Ligand source activities (1 row/activity)





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90469674 171820 7 None 3 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 171820 7 None 3 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
2181 1330 42 None 6 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 None None None None 10.1021/acs.jmedchem.9b00132
2182 1330 42 None 6 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 None None None None 10.1021/acs.jmedchem.9b00132
27991 1330 42 None 6 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 None None None None 10.1021/acs.jmedchem.9b00132
5311065 1330 42 None 6 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 None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL1429 1330 42 None 6 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 None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL264448 1330 42 None 6 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 None None None None 10.1021/acs.jmedchem.9b00132
DB00035 1330 42 None 6 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 None None None None 10.1021/acs.jmedchem.9b00132
44419026 168497 17 None 478 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 168497 17 None 478 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
2168 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
2810 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
644077 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
CHEMBL373742 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
DB00067 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
118476355 173862 3 None 5 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 173862 3 None 5 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
2168 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
2810 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
644077 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
CHEMBL373742 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
DB00067 3974 38 None -12 6 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 None None None None 10.1021/jm200278m
2168 3974 38 None -12 6 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 None None None None 10.1016/j.bmcl.2005.10.107
2810 3974 38 None -12 6 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 None None None None 10.1016/j.bmcl.2005.10.107
644077 3974 38 None -12 6 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 None None None None 10.1016/j.bmcl.2005.10.107
CHEMBL373742 3974 38 None -12 6 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 None None None None 10.1016/j.bmcl.2005.10.107
DB00067 3974 38 None -12 6 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 None None None None 10.1016/j.bmcl.2005.10.107
90469674 171820 7 None -3 3 Human 10.2 pEC50 = 10.2 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 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 171820 7 None -3 3 Human 10.2 pEC50 = 10.2 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 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
155523986 170908 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 170908 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
90469608 172258 0 None 812 2 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4474518 172258 0 None 812 2 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 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 10.1021/acs.jmedchem.9b00132
118476384 170871 0 None 1778 2 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4454160 170871 0 None 1778 2 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 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 10.1021/acs.jmedchem.9b00132
90469675 171415 0 None 1412 2 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 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
CHEMBL4462743 171415 0 None 1412 2 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 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
118476338 173389 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 173389 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
118476337 173587 0 None 1584 2 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4533159 173587 0 None 1584 2 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 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 10.1021/acs.jmedchem.9b00132
118476357 175588 0 None 2630 2 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4579754 175588 0 None 2630 2 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 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 10.1021/acs.jmedchem.9b00132
118476361 173733 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 173733 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
118476343 174095 0 None 1174 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4544907 174095 0 None 1174 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 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 10.1021/acs.jmedchem.9b00132
118476360 173560 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 173560 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 172057 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 172057 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 170189 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 170189 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 171209 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 171209 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
118476365 173848 0 None 794 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4539100 173848 0 None 794 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 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 10.1021/acs.jmedchem.9b00132
2181 1330 42 None -6 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 None None None None 10.1021/acs.jmedchem.9b00132
2182 1330 42 None -6 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 None None None None 10.1021/acs.jmedchem.9b00132
27991 1330 42 None -6 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 None None None None 10.1021/acs.jmedchem.9b00132
5311065 1330 42 None -6 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 None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL1429 1330 42 None -6 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 None None None None 10.1021/acs.jmedchem.9b00132
CHEMBL264448 1330 42 None -6 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 None None None None 10.1021/acs.jmedchem.9b00132
DB00035 1330 42 None -6 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 None None None None 10.1021/acs.jmedchem.9b00132
132095331 175222 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 175222 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
118476362 170946 0 None 575 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4455496 170946 0 None 575 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 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 10.1021/acs.jmedchem.9b00132
118476356 172207 0 None 1513 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4473843 172207 0 None 1513 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 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 10.1021/acs.jmedchem.9b00132
118476335 170315 0 None - 1 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4446853 170315 0 None - 1 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 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 10.1021/acs.jmedchem.9b00132
118476329 173164 0 None 954 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4521807 173164 0 None 954 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 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 10.1021/acs.jmedchem.9b00132
118476347 175333 0 None 501 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4574065 175333 0 None 501 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 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 10.1021/acs.jmedchem.9b00132
118476358 170666 0 None 2089 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4451555 170666 0 None 2089 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 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 10.1021/acs.jmedchem.9b00132
118476331 173524 0 None 2089 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 -0.8 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 10.1021/acs.jmedchem.9b00132
CHEMBL4531173 173524 0 None 2089 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 -0.8 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 10.1021/acs.jmedchem.9b00132
118476355 173862 3 None -5 3 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 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 173862 3 None -5 3 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 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
118476366 174051 0 None 741 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4543908 174051 0 None 741 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 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 10.1021/acs.jmedchem.9b00132
118476346 174513 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 174513 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 170680 0 None 1288 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 170680 0 None 1288 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
118476385 174609 0 None 169 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4557473 174609 0 None 169 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 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 10.1021/acs.jmedchem.9b00132
118476359 171407 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 171407 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
90468623 174160 0 None 588 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4546884 174160 0 None 588 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 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 10.1021/acs.jmedchem.9b00132
118476342 174592 0 None - 1 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4557118 174592 0 None - 1 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 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 10.1021/acs.jmedchem.9b00132
155513872 169796 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 169796 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
118476383 169756 0 None 457 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4438723 169756 0 None 457 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 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 10.1021/acs.jmedchem.9b00132
118476348 173520 0 None 457 3 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4531053 173520 0 None 457 3 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 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 10.1021/acs.jmedchem.9b00132
118476344 173376 0 None - 1 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 173376 0 None - 1 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
118476367 170199 0 None 758 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4445168 170199 0 None 758 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 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 10.1021/acs.jmedchem.9b00132
118476332 169540 0 None 630 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4435502 169540 0 None 630 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 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 10.1021/acs.jmedchem.9b00132
155542670 173158 0 None - 1 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 173158 0 None - 1 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
118476339 172795 0 None - 1 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4513567 172795 0 None - 1 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 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 10.1021/acs.jmedchem.9b00132
90469676 174403 0 None 2089 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL4552500 174403 0 None 2089 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 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 10.1021/acs.jmedchem.9b00132
CHEMBL1819440 209011 23 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 None None None 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 169609 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 169609 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 209011 23 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 None None None 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 4002 22 None 3 4 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 4002 22 None 3 4 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 4002 22 None 3 4 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 4002 22 None 3 4 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 4002 22 None 3 4 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 4002 22 None 3 4 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 199797 0 None - 1 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 199797 0 None - 1 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 201711 0 None - 1 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 201711 0 None - 1 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 199706 0 None - 1 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 199706 0 None - 1 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 199862 0 None - 1 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 199862 0 None - 1 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 12575 0 None - 1 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 12575 0 None - 1 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
CHEMBL479918 12575 0 None - 1 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 209012 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 None None None 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 209012 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 None None None 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 73858 0 None 43 3 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 73858 0 None 43 3 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 194485 0 None - 1 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
CHEMBL487164 194485 0 None - 1 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 194485 0 None - 1 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 194485 0 None - 1 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
CHEMBL487164 194485 0 None - 1 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 194485 0 None - 1 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 188351 0 None - 1 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 188351 0 None - 1 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 188916 0 None - 1 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 188916 0 None - 1 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 176741 0 None - 1 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 176741 0 None - 1 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 189841 0 None - 1 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 189841 0 None - 1 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 180338 0 None - 1 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 180338 0 None - 1 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 12579 0 None - 1 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 12579 0 None - 1 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
CHEMBL480104 12579 0 None - 1 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 161479 0 None -309 4 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 161479 0 None -309 4 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 174588 0 None - 1 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 174588 0 None - 1 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 796 37 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 None None None 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
131676677 796 37 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 None None None 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 796 37 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 None None None 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 796 37 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 None None None 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
495 796 37 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 None None None 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 796 37 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 None None None 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 796 37 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 None None None 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 12576 0 None - 1 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 12576 0 None - 1 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
CHEMBL479919 12576 0 None - 1 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 208980 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 None None None 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 208980 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 None None None 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 209021 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 None None None 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 209026 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 None None None 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 180509 0 None - 1 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 180509 0 None - 1 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 190783 0 None - 1 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 190783 0 None - 1 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 209021 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 None None None 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 64618 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 64618 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 209025 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 None None None 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 209026 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 None None None 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 64618 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 64618 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 209025 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 None None None 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 66063 0 None -74 2 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 66063 0 None -74 2 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 174589 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 174589 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 173413 0 None - 1 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 173413 0 None - 1 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 208985 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 None None None 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 208985 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 None None None 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 208986 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 None None None 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 174242 0 None - 1 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 174242 0 None - 1 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 176750 0 None - 1 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 176750 0 None - 1 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 176751 0 None - 1 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 176751 0 None - 1 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 193222 0 None - 1 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 193222 0 None - 1 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 208986 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 None None None 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 179228 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 179228 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 176900 0 None - 1 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 176900 0 None - 1 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 190586 33 None -6 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 190586 33 None -6 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 209015 9 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 None None None 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 209015 9 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 None None None 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 180817 0 None - 1 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 180817 0 None - 1 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 64631 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 64631 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 208982 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 None None None 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 64631 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 64631 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 64619 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 64619 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 208982 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 None None None 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 64801 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 64801 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 64619 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 64619 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 180337 0 None - 1 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 180337 0 None - 1 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 64801 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 64801 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 174587 0 None - 1 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 174587 0 None - 1 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 176749 0 None - 1 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 176749 0 None - 1 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 208988 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 None None None 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 2954 13 None -1 2 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 2954 13 None -1 2 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 2954 13 None -1 2 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 2954 13 None -1 2 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 161362 0 None -1348 4 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 161362 0 None -1348 4 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 208988 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 None None None 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 174589 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 174589 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 176988 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 176988 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 199942 0 None - 1 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 199942 0 None - 1 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 178935 0 None - 1 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 178935 0 None - 1 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 209022 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 None None None 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 209022 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 None None None 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 64798 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 64798 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 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
