c(Nc3ccccc13)n(nc2)C)CNC(=O)N1CCC[C@H]1C(=S)N(C)C 30199637
2184 3071 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2184 3071 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1649739
2184 3071 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2173 6017 25 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
3038506 6017 25 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
CHEMBL332447 6017 25 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
DB05838 6017 25 None 8 2 Human 7.0 pKi = 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 5 1 3 5.4 CC(NC(=O)C[C@H]1CCCN(c2c1cccc2)C(=O)c1ccc(cc1Cl)N1CCCC1)C 10780976
2236 2773 0 None None None Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1072 30 12 13 -1.4 CC[C@H]([C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)CS)CC(=O)N)NC(=O)[C@@H](NC(=O)[C@H]([C@H](CC)C)NC(=O)CC1CCCCC1=S)Cc1ccccc1)C 11012895
2236 2773 0 None None None Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1072 30 12 13 -1.4 CC[C@H]([C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)CS)CC(=O)N)NC(=O)[C@@H](NC(=O)[C@H]([C@H](CC)C)NC(=O)CC1CCCCC1=S)Cc1ccccc1)C 9792651
3080966 2773 0 None None None Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1072 30 12 13 -1.4 CC[C@H]([C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)CS)CC(=O)N)NC(=O)[C@@H](NC(=O)[C@H]([C@H](CC)C)NC(=O)CC1CCCCC1=S)Cc1ccccc1)C 11012895
3080966 2773 0 None None None Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1072 30 12 13 -1.4 CC[C@H]([C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)CS)CC(=O)N)NC(=O)[C@@H](NC(=O)[C@H]([C@H](CC)C)NC(=O)CC1CCCCC1=S)Cc1ccccc1)C 9792651
2172 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 11012895
2172 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 9322919
2959 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 11012895
2959 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 9322919
644076 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 11012895
644076 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 9322919
CHEMBL1200690 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 11012895
CHEMBL1200690 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 9322919
DB14642 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 11012895
DB14642 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 9322919
P01183 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 11012895
P01183 4864 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1055 19 13 16 -4.3 NCCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1 9322919
119369 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
119369 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
119369 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
119369 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
119369 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
2197 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
2197 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
2197 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
2197 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
2197 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
4004 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
4004 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
4004 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
4004 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
4004 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
CHEMBL420762 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 11012895
CHEMBL420762 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9322919
CHEMBL420762 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
CHEMBL420762 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
CHEMBL420762 5304 49 None 1 6 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9884074
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
16051933 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
2181 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
2182 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
27991 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
46783812 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
CHEMBL264448 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
CHEMBL376685 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 10780976
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 11012895
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 7774575
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9264324
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9322919
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
DB00035 2746 7 None -3 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9884074
2169 963 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1049 19 14 16 -5.6 CC[C@@H](C1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)C 7774575
2169 963 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1049 19 14 16 -5.6 CC[C@@H](C1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)C 9322919
68649 963 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1049 19 14 16 -5.6 CC[C@@H](C1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)C 7774575
68649 963 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1049 19 14 16 -5.6 CC[C@@H](C1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)C 9322919
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
146681949 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
2168 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
2810 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
644077 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
CHEMBL373742 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
DB00067 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
P01185 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
P01186 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10519430
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 10780976
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 11012895
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 12446593
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 15084136
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 7774575
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9264324
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9322919
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9459574
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9864265
P35455 8624 35 None -5 8 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1083 19 14 16 -5.4 NC(=O)C[C@@H]1NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N)N 9884074
158348 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
158348 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
158348 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
158348 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
158348 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
2199 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
2199 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
2199 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
2199 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
2199 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
CHEMBL4283439 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
CHEMBL4283439 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
CHEMBL4283439 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
CHEMBL4283439 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
CHEMBL4283439 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
DB14923 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 10519430
DB14923 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 11012895
DB14923 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 8981918
DB14923 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
DB14923 7090 19 None -2 4 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9884074
172997 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
172997 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
2238 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
2238 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
CHEMBL49429 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
CHEMBL49429 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
DB06666 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 11012895
DB06666 4754 54 None 64 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 3 1 3 6.1 Fc1ccc(c(c1)C(=O)Nc1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2)C 9651149
216237 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
2226 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
4110 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
CHEMBL344159 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
DB06212 8365 53 None 2 7 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