2174 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
2176 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
439302 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
CHEMBL395429 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
DB00107 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
18759802 176973 0 None - 1 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 176973 0 None - 1 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 64798 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 64798 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 66062 0 None -204 2 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 66062 0 None -204 2 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 179507 0 None - 1 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 179507 0 None - 1 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 179505 0 None - 1 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 179505 0 None - 1 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 137898 23 None -48 4 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 137898 23 None -48 4 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 190586 33 None 6 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 190586 33 None 6 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 209020 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 None None None 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 209020 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 None None None 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 208987 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 None None None 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 208987 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 None None None 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 64623 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 64623 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 64799 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 64799 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 3575 11 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 None None None None 10.1021/jm200278m
53330936 3575 11 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 None None None None 10.1021/jm200278m
CHEMBL1817709 3575 11 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 None None None None 10.1021/jm200278m
DB12495 3575 11 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 None None None None 10.1021/jm200278m
53362259 64623 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 64623 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 64799 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 64799 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 66058 10 None -102 2 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 66058 10 None -102 2 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 179255 0 None - 1 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 179255 0 None - 1 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 176744 0 None - 1 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 176744 0 None - 1 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 3575 11 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 None None None None 10.1021/jm200278m
53330936 3575 11 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 None None None None 10.1021/jm200278m
CHEMBL1817709 3575 11 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 None None None None 10.1021/jm200278m
DB12495 3575 11 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 None None None None 10.1021/jm200278m
CHEMBL1817704 208984 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 None None None 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 2981 58 None -26 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 None None None None 10.1016/j.bmc.2018.03.019
2174 2981 58 None -26 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 None None None None 10.1016/j.bmc.2018.03.019
2176 2981 58 None -26 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 None None None None 10.1016/j.bmc.2018.03.019
439302 2981 58 None -26 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 None None None None 10.1016/j.bmc.2018.03.019
CHEMBL395429 2981 58 None -26 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 None None None None 10.1016/j.bmc.2018.03.019
DB00107 2981 58 None -26 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 None None None None 10.1016/j.bmc.2018.03.019
CHEMBL1817704 208984 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 None None None 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 12732 0 None - 1 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 12732 0 None - 1 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
CHEMBL516757 12732 0 None - 1 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 176946 0 None - 1 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 176946 0 None - 1 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 174593 0 None - 1 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 174593 0 None - 1 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 64800 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 64800 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 64800 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 64800 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 66059 0 None -9 2 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 66059 0 None -9 2 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 209023 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 None None None 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 209023 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 None None None 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 176869 0 None - 1 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 176869 0 None - 1 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 161559 0 None -33 4 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 161559 0 None -33 4 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 189859 0 None - 1 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 189859 0 None - 1 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 208990 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 None None None 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 208990 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 None None None 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
25178787 176870 0 None - 1 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 176870 0 None - 1 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 209028 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 None None None 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 209028 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 None None None 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 208999 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 None None None 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 176994 0 None - 1 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 176994 0 None - 1 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 208999 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 None None None 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 161575 0 None -114 4 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 161575 0 None -114 4 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 163713 0 None 2 3 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 163713 0 None 2 3 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 209014 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 None None None 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 209014 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 None None None 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 182663 0 None - 1 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 182663 0 None - 1 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 179228 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 179228 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 189715 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 189715 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 189082 0 None - 1 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 189082 0 None - 1 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 2324 14 None -9 4 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
139030525 2324 14 None -9 4 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 2324 14 None -9 4 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 2324 14 None -9 4 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 176988 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 176988 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 189316 0 None - 1 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 189316 0 None - 1 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 209024 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 None None None 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 174594 0 None - 1 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 174594 0 None - 1 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 209024 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 None None None 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 179381 0 None - 1 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 179381 0 None - 1 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 65275 3 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 65275 3 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 64630 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 64630 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 64630 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 64630 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 65275 3 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 65275 3 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 182192 0 None - 1 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 182192 0 None - 1 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 182192 0 None - 1 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 182192 0 None - 1 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 12608 0 None - 1 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 12608 0 None - 1 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
CHEMBL485760 12608 0 None - 1 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 12693 0 None - 1 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 12693 0 None - 1 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
CHEMBL505517 12693 0 None - 1 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 189715 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 189715 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 2324 14 None -9 4 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
139030525 2324 14 None -9 4 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 2324 14 None -9 4 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 2324 14 None -9 4 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 796 37 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 None None None 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
131676677 796 37 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 None None None 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 796 37 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 None None None 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 796 37 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 None None None 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
495 796 37 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 None None None 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 796 37 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 None None None 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 796 37 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 None None None 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 176992 0 None - 1 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 176992 0 None - 1 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 209016 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 None None None 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 208983 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 None None None 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 208983 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 None None None 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 209016 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 None None None 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 189910 0 None - 1 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 189910 0 None - 1 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 209027 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 None None None 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 209027 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 None None None 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 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
2174 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
2176 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
439302 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
CHEMBL395429 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
DB00107 2981 58 None -26 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 None None None None 10.1021/acs.jmedchem.8b00697
21083212 174239 1 None - 1 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 174239 1 None - 1 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 176972 0 None - 1 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 176972 0 None - 1 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 180862 0 None - 1 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 180862 0 None - 1 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 122928 25 None -107 3 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 122928 25 None -107 3 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 209013 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 None None None 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 209013 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 None None None 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 189839 0 None - 1 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 189839 0 None - 1 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 208994 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 None None None 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 208994 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 None None None 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 209008 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 None None None 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 209008 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 None None None 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 201232 0 None 2 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 201232 0 None 2 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 168391 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 168391 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
11432362 94135 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 94135 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 107299 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 107299 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 116779 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 116779 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 110957 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 110957 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 154901 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 154901 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 1163 50 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
216322 1163 50 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 1163 50 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 1163 50 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 1163 50 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 1163 50 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 94192 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 94192 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 3841 89 None 41 7 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 3841 89 None 41 7 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 3841 89 None 41 7 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
443894 3841 89 None 41 7 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 3841 89 None 41 7 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 3841 89 None 41 7 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 154618 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 154618 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 163713 0 None 2 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 163713 0 None 2 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 94095 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 94095 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 168906 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 168906 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 199930 44 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 199930 44 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 191837 0 None - 1 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 191837 0 None - 1 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 164163 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 164163 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 154802 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 154802 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 94275 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 94275 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
44336784 109206 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 109206 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
135192997 173828 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 173828 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 192399 0 None - 1 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 192399 0 None - 1 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 175836 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 175836 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 174902 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 174902 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 199930 44 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 199930 44 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 94193 7 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 94193 7 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 18957 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 18957 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 116619 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 116619 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 107415 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 107415 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 176116 14 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 176116 14 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 57531 0 None - 1 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 57531 0 None - 1 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 163350 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 163350 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 154727 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 154727 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 63035 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 63035 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 118452 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 118452 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 154801 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 154801 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
25132666 94527 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 94527 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 115254 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 115254 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 117009 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 117009 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 154617 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 154617 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 108185 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 108185 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 66062 0 None -204 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 66062 0 None -204 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 4965 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 4965 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 5365 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 5365 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 94193 7 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 94193 7 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 63036 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 63036 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 57460 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 57460 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 165550 0 None - 1 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 165550 0 None - 1 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 66063 0 None -74 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 66063 0 None -74 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 94496 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 94496 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 171526 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 171526 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 6725 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 6725 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 66058 10 None -102 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 66058 10 None -102 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 4965 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 4965 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 192467 0 None - 1 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 192467 0 None - 1 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 190124 1 None - 1 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 190124 1 None - 1 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 160063 0 None - 0 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 160063 0 None - 0 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 79687 0 None - 0 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 79687 0 None - 0 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 210375 0 None - 0 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 None None None 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 97057 0 None - 0 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 97057 0 None - 0 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
44335358 155995 0 None - 0 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 155995 0 None - 0 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 209838 0 None - 0 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 None None None 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 209840 0 None - 0 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 None None None 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 209839 0 None - 0 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 None None None 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 97323 0 None - 0 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 97323 0 None - 0 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 210378 0 None - 0 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 None None None 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 160639 0 None - 0 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 160639 0 None - 0 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 210374 0 None - 0 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 None None None 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 210376 0 None - 0 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 None None None 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 157560 0 None - 0 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 157560 0 None - 0 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 168225 0 None - 0 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 168225 0 None - 0 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 210206 0 None - 0 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 None None None 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 186826 0 None - 0 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 186826 0 None - 0 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 178581 0 None - 0 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 178581 0 None - 0 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 112559 0 None - 0 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 112559 0 None - 0 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 199109 0 None - 0 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 199109 0 None - 0 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 111560 0 None - 0 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 111560 0 None - 0 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 207441 0 None - 0 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 207441 0 None - 0 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 175884 0 None - 0 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 175884 0 None - 0 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 132567 0 None - 0 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 132567 0 None - 0 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 112518 0 None - 0 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 112518 0 None - 0 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 207389 0 None - 0 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 207389 0 None - 0 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 178580 0 None - 0 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 178580 0 None - 0 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 12996 0 None - 0 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 12996 0 None - 0 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
CHEMBL539285 12996 0 None - 0 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 78345 0 None - 0 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
CHEMBL2093899 78345 0 None - 0 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 78345 0 None - 0 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 168004 0 None - 0 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 168004 0 None - 0 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 207342 0 None - 0 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 207342 0 None - 0 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
44386594 128199 0 None - 0 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 128199 0 None - 0 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 158444 0 None - 0 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 158444 0 None - 0 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 89477 0 None - 0 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 89477 0 None - 0 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 111424 0 None - 0 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 111424 0 None - 0 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 112567 0 None - 0 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 112567 0 None - 0 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 2330 57 None -4 5 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 2330 57 None -4 5 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 2330 57 None -4 5 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 2330 57 None -4 5 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 207308 0 None - 0 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 207308 0 None - 0 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 127903 0 None - 0 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 127903 0 None - 0 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 8261 0 None - 0 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 8261 0 None - 0 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 8432 0 None - 0 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 8432 0 None - 0 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 175885 0 None - 0 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 175885 0 None - 0 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 201050 0 None - 0 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 201050 0 None - 0 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 7994 0 None - 0 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 7994 0 None - 0 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 112154 0 None - 0 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 112154 0 None - 0 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 210214 0 None - 0 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 None None None 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 210209 0 None - 0 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 None None None 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
44382370 141548 0 None - 0 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(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(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
CHEMBL384776 141548 0 None - 0 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(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(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
44325915 112736 0 None - 0 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 112736 0 None - 0 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 3418 2 None - 0 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 3418 2 None - 0 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 3418 2 None - 0 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
44325896 207809 0 None - 0 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 207809 0 None - 0 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
44325895 207906 0 None - 0 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 207906 0 None - 0 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
44385658 158850 0 None - 0 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 158850 0 None - 0 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 106608 0 None - 0 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 106608 0 None - 0 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 89465 0 None - 0 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 89465 0 None - 0 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 178579 0 None - 0 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 178579 0 None - 0 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 189722 0 None - 0 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 189722 0 None - 0 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 111401 0 None - 0 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 111401 0 None - 0 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
44375638 168846 0 None - 0 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 168846 0 None - 0 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 175393 0 None - 0 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 175393 0 None - 0 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 192975 0 None - 0 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 192975 0 None - 0 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 112305 0 None - 0 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 112305 0 None - 0 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 164275 0 None - 0 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 164275 0 None - 0 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 2981 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
2174 2981 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
2176 2981 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
439302 2981 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
CHEMBL395429 2981 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
DB00107 2981 58 None -26 5 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central None None None None None
5280343 188273 124 None -31 12 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
CHEMBL1520590 188273 124 None -31 12 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 188273 124 None -31 12 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 4777 101 None -16 44 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 4777 101 None -16 44 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
3793 203207 77 None -2 4 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
45039617 203207 77 None -2 4 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 203207 77 None -2 4 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 4002 22 None 3 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 4002 22 None 3 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 4002 22 None 3 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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Type
Activity
Relation
Activity
Value
Assay
Type
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

3686 94665 108 None - 0 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 94665 108 None - 0 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 11846 22 None - 12 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
8478 11846 22 None - 12 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 11846 22 None - 12 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
CHEMBL221753 11846 22 None - 12 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 31219 105 None - 0 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 31219 105 None - 0 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 3777 74 None - 13 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 3777 74 None - 13 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 3777 74 None - 13 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 3777 74 None - 13 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 3777 74 None - 13 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 111579 48 None - 0 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 111579 48 None - 0 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 120246 49 None - 0 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 120246 49 None - 0 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 3858 58 None - 30 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 3858 58 None - 30 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 3858 58 None - 30 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 3858 58 None - 30 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 3858 58 None - 30 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 3858 58 None - 30 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 937 74 None - 1 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 937 74 None - 1 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
647 937 74 None - 1 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 937 74 None - 1 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 937 74 None - 1 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
68617 205525 62 None - 26 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
CHEMBL1709 205525 62 None - 26 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 205525 62 None - 26 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 3804 47 None - 25 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 3804 47 None - 25 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 3804 47 None - 25 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 3804 47 None - 25 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 3804 47 None - 25 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 3771 41 None - 2 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 3771 41 None - 2 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 3771 41 None - 2 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 100214 107 None - 0 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 100214 107 None - 0 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 63540 93 None - 0 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 63540 93 None - 0 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 1662 49 None - 33 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 1662 49 None - 33 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 1662 49 None - 33 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 1662 49 None - 33 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 1662 49 None - 33 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 3123 71 None - 30 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 3123 71 None - 30 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 3123 71 None - 30 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 3123 71 None - 30 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 3123 71 None - 30 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
191 403 98 None - 29 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
201 403 98 None - 29 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 403 98 None - 29 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 403 98 None - 29 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 403 98 None - 29 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 55114 45 None - 0 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 55114 45 None - 0 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 196533 92 None - 30 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 196533 92 None - 30 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 3588 83 None - 49 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 3588 83 None - 49 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 3588 83 None - 49 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 3588 83 None - 49 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 3588 83 None - 49 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
176 398 66 None - 31 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 398 66 None - 31 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 398 66 None - 31 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 398 66 None - 31 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 398 66 None - 31 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
118422671 2755 65 None - 4 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
1887 2755 65 None - 4 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 2755 65 None - 4 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 2755 65 None - 4 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 2755 65 None - 4 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 2755 65 None - 4 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 2755 65 None - 4 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 2755 65 None - 4 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 2755 65 None - 4 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 2755 65 None - 4 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 136966 32 None - 0 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 136966 32 None - 0 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 136966 32 None - 0 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 2481 33 None - 2 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 2481 33 None - 2 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 2481 33 None - 2 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 2481 33 None - 2 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