151171 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
2203 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
732 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
CHEMBL1755 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
DB00872 2408 36 None 2 5 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 20471258
8529 6823 0 None -30199 3 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 4 0 4 3.9 CN(CCN1CC(c2c1cc(Cl)cc2)C(=O)N1CCC2(CC1)OCc1c2cccc1)C 25654260
91827367 6823 0 None -30199 3 Human 4.5 pKi > 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 4 0 4 3.9 CN(CCN1CC(c2c1cc(Cl)cc2)C(=O)N1CCC2(CC1)OCc1c2cccc1)C 25654260
114904 6013 43 None -1148 5 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 9322919
2196 6013 43 None -1148 5 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 9322919
CHEMBL296908 6013 43 None -1148 5 Human 4.5 pKi None 4.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 9322919
2222 2786 0 None -794 3 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2209 6290 0 None -707 3 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2213 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 12660315
2213 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 14722330
3008 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 12660315
3008 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 14722330
5311010 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 12660315
5311010 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 14722330
68613 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 12660315
68613 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 14722330
CHEMBL378642 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 12660315
CHEMBL378642 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 14722330
CHEMBL382301 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 12660315
CHEMBL382301 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 14722330
DB09059 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 12660315
DB09059 1072 37 None -87 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 993 18 11 15 -3.0 NCCC[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@H](Cc2ccc(cc2)OCC)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)[C@H](O)C)[C@H](CC)C 14722330
2202 5638 34 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
9895468 5638 34 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
CHEMBL582857 5638 34 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
DB12643 5638 34 None -489 5 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 629 8 1 9 2.9 COc1cc(OC)ccc1S(=O)(=O)N1c2ccc(cc2[C@@](C1=O)(N1C[C@@H](C[C@H]1C(=O)N(C)C)O)c1ccccc1OC)Cl 11861823
2221 2793 0 None -3981 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2221 2793 0 None -3981 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2042 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
2042 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
2042 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
2042 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
2042 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
2042 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
2174 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
2174 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
2174 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
2174 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
2174 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
2174 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
439302 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
439302 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
439302 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
439302 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
439302 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
439302 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
CHEMBL395429 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
CHEMBL395429 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
CHEMBL395429 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
CHEMBL395429 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
CHEMBL395429 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
CHEMBL395429 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
DB00107 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
DB00107 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
DB00107 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
DB00107 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
DB00107 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
DB00107 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
P01178 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
P01178 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
P01178 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
P01178 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
P01178 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
P01178 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
P01179 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
P01179 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
P01179 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
P01179 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
P01179 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
P01179 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
P35454 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 12660315
P35454 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 7774575
P35454 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9264324
P35454 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9322919
P35454 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9459574
P35454 6074 0 None -234 7 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1006 17 12 15 -3.6 CC[C@@H]([C@@H]1NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@@H](N)CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CC(C)C)C 9884074
2188 2768 0 None -316 4 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2186 2766 0 None -630 4 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2195 5927 0 None -794 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2204 8913 7 None -1258 4 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 15661579
9917025 8913 7 None -1258 4 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 15661579
CHEMBL3307200 8913 7 None -1258 4 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 616 5 1 5 6.4 O=C(N1CCC(CC1)N1CCCCC1)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccoc1C 15661579
2187 2764 0 None -707 4 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2210 6291 0 None -398 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
119517 3038 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1110 20 12 15 -3.3 COc1ccc(cc1)CC1NC(=O)CC(C)(C)SSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N 11012895
119517 3038 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1110 20 12 15 -3.3 COc1ccc(cc1)CC1NC(=O)CC(C)(C)SSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N 9884074
2225 3038 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1110 20 12 15 -3.3 COc1ccc(cc1)CC1NC(=O)CC(C)(C)SSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N 11012895
2225 3038 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1110 20 12 15 -3.3 COc1ccc(cc1)CC1NC(=O)CC(C)(C)SSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N 9884074
2208 6288 0 None -281 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2208 6288 0 None -281 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2190 2975 0 None -501 4 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2189 2977 0 None -630 4 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2185 3073 0 None -501 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2211 6293 0 None -398 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2219 2788 0 None -199 4 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11337500
2200 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
2200 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
2200 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
2200 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
2200 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
60943 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
60943 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
60943 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
60943 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
60943 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
CHEMBL419667 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
CHEMBL419667 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
CHEMBL419667 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
CHEMBL419667 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