21722 17990 31 None - 6 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 17990 31 None - 6 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 14500 85 None - 0 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 14500 85 None - 0 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 518 46 None -660 5 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 None None None None 10.1038/s41467-023-40064-9
3008 518 46 None -660 5 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 None None None None 10.1038/s41467-023-40064-9
5311010 518 46 None -660 5 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 None None None None 10.1038/s41467-023-40064-9
68613 518 46 None -660 5 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 None None None None 10.1038/s41467-023-40064-9
CHEMBL378642 518 46 None -660 5 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 None None None None 10.1038/s41467-023-40064-9
CHEMBL382301 518 46 None -660 5 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 None None None None 10.1038/s41467-023-40064-9
DB09059 518 46 None -660 5 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 None None None None 10.1038/s41467-023-40064-9
2713 205269 82 None - 0 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 205269 82 None - 0 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 205269 82 None - 0 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 205269 82 None - 0 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 205269 82 None - 0 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
CHEMBL1330113 205269 82 None - 0 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 205269 82 None - 0 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 194724 86 None - 0 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 194724 86 None - 0 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 14490 19 None - 0 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 14490 19 None - 0 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 14490 19 None - 0 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 14490 19 None - 0 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 12612 15 None - 0 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 12612 15 None - 0 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 35059 9 None - 0 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 35059 9 None - 0 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
CHEMBL2103773 35059 9 None - 0 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
2168 3974 38 None -15 9 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 None None None None 10.1021/jm500365s
2810 3974 38 None -15 9 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 None None None None 10.1021/jm500365s
644077 3974 38 None -15 9 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 None None None None 10.1021/jm500365s
CHEMBL373742 3974 38 None -15 9 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 None None None None 10.1021/jm500365s
DB00067 3974 38 None -15 9 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 None None None None 10.1021/jm500365s
2181 1330 42 None -14 7 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 None None None None 10.1021/jm500365s
2182 1330 42 None -14 7 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 None None None None 10.1021/jm500365s
27991 1330 42 None -14 7 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 None None None None 10.1021/jm500365s
5311065 1330 42 None -14 7 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 None None None None 10.1021/jm500365s
CHEMBL1429 1330 42 None -14 7 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 None None None None 10.1021/jm500365s
CHEMBL264448 1330 42 None -14 7 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 None None None None 10.1021/jm500365s
DB00035 1330 42 None -14 7 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 None None None None 10.1021/jm500365s
118719821 115743 0 None - 0 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 115743 0 None - 0 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 115751 0 None - 0 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 115751 0 None - 0 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 115754 0 None - 0 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 115754 0 None - 0 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 115858 0 None - 0 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 115858 0 None - 0 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 64553 0 None - 0 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 64553 0 None - 0 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
118720277 115847 0 None - 0 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 115847 0 None - 0 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 115750 0 None - 0 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 115750 0 None - 0 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 115845 0 None - 0 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 115845 0 None - 0 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
118720266 115837 0 None - 0 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 115837 0 None - 0 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 123813 0 None - 0 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 123813 0 None - 0 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
118720274 115844 0 None - 0 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 115844 0 None - 0 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 169501 0 None - 0 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 169501 0 None - 0 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 115838 0 None - 0 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 115838 0 None - 0 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 126200 0 None - 0 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 126200 0 None - 0 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 115848 0 None - 0 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 115848 0 None - 0 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 115855 0 None - 0 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 115855 0 None - 0 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
118720262 115833 0 None - 0 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 115833 0 None - 0 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 115834 0 None - 0 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 115834 0 None - 0 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 115856 0 None - 0 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 115856 0 None - 0 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 115840 0 None - 0 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 115840 0 None - 0 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 115857 0 None - 0 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 115857 0 None - 0 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 115853 0 None - 0 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 115853 0 None - 0 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 796 37 None -1 2 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 None None None 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
131676677 796 37 None -1 2 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 None None None 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 796 37 None -1 2 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 None None None 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 796 37 None -1 2 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 None None None 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
495 796 37 None -1 2 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 None None None 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 796 37 None -1 2 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 None None None 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 796 37 None -1 2 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 None None None 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 115762 0 None - 0 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 115762 0 None - 0 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
118720272 115842 0 None - 0 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 115842 0 None - 0 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 115761 0 None - 0 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 115761 0 None - 0 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 115765 0 None - 0 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 115765 0 None - 0 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 66273 0 None - 0 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 66273 0 None - 0 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 66359 0 None - 0 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 66359 0 None - 0 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
44393911 65224 0 None - 0 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 65224 0 None - 0 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
118720273 115843 0 None - 0 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 115843 0 None - 0 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 115851 0 None - 0 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 115851 0 None - 0 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
118720276 115846 0 None - 0 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 115846 0 None - 0 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
118720261 115832 0 None - 0 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 115832 0 None - 0 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 123833 0 None - 0 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 123833 0 None - 0 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
118720288 115860 0 None - 0 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 115860 0 None - 0 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
118720270 115512 0 None - 0 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 115512 0 None - 0 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
449224 168973 12 None - 1 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 168973 12 None - 1 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 115757 0 None - 0 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 115757 0 None - 0 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 115861 0 None - 0 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 115861 0 None - 0 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
118720287 115859 0 None - 0 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 115859 0 None - 0 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
76073634 115854 3 None - 1 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 115854 3 None - 1 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
118719833 115755 0 None - 0 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 115755 0 None - 0 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 115742 0 None - 0 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 115742 0 None - 0 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
118720279 115849 0 None - 0 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 115849 0 None - 0 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 2228 48 None -10000 5 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 2228 48 None -10000 5 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 2228 48 None -10000 5 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 115763 0 None - 0 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 115763 0 None - 0 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
3537 4002 22 None 3 3 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 4002 22 None 3 3 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 4002 22 None 3 3 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
118719818 115740 0 None - 0 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 115740 0 None - 0 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 115746 0 None - 0 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 115746 0 None - 0 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
118719825 115747 0 None - 0 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 115747 0 None - 0 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 115748 0 None - 0 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 115748 0 None - 0 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
118719844 115766 0 None - 0 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 115766 0 None - 0 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
118720268 115839 0 None - 1 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 115839 0 None - 1 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 115836 0 None - 0 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 115836 0 None - 0 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 115852 0 None - 0 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 115852 0 None - 0 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 115752 0 None - 0 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 115752 0 None - 0 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 115767 0 None - 0 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 115767 0 None - 0 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 170846 0 None - 0 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 170846 0 None - 0 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 115830 0 None - 0 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 115830 0 None - 0 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 115764 0 None - 0 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 115764 0 None - 0 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 115745 0 None - 0 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 115745 0 None - 0 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 115756 0 None - 0 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 115756 0 None - 0 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 115744 0 None - 0 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 115744 0 None - 0 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 2981 58 None -831 8 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 None None None None 10.1021/jm500365s
2174 2981 58 None -831 8 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 None None None None 10.1021/jm500365s
2176 2981 58 None -831 8 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 None None None None 10.1021/jm500365s
439302 2981 58 None -831 8 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 None None None None 10.1021/jm500365s
CHEMBL395429 2981 58 None -831 8 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 None None None None 10.1021/jm500365s
DB00107 2981 58 None -831 8 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 None None None None 10.1021/jm500365s
10411308 201232 0 None 2 3 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 201232 0 None 2 3 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 115835 0 None - 0 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 115835 0 None - 0 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
118720280 115850 0 None - 0 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 115850 0 None - 0 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 115841 0 None - 0 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 115841 0 None - 0 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 115862 0 None - 0 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 115862 0 None - 0 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 115749 0 None - 0 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 115749 0 None - 0 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 115760 0 None - 0 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 115760 0 None - 0 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 115753 0 None - 0 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 115753 0 None - 0 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
118719837 115759 0 None - 0 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 115759 0 None - 0 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 115758 0 None - 0 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 115758 0 None - 0 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 122928 25 None - 2 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 122928 25 None - 2 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 122928 25 None - 2 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 122928 25 None - 2 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 115831 0 None - 0 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 115831 0 None - 0 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 127288 0 None - 0 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 127288 0 None - 0 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 115741 0 None - 0 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 115741 0 None - 0 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 4531 0 None - 0 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 4531 0 None - 0 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 105418 0 None - 0 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 105418 0 None - 0 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 163477 0 None - 0 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 163477 0 None - 0 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 187342 0 None - 0 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 187342 0 None - 0 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 57460 0 None - 0 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 57460 0 None - 0 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 146750 0 None - 0 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 146750 0 None - 0 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 177016 0 None - 0 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 177016 0 None - 0 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 104484 0 None - 0 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 104484 0 None - 0 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 161736 0 None - 0 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 161736 0 None - 0 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 130687 0 None - 0 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 130687 0 None - 0 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 102028 0 None - 0 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 102028 0 None - 0 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 119665 0 None - 0 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 119665 0 None - 0 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 57416 0 None - 0 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 57416 0 None - 0 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 151801 0 None - 0 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 151801 0 None - 0 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 52649 0 None - 0 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 52649 0 None - 0 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 148547 0 None - 0 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 148547 0 None - 0 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 203771 0 None - 0 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 203771 0 None - 0 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 203771 0 None - 0 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 203771 0 None - 0 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 101718 0 None - 0 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 101718 0 None - 0 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 120101 0 None - 0 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 120101 0 None - 0 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 101912 0 None - 0 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 101912 0 None - 0 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 205394 0 None - 0 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 205394 0 None - 0 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 205567 0 None - 0 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 205567 0 None - 0 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 108185 0 None - 0 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 108185 0 None - 0 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 146671 0 None - 0 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 146671 0 None - 0 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 5169 0 None 4 2 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 5169 0 None 4 2 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 60438 0 None - 0 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 60438 0 None - 0 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 60798 0 None - 0 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 60798 0 None - 0 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 61777 0 None - 0 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 61777 0 None - 0 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 131355 0 None - 0 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 131355 0 None - 0 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 204286 0 None - 0 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 204286 0 None - 0 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 115119 0 None - 0 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 115119 0 None - 0 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 151777 0 None - 0 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 151777 0 None - 0 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 128670 0 None - 0 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 128670 0 None - 0 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 132353 0 None - 0 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 132353 0 None - 0 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 12785 0 None - 0 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 12785 0 None - 0 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 14030 0 None - 0 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 14030 0 None - 0 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 89924 0 None - 0 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 89924 0 None - 0 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 90185 0 None - 0 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 90185 0 None - 0 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 119245 0 None - 0 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 119245 0 None - 0 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 18897 0 None - 0 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 18897 0 None - 0 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 18955 0 None - 0 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 18955 0 None - 0 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 19382 0 None - 0 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 19382 0 None - 0 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 21167 0 None - 0 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 21167 0 None - 0 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 21516 0 None - 0 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 21516 0 None - 0 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 116769 0 None - 0 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 116769 0 None - 0 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 117055 0 None - 0 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 117055 0 None - 0 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 168550 0 None - 0 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 168550 0 None - 0 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 98314 0 None - 0 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 98314 0 None - 0 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 209533 0 None - 0 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 None None None 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
10461417 107299 0 None - 0 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 107299 0 None - 0 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 164163 0 None - 0 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 164163 0 None - 0 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 150063 0 None - 0 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 150063 0 None - 0 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 145615 0 None - 0 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 145615 0 None - 0 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 165550 0 None - 0 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 165550 0 None - 0 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 146650 0 None - 0 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 146650 0 None - 0 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 11724 0 None - 0 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 11724 0 None - 0 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
CHEMBL164387 11724 0 None - 0 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 142453 0 None - 0 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 142453 0 None - 0 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 113502 0 None - 0 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 113502 0 None - 0 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 94095 0 None - 0 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 94095 0 None - 0 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 211600 0 None - 0 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 None None None 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 146197 0 None - 0 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 146197 0 None - 0 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 209233 0 None - 2 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 None None None 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 98792 0 None - 0 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 98792 0 None - 0 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 18874 0 None - 0 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 18874 0 None - 0 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 117273 0 None - 0 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 117273 0 None - 0 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 120243 0 None - 1 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 120243 0 None - 1 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 208680 0 None - 0 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 None None None 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 211601 0 None - 0 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 None None None 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 22117 0 None - 0 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 22117 0 None - 0 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 99182 0 None - 0 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 99182 0 None - 0 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
3793 203207 77 None - 1 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
45039617 203207 77 None - 1 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 203207 77 None - 1 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 21380 0 None - 0 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 21380 0 None - 0 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 145895 0 None - 0 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 145895 0 None - 0 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 153726 0 None - 0 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 153726 0 None - 0 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 57512 0 None - 0 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 57512 0 None - 0 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 120036 0 None - 0 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 120036 0 None - 0 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 26537 0 None - 0 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 26537 0 None - 0 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 151793 0 None - 0 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 151793 0 None - 0 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 11721 0 None - 0 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 11721 0 None - 0 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
CHEMBL2370623 209889 0 None - 0 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 None None None 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 18894 0 None - 0 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 18894 0 None - 0 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 21125 0 None - 0 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 21125 0 None - 0 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
10483039 78495 0 None - 0 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 78495 0 None - 0 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
44433360 89447 0 None - 0 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 89447 0 None - 0 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
3793 203207 77 None - 1 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
45039617 203207 77 None - 1 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 203207 77 None - 1 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 151624 0 None - 0 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 151624 0 None - 0 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 147035 0 None - 0 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 147035 0 None - 0 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 13912 0 None - 0 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 13912 0 None - 0 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 110377 0 None - 0 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 110377 0 None - 0 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 57448 0 None - 0 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 57448 0 None - 0 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 102531 0 None - 0 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 102531 0 None - 0 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 102734 0 None - 0 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 102734 0 None - 0 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 26588 0 None - 0 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 26588 0 None - 0 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 116008 0 None - 0 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 116008 0 None - 0 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 107468 0 None 1 2 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 107468 0 None 1 2 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 78869 0 None - 0 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 78869 0 None - 0 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 120036 0 None - 0 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 120036 0 None - 0 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 209232 0 None - 0 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 None None None 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
9805972 98613 0 None - 0 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 98613 0 None - 0 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 162945 0 None - 0 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 162945 0 None - 0 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 18968 0 None - 0 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 18968 0 None - 0 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
44352150 18863 0 None - 0 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 18863 0 None - 0 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
10413998 19046 0 None - 0 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 19046 0 None - 0 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
44352299 116801 0 None - 0 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 116801 0 None - 0 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 116925 0 None - 0 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 116925 0 None - 0 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 117489 0 None - 0 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 117489 0 None - 0 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 112986 0 None - 0 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 112986 0 None - 0 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 114058 0 None - 0 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 114058 0 None - 0 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 120041 0 None - 0 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 120041 0 None - 0 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 204610 0 None - 0 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 204610 0 None - 0 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 154801 0 None - 0 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 154801 0 None - 0 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 203898 0 None - 0 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 203898 0 None - 0 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 204610 0 None - 0 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 204610 0 None - 0 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 56677 0 None - 0 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 56677 0 None - 0 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 13959 0 None - 0 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 13959 0 None - 0 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 56145 0 None - 0 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 56145 0 None - 0 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 113509 0 None - 0 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 113509 0 None - 0 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
CHEMBL338294 211604 0 None - 0 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 None None None 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 118464 0 None - 0 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 118464 0 None - 0 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 118552 0 None - 0 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 118552 0 None - 0 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 164331 0 None - 0 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 164331 0 None - 0 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 18957 0 None - 0 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 18957 0 None - 0 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 160765 0 None - 0 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 160765 0 None - 0 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 57299 0 None - 0 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 57299 0 None - 0 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 102221 0 None - 0 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 102221 0 None - 0 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 108000 0 None - 1 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 108000 0 None - 1 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 118179 0 None - 0 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 118179 0 None - 0 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 118179 0 None - 0 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 118179 0 None - 0 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 150923 0 None - 0 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 150923 0 None - 0 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 13847 0 None - 0 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 13847 0 None - 0 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 119929 0 None - 0 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 119929 0 None - 0 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 211630 0 None - 0 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 None None None 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 99604 0 None - 0 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 99604 0 None - 0 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 117019 0 None - 0 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 117019 0 None - 0 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 118464 0 None - 0 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 118464 0 None - 0 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 133558 0 None - 0 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 133558 0 None - 0 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 21484 0 None - 0 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 21484 0 None - 0 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 116646 0 None - 0 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 116646 0 None - 0 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 4777 101 None - 34 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 4777 101 None - 34 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
5280343 188273 124 None -147 32 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
CHEMBL1520590 188273 124 None -147 32 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 188273 124 None -147 32 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 188273 124 None -147 32 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
CHEMBL1520590 188273 124 None -147 32 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 188273 124 None -147 32 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 4777 101 None - 34 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 4777 101 None - 34 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 4243 0 None - 0 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 4243 0 None - 0 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 115254 0 None - 0 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 115254 0 None - 0 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 109206 0 None - 0 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 109206 0 None - 0 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 153176 0 None - 0 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 153176 0 None - 0 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 104727 0 None - 0 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 104727 0 None - 0 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 27185 0 None - 0 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 27185 0 None - 0 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 188081 0 None - 0 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 188081 0 None - 0 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 78867 0 None - 0 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 78867 0 None - 0 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 11873 1 None - 0 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 11873 1 None - 0 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 211606 0 None - 2 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 None None None 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 21448 0 None - 0 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 21448 0 None - 0 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 117043 0 None - 0 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 117043 0 None - 0 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 98617 0 None - 0 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 98617 0 None - 0 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 114536 0 None - 0 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 114536 0 None - 0 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 119989 0 None - 0 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 119989 0 None - 0 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 150775 0 None - 0 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 150775 0 None - 0 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 114797 0 None - 0 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 114797 0 None - 0 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 204280 0 None - 0 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 204280 0 None - 0 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 212552 0 None - 0 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 None None None 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 96816 0 None - 0 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 96816 0 None - 0 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 117025 0 None - 0 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 117025 0 None - 0 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 168449 0 None - 0 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 168449 0 None - 0 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 74177 0 None - 0 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 74177 0 None - 0 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 2222 5 None - 2 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 2222 5 None - 2 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 2222 5 None - 2 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