CHEMBL419667 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
DB13929 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 10866830
DB13929 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11012895
DB13929 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 11429400
DB13929 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9322919
DB13929 6732 0 None -89 4 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 619 7 2 7 3.3 COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl 9884074
2223 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 10866830
2223 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 11012895
2223 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9264324
2223 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9322919
2223 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9459574
2223 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9884074
6917952 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 10866830
6917952 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 11012895
6917952 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9264324
6917952 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9322919
6917952 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9459574
6917952 2784 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1151 20 12 15 -2.3 COc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)CCC(=O)N)CC(=O)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C(=O)NCC(=O)N)CCCN=C(N)N 9884074
2235 2775 0 None -31 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2191 2979 0 None -630 4 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2215 2770 0 None -1 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
164712 6321 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1040 17 12 15 -3.4 CC(C[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1)C 7774575
2178 6321 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1040 17 12 15 -3.4 CC(C[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1)C 7774575
CHEMBL3272682 6321 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1040 17 12 15 -3.4 CC(C[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccc(cc2)O)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CC(=O)N)CCC(=O)N)Cc1ccccc1)C 7774575
2237 2777 0 None -19 2 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2212 8201 0 None -63 3 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2214 2771 0 None -1 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2214 2771 0 None -1 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2170 2748 0 None -7 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2170 2748 0 None -7 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
119369 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
119369 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
2197 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
2197 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
4004 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
4004 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
CHEMBL420762 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9792651
CHEMBL420762 5304 49 None -1 6 Rat 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 9864265
122322 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 11012895
122322 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 9884074
2217 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 11012895
2217 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 9884074
44294542 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 11012895
44294542 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 9884074
44382370 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 11012895
44382370 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 9884074
CHEMBL262423 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 11012895
CHEMBL262423 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 9884074
CHEMBL384776 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 11012895
CHEMBL384776 2781 0 None -3 4 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1079 17 10 13 0.3 CCOc1ccc(cc1)C[C@H]1NC(=O)CC2(CCCCC2)SSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)Cc1ccccc1)C(C)C)CC(=O)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N)CCCN=C(N)N 9884074
16051933 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
16051933 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
2181 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
2181 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
2182 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
2182 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
27991 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
27991 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
46783812 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
46783812 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
CHEMBL264448 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
CHEMBL264448 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
CHEMBL376685 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
CHEMBL376685 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
DB00035 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 12446593
DB00035 2746 7 None -3 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 15084136
2170 2748 0 None 7 3 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2235 2775 0 None 31 2 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
171113 8611 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1054 17 13 15 -4.0 NC(=O)C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)NCC(=O)N)CCCN=C(N)N)N)Cc1ccc(cc1)O)Cc1ccccc1)C(C)C 12446593
2180 8611 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1054 17 13 15 -4.0 NC(=O)C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)NCC(=O)N)CCCN=C(N)N)N)Cc1ccc(cc1)O)Cc1ccccc1)C(C)C 12446593
CHEMBL3274309 8611 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1054 17 13 15 -4.0 NC(=O)C[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)NCC(=O)N)CCCN=C(N)N)N)Cc1ccc(cc1)O)Cc1ccccc1)C(C)C 12446593
2237 2777 0 None 19 2 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
16051933 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
2181 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
2182 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
27991 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
46783812 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
CHEMBL264448 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
CHEMBL376685 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
DB00035 2746 7 None 2 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 1068 19 13 15 -4.3 NC(=O)CC1NC(=O)C(CCC(=O)N)NC(=O)C(Cc2ccccc2)NC(=O)C(NC(=O)CCSSCC(NC1=O)C(=O)N1CCCC1C(=O)NC(C(=O)NCC(=O)N)CCCN=C(N)N)Cc1ccc(cc1)O 9792651
2183 3114 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2183 3114 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
6441676 3114 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
6441676 3114 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2229 7340 0 None None None Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
216237 8365 53 None -2 7 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
2226 8365 53 None -2 7 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
4110 8365 53 None -2 7 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
CHEMBL344159 8365 53 None -2 7 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
DB06212 8365 53 None -2 7 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 9864265
2205 8924 8 None -3 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 11429400
9810140 8924 8 None -3 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 11429400
CHEMBL307483 8924 8 None -3 5 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 648 6 1 4 7.2 CN(C1CCN(CC1)C(=O)/C=C\1/c2ccccc2N(CCC1(F)F)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1)C 11429400
2198 6959 2 None 46 2 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 16620295
9807249 6959 2 None 46 2 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 16620295
CHEMBL1192593 6959 2 None 46 2 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 537 4 1 4 6.1 Clc1cc(ccc1C(=O)N1C[C@H]2COCCN2Cc2c1cccc2)NC(=O)c1ccccc1c1ccccc1 16620295
2216 2779 0 None -1 2 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10866830
158348 7090 19 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
2199 7090 19 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
CHEMBL4283439 7090 19 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651
DB14923 7090 19 None 2 4 Rat 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 643 10 1 9 3.9 CCOc1ccc2c(c1)[C@@]1(CC[C@H](CC1)OCCN1CCOCC1)C(=O)N2S(=O)(=O)c1ccc(cc1OC)C(=O)NC(C)(C)C 9792651