44336768 163350 0 None - 0 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 163350 0 None - 0 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 14106 0 None - 3 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 14106 0 None - 3 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 115125 0 None - 0 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 115125 0 None - 0 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 94275 0 None - 0 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 94275 0 None - 0 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 26660 0 None - 0 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 26660 0 None - 0 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 119297 0 None - 0 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 119297 0 None - 0 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 113801 0 None - 0 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 113801 0 None - 0 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 119889 0 None - 0 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 119889 0 None - 0 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 4319 0 None - 0 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 4319 0 None - 0 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 119423 7 None - 1 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 119423 7 None - 1 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 13760 0 None - 0 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 13760 0 None - 0 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 18867 0 None - 0 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 18867 0 None - 0 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 116863 0 None - 0 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 116863 0 None - 0 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 75049 0 None - 0 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 75049 0 None - 0 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 53155 0 None - 0 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 53155 0 None - 0 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 101404 0 None - 0 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 101404 0 None - 0 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 115226 0 None - 0 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 115226 0 None - 0 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 107488 0 None - 0 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 107488 0 None - 0 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 12873 0 None - 0 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 12873 0 None - 0 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 57532 0 None - 0 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 57532 0 None - 0 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 13789 0 None - 0 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 13789 0 None - 0 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 116943 0 None - 0 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 116943 0 None - 0 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 118043 0 None - 0 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 118043 0 None - 0 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 209241 0 None - 0 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 None None None 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 149869 0 None - 0 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 149869 0 None - 0 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 145191 0 None - 0 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 145191 0 None - 0 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 151679 0 None - 0 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 151679 0 None - 0 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 104894 0 None - 0 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 104894 0 None - 0 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 105448 0 None - 0 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 105448 0 None - 0 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 120089 0 None - 0 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 120089 0 None - 0 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 132573 0 None - 0 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 132573 0 None - 0 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 205555 0 None - 0 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 205555 0 None - 0 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 57406 0 None - 0 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 57406 0 None - 0 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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
172997 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 2330 57 None - 2 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 53148 0 None - 0 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 53148 0 None - 0 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 119907 0 None - 0 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 119907 0 None - 0 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 52649 0 None - 0 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 52649 0 None - 0 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
44352776 21593 0 None - 0 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 21593 0 None - 0 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 110957 0 None - 0 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 110957 0 None - 0 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 13462 0 None - 0 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 13462 0 None - 0 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 57460 0 None - 0 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 57460 0 None - 0 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 130686 0 None - 0 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 130686 0 None - 0 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 131347 0 None - 0 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 131347 0 None - 0 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 168500 0 None - 0 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 168500 0 None - 0 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 60438 0 None - 0 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 60438 0 None - 0 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 167589 0 None - 0 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 167589 0 None - 0 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 15380 0 None - 0 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 15380 0 None - 0 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 113062 0 None - 0 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 113062 0 None - 0 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 60437 0 None - 0 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 60437 0 None - 0 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 169294 0 None - 0 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 169294 0 None - 0 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 60798 0 None - 0 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 60798 0 None - 0 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 209532 0 None - 0 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 None None None 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 72473 0 None - 0 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 72473 0 None - 0 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 118464 0 None - 0 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 118464 0 None - 0 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 21120 0 None - 0 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 21120 0 None - 0 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
18917500 187443 0 None - 0 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 187443 0 None - 0 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 11031 0 None - 0 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 11031 0 None - 0 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 57384 0 None - 0 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 57384 0 None - 0 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 115424 0 None - 0 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 115424 0 None - 0 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 13633 0 None - 0 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 13633 0 None - 0 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 18961 0 None - 0 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 18961 0 None - 0 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 20709 0 None - 0 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 20709 0 None - 0 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 116901 0 None - 0 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 116901 0 None - 0 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 18902 0 None - 0 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 18902 0 None - 0 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 143716 0 None - 0 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 143716 0 None - 0 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 12853 0 None - 0 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 12853 0 None - 0 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 204286 0 None - 0 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 204286 0 None - 0 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 30629 0 None - 0 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 30629 0 None - 0 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 120167 0 None - 0 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 120167 0 None - 0 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 22318 0 None - 0 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 22318 0 None - 0 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 13427 5 None - 0 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 13427 5 None - 0 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 107415 0 None - 0 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 107415 0 None - 0 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 145540 0 None - 0 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 145540 0 None - 0 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 149076 0 None - 0 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 149076 0 None - 0 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 151864 0 None - 0 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 151864 0 None - 0 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
2173 2954 13 None - 2 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 2954 13 None - 2 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 2954 13 None - 2 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 2954 13 None - 2 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 53374 0 None - 0 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 53374 0 None - 0 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 78875 0 None - 0 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 78875 0 None - 0 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 2216 1 None -208 4 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 None None None None 10.1021/jm00099a019
9810632 2216 1 None -208 4 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 None None None None 10.1021/jm00099a019
CHEMBL127686 2216 1 None -208 4 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 None None None None 10.1021/jm00099a019
44273425 98901 0 None - 0 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 98901 0 None - 0 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
44273369 99542 0 None - 0 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 99542 0 None - 0 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 98598 0 None - 0 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 98598 0 None - 0 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 120167 0 None - 0 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 120167 0 None - 0 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 110416 0 None - 0 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 110416 0 None - 0 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 187895 0 None - 0 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 187895 0 None - 0 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 78876 0 None - 0 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 78876 0 None - 0 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 78877 0 None - 0 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 78877 0 None - 0 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 78780 0 None - 0 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 78780 0 None - 0 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 155684 0 None - 0 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 155684 0 None - 0 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
2168 3974 38 None -15 9 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 None None None None 10.1016/j.bmcl.2012.12.041
2810 3974 38 None -15 9 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 None None None None 10.1016/j.bmcl.2012.12.041
644077 3974 38 None -15 9 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 None None None None 10.1016/j.bmcl.2012.12.041
CHEMBL373742 3974 38 None -15 9 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 None None None None 10.1016/j.bmcl.2012.12.041
DB00067 3974 38 None -15 9 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 None None None None 10.1016/j.bmcl.2012.12.041
10647295 110272 0 None - 0 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 110272 0 None - 0 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 103673 0 None - 0 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 103673 0 None - 0 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 13164 0 None - 0 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 13164 0 None - 0 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 135337 0 None - 0 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 135337 0 None - 0 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 72782 0 None - 0 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 72782 0 None - 0 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 116693 0 None - 0 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 116693 0 None - 0 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 168628 0 None - 0 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 168628 0 None - 0 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 4777 101 None - 34 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 4777 101 None - 34 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
44335386 108008 0 None 14 2 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 108008 0 None 14 2 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 20814 0 None - 0 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 20814 0 None - 0 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 116690 0 None - 0 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 116690 0 None - 0 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 144778 0 None - 0 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 144778 0 None - 0 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 11918 0 None - 0 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 11918 0 None - 0 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 114913 0 None - 0 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 114913 0 None - 0 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 78871 0 None - 0 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 78871 0 None - 0 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 117051 0 None - 0 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 117051 0 None - 0 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 4777 101 None - 34 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 4777 101 None - 34 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 107260 0 None - 0 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 107260 0 None - 0 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 152941 0 None - 0 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 152941 0 None - 0 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 14128 0 None - 0 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 14128 0 None - 0 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 5223 0 None 5 2 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 5223 0 None 5 2 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 21403 0 None - 0 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 21403 0 None - 0 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 71719 0 None - 0 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 71719 0 None - 0 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 11920 0 None - 2 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 11920 0 None - 2 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 12084 0 None - 0 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 12084 0 None - 0 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 12939 0 None - 0 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 12939 0 None - 0 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 113063 0 None - 0 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 113063 0 None - 0 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 101337 0 None - 0 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 101337 0 None - 0 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 4449 0 None - 0 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 4449 0 None - 0 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 204279 1 None - 0 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 204279 1 None - 0 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 204555 0 None - 0 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 204555 0 None - 0 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 187345 0 None - 0 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 187345 0 None - 0 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 78870 0 None - 1 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 78870 0 None - 1 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 117272 0 None - 0 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 117272 0 None - 0 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 75291 0 None - 0 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 75291 0 None - 0 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 147938 0 None - 0 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 147938 0 None - 0 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 101506 0 None - 0 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 101506 0 None - 0 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 163307 0 None - 0 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 163307 0 None - 0 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 131355 0 None - 0 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 131355 0 None - 0 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 167589 0 None - 0 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 167589 0 None - 0 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 163307 0 None - 0 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 163307 0 None - 0 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 163307 0 None - 0 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 163307 0 None - 0 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 53179 0 None - 0 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 53179 0 None - 0 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 163307 0 None - 0 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 163307 0 None - 0 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 163307 0 None - 0 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 163307 0 None - 0 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 150627 0 None - 0 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 150627 0 None - 0 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
2168 3974 38 None - 9 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 None None None None 10.1016/S0960-894X(97)00050-4
2810 3974 38 None - 9 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 None None None None 10.1016/S0960-894X(97)00050-4
644077 3974 38 None - 9 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 None None None None 10.1016/S0960-894X(97)00050-4
CHEMBL373742 3974 38 None - 9 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 None None None None 10.1016/S0960-894X(97)00050-4
DB00067 3974 38 None - 9 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 None None None None 10.1016/S0960-894X(97)00050-4
44374802 120001 0 None - 0 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 120001 0 None - 0 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 109195 0 None - 0 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 109195 0 None - 0 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 60429 0 None - 0 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 60429 0 None - 0 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 60559 0 None - 0 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 60559 0 None - 0 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 60559 0 None - 0 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 60559 0 None - 0 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 130686 0 None - 0 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 130686 0 None - 0 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 131347 0 None - 0 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 131347 0 None - 0 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 144536 0 None - 0 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 144536 0 None - 0 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 114381 0 None - 0 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 114381 0 None - 0 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 165748 0 None - 0 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 165748 0 None - 0 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 60469 0 None - 0 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 60469 0 None - 0 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
44273426 77104 0 None - 0 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 77104 0 None - 0 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 18950 0 None - 0 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 18950 0 None - 0 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 20640 0 None - 0 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 20640 0 None - 0 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 22118 0 None - 0 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 22118 0 None - 0 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 78777 0 None - 0 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 78777 0 None - 0 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 116811 0 None - 0 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 116811 0 None - 0 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 168448 0 None - 0 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 168448 0 None - 0 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 73518 0 None - 0 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 73518 0 None - 0 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 28386 0 None - 0 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 28386 0 None - 0 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 78868 0 None - 0 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 78868 0 None - 0 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 60532 0 None - 0 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 60532 0 None - 0 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 208904 0 None - 2 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 None None None 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 154270 0 None - 0 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 154270 0 None - 0 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 164036 0 None - 0 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 164036 0 None - 0 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
10591515 118881 0 None - 0 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 118881 0 None - 0 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 18892 0 None - 0 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 18892 0 None - 0 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 189819 0 None - 0 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 189819 0 None - 0 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 102254 0 None - 0 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 102254 0 None - 0 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 2954 13 None 8 2 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 2954 13 None 8 2 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 2954 13 None 8 2 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 2954 13 None 8 2 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 208666 0 None - 0 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 None None None 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 117272 0 None - 0 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 117272 0 None - 0 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 89845 0 None - 0 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 89845 0 None - 0 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 94193 7 None - 0 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 94193 7 None - 0 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 24860 0 None - 0 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 24860 0 None - 0 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 56145 0 None - 0 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 56145 0 None - 0 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 163461 0 None - 0 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 163461 0 None - 0 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 63036 1 None - 0 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 63036 1 None - 0 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 169448 0 None - 0 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 169448 0 None - 0 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 116672 0 None - 0 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 116672 0 None - 0 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 78872 0 None - 0 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 78872 0 None - 0 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 90678 1 None - 4 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 90678 1 None - 4 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 150479 0 None - 0 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 150479 0 None - 0 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 120204 0 None - 0 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 120204 0 None - 0 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 20688 0 None - 0 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 20688 0 None - 0 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
5280343 188273 124 None -147 32 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
CHEMBL1520590 188273 124 None -147 32 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 188273 124 None -147 32 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 119929 0 None - 0 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 119929 0 None - 0 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 168391 0 None - 0 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 168391 0 None - 0 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 107237 0 None - 0 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 107237 0 None - 0 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 61005 0 None - 0 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 61005 0 None - 0 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 211615 0 None -19 2 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 None None None 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 19559 0 None - 0 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 19559 0 None - 0 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 4965 0 None - 0 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 4965 0 None - 0 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 5365 0 None - 0 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 5365 0 None - 0 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 17785 1 None - 0 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 17785 1 None - 0 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 140718 0 None - 0 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 140718 0 None - 0 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 4483 0 None - 0 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 4483 0 None - 0 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 140571 0 None - 0 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 140571 0 None - 0 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
44273316 98869 0 None - 0 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 98869 0 None - 0 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 87005 0 None - 0 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 87005 0 None - 0 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
5280343 188273 124 None -147 32 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
CHEMBL1520590 188273 124 None -147 32 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 188273 124 None -147 32 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 188107 0 None - 0 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 188107 0 None - 0 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 103022 0 None - 0 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 103022 0 None - 0 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 205630 0 None - 0 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 205630 0 None - 0 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 119897 0 None - 0 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 119897 0 None - 0 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 204232 0 None - 0 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 204232 0 None - 0 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 101910 4 None - 0 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 101910 4 None - 0 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 103022 0 None - 0 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 103022 0 None - 0 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 204232 0 None - 0 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 204232 0 None - 0 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 204377 0 None - 0 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 204377 0 None - 0 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 4952 0 None - 0 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 4952 0 None - 0 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 169521 0 None 14 2 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 169521 0 None 14 2 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 62304 0 None - 0 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 62304 0 None - 0 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 204377 0 None - 0 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 204377 0 None - 0 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 115125 0 None - 0 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 115125 0 None - 0 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 163502 0 None - 0 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 163502 0 None - 0 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
44293778 101618 0 None - 0 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 101618 0 None - 0 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 145027 0 None - 0 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 145027 0 None - 0 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 104484 0 None - 0 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 104484 0 None - 0 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 142369 0 None - 0 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 142369 0 None - 0 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 102171 0 None - 0 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 102171 0 None - 0 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
86690918 151818 0 None - 0 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 151818 0 None - 0 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 147915 0 None - 0 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 147915 0 None - 0 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 12382 0 None - 0 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 12382 0 None - 0 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 12814 0 None - 0 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 12814 0 None - 0 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 87005 0 None - 0 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 87005 0 None - 0 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 12433 12 None - 0 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 12433 12 None - 0 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 213239 0 None - 0 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 None None None 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 10514 0 None - 0 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 10514 0 None - 0 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 73263 0 None - 0 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 73263 0 None - 0 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 116938 0 None - 0 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 116938 0 None - 0 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 140344 0 None - 0 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 140344 0 None - 0 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 204226 0 None - 0 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 204226 0 None - 0 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 12521 7 None - 0 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 12521 7 None - 0 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 18914 0 None - 0 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 18914 0 None - 0 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 18956 0 None - 0 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 18956 0 None - 0 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 208905 0 None - 0 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 None None None 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 10159 0 None - 0 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 10159 0 None - 0 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 120150 0 None - 0 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 120150 0 None - 0 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 154802 0 None - 0 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 154802 0 None - 0 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 172628 0 None - 0 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 172628 0 None - 0 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 202129 0 None - 0 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 202129 0 None - 0 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 63036 1 None - 0 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 63036 1 None - 0 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 149125 0 None - 0 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 149125 0 None - 0 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 117278 0 None - 0 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 117278 0 None - 0 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 21462 0 None - 0 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 21462 0 None - 0 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 87005 0 None - 0 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 87005 0 None - 0 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 180931 0 None - 0 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 180931 0 None - 0 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 168577 0 None - 0 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 168577 0 None - 0 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 18903 0 None - 0 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 18903 0 None - 0 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 75916 0 None - 0 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 75916 0 None - 0 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 148410 0 None - 0 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 148410 0 None - 0 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 101313 1 None - 0 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 101313 1 None - 0 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 116804 0 None - 0 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 116804 0 None - 0 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 116973 0 None - 0 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 116973 0 None - 0 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
44352374 18525 0 None - 0 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 18525 0 None - 0 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 73858 0 None - 0 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 73858 0 None - 0 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 149553 0 None - 0 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 149553 0 None - 0 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 151843 0 None - 0 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 151843 0 None - 0 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 102734 0 None - 0 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 102734 0 None - 0 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 63035 0 None - 0 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 63035 0 None - 0 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 102171 0 None - 0 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 102171 0 None - 0 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 119298 0 None - 0 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 119298 0 None - 0 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 2330 57 None 64 2 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 167836 0 None 1 2 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 167836 0 None 1 2 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 60532 0 None - 0 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 60532 0 None - 0 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 120221 0 None - 0 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 120221 0 None - 0 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 152127 0 None - 0 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 152127 0 None - 0 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 27207 0 None - 0 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 27207 0 None - 0 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 12451 0 None - 0 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 12451 0 None - 0 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 57531 0 None - 0 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 57531 0 None - 0 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 62104 0 None - 0 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 62104 0 None - 0 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 61777 0 None - 0 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 61777 0 None - 0 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 62104 0 None - 0 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 62104 0 None - 0 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 204347 0 None - 0 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 204347 0 None - 0 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 87005 0 None - 0 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 87005 0 None - 0 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 27381 0 None - 0 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 27381 0 None - 0 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 72038 0 None - 0 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 72038 0 None - 0 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 78873 0 None - 0 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 78873 0 None - 0 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
10256467 20505 0 None - 0 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 20505 0 None - 0 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 115219 0 None - 0 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 115219 0 None - 0 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 115497 0 None - 0 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 115497 0 None - 0 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 122611 0 None - 0 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 122611 0 None - 0 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 208904 0 None - 2 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 None None None 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 117056 0 None - 0 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 117056 0 None - 0 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
11432362 94135 0 None - 0 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 94135 0 None - 0 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 114260 0 None - 0 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 114260 0 None - 0 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 204465 0 None - 0 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 204465 0 None - 0 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 116812 0 None - 0 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 116812 0 None - 0 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 118097 0 None - 0 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 118097 0 None - 0 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 167959 0 None - 0 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 167959 0 None - 0 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 167500 0 None - 0 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 167500 0 None - 0 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 120077 0 None - 0 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 120077 0 None - 0 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 4364 0 None - 0 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 4364 0 None - 0 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 116340 0 None - 0 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 116340 0 None - 0 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 116523 0 None - 0 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 116523 0 None - 0 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 117950 0 None - 0 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 117950 0 None - 0 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 118469 0 None - 0 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 118469 0 None - 0 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
10437668 78878 1 None - 2 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 78878 1 None - 2 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 168238 0 None - 0 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 168238 0 None - 0 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 2225 18 None -54 6 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 2225 18 None -54 6 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 2225 18 None -54 6 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 11814 0 None - 0 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 11814 0 None - 0 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 71780 0 None - 0 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 71780 0 None - 0 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
9805201 56255 0 None - 0 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 56255 0 None - 0 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 107353 0 None - 0 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 107353 0 None - 0 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 129648 0 None - 0 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 129648 0 None - 0 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 161736 0 None - 0 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 161736 0 None - 0 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
10390899 186721 0 None - 0 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 186721 0 None - 0 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 60429 0 None - 0 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 60429 0 None - 0 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 61005 0 None - 0 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 61005 0 None - 0 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 118275 0 None - 0 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 118275 0 None - 0 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
3793 203207 77 None - 1 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
45039617 203207 77 None - 1 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 203207 77 None - 1 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 114104 0 None - 0 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 114104 0 None - 0 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 116854 0 None - 0 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 116854 0 None - 0 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 99468 0 None - 0 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 99468 0 None - 0 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 117012 0 None - 0 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 117012 0 None - 0 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 22062 0 None - 0 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 22062 0 None - 0 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 22321 0 None - 0 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 22321 0 None - 0 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
5280343 188273 124 None -147 32 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
CHEMBL1520590 188273 124 None -147 32 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 188273 124 None -147 32 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
3793 203207 77 None - 1 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
45039617 203207 77 None - 1 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 203207 77 None - 1 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 110645 0 None - 0 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 110645 0 None - 0 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 12889 6 None - 0 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 12889 6 None - 0 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 117362 0 None - 0 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 117362 0 None - 0 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 113331 7 None - 0 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 113331 7 None - 0 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 116063 0 None - 0 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 116063 0 None - 0 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 117050 0 None - 0 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 117050 0 None - 0 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 203767 0 None - 0 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 203767 0 None - 0 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 20695 0 None - 0 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 20695 0 None - 0 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 116927 0 None - 0 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 116927 0 None - 0 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 149713 0 None - 0 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 149713 0 None - 0 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 4689 0 None - 0 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 4689 0 None - 0 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
10393965 22054 0 None - 0 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 22054 0 None - 0 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 118089 0 None - 0 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 118089 0 None - 0 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
15307968 103053 0 None - 0 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 103053 0 None - 0 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 11843 0 None - 0 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 11843 0 None - 0 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 18965 0 None - 0 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 18965 0 None - 0 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 120002 0 None - 0 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 120002 0 None - 0 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 213659 2 None - 2 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 None None None 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 117009 0 None - 0 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 117009 0 None - 0 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 118452 0 None - 0 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 118452 0 None - 0 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 120105 0 None - 0 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 120105 0 None - 0 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 204292 0 None - 0 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 204292 0 None - 0 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 108590 0 None 4 2 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 108590 0 None 4 2 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 130687 0 None - 0 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 130687 0 None - 0 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 101837 0 None - 0 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 101837 0 None - 0 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 165544 0 None - 0 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 165544 0 None - 0 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 118880 0 None - 0 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 118880 0 None - 0 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
67409800 146896 0 None - 0 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 146896 0 None - 0 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 152417 0 None - 0 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 152417 0 None - 0 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 114423 0 None - 0 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 114423 0 None - 0 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 169115 0 None - 0 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 169115 0 None - 0 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 128647 0 None - 0 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 128647 0 None - 0 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
5280343 188273 124 None -147 32 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
CHEMBL1520590 188273 124 None -147 32 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 188273 124 None -147 32 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 118475 4 None -77 6 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 118475 4 None -77 6 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 114530 0 None - 0 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 114530 0 None - 0 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 168906 0 None - 0 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 168906 0 None - 0 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 120002 0 None - 0 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 120002 0 None - 0 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 10087 12 None - 0 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 10087 12 None - 0 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 99023 0 None - 0 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 99023 0 None - 0 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 167996 0 None - 0 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 167996 0 None - 0 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 209235 0 None - 0 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 None None None 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 99046 0 None - 0 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 99046 0 None - 0 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 167882 0 None - 0 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 167882 0 None - 0 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 117368 0 None - 0 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 117368 0 None - 0 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 209242 0 None - 0 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 None None None 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 117215 0 None - 0 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 117215 0 None - 0 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 118227 0 None - 0 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 118227 0 None - 0 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 209240 0 None - 0 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 None None None 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
10369550 118474 0 None - 0 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 118474 0 None - 0 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 154617 0 None - 0 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 154617 0 None - 0 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 113131 0 None - 0 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 113131 0 None - 0 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 12953 0 None - 0 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 12953 0 None - 0 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 114810 0 None - 0 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 114810 0 None - 0 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 103808 0 None - 0 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 103808 0 None - 0 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 203310 0 None - 0 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 203310 0 None - 0 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 12706 0 None - 0 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 12706 0 None - 0 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 21539 0 None - 0 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 21539 0 None - 0 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
3793 203207 77 None - 1 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
45039617 203207 77 None - 1 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 203207 77 None - 1 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 116619 0 None - 0 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 116619 0 None - 0 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 116779 0 None - 0 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 116779 0 None - 0 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 4965 0 None - 0 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 4965 0 None - 0 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 63035 0 None - 0 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 63035 0 None - 0 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 151747 0 None - 0 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 151747 0 None - 0 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 120056 0 None - 0 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 120056 0 None - 0 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 205700 0 None - 0 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 205700 0 None - 0 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 154727 0 None - 0 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 154727 0 None - 0 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 61772 0 None - 0 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 61772 0 None - 0 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 62304 0 None - 0 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 62304 0 None - 0 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 150409 0 None - 0 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 150409 0 None - 0 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 101460 0 None - 0 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 101460 0 None - 0 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 106682 0 None - 0 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 106682 0 None - 0 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 104894 0 None - 0 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 104894 0 None - 0 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 149027 0 None - 0 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 149027 0 None - 0 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 146133 0 None - 0 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 146133 0 None - 0 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 168636 0 None - 0 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 168636 0 None - 0 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 30976 1 None - 0 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 30976 1 None - 0 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 4002 22 None 3 3 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 4002 22 None 3 3 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 4002 22 None 3 3 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 61772 0 None - 0 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 61772 0 None - 0 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 128647 0 None - 0 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 128647 0 None - 0 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 168500 0 None - 0 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 168500 0 None - 0 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 4002 22 None 3 3 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 4002 22 None 3 3 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 4002 22 None 3 3 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
3793 203207 77 None - 1 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
45039617 203207 77 None - 1 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 203207 77 None - 1 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 100806 0 None - 0 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 100806 0 None - 0 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 209234 1 None - 2 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 None None None 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 116437 0 None - 0 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 116437 0 None - 0 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 110504 9 None - 0 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 110504 9 None - 0 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 215703 0 None -23 2 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 None None None 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 13934 0 None - 0 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 13934 0 None - 0 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 200550 0 None - 0 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 200550 0 None - 0 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
44273417 99505 0 None - 0 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 99505 0 None - 0 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 18869 0 None - 0 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 18869 0 None - 0 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 21474 0 None - 0 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 21474 0 None - 0 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 102289 0 None - 0 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 102289 0 None - 0 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 204360 0 None - 0 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 204360 0 None - 0 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 168519 0 None - 0 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 168519 0 None - 0 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 73925 0 None - 0 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 73925 0 None - 0 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 22117 0 None - 0 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 22117 0 None - 0 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 74945 0 None - 0 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 74945 0 None - 0 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 118179 0 None - 0 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 118179 0 None - 0 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 144880 0 None - 0 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 144880 0 None - 0 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 101095 0 None - 0 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 101095 0 None - 0 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 118179 0 None - 0 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 118179 0 None - 0 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 129648 0 None - 0 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 129648 0 None - 0 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 97092 0 None - 0 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 97092 0 None - 0 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 74352 0 None - 0 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 74352 0 None - 0 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 209234 1 None - 2 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 None None None 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
11261339 154618 0 None - 0 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 154618 0 None - 0 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 21323 0 None - 0 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 21323 0 None - 0 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 116955 0 None - 0 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 116955 0 None - 0 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 73940 0 None - 0 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 73940 0 None - 0 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 118385 0 None - 0 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 118385 0 None - 0 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 22446 0 None - 0 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 22446 0 None - 0 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 14568 0 None - 0 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 14568 0 None - 0 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 140274 0 None - 0 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 140274 0 None - 0 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 18886 0 None - 0 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 18886 0 None - 0 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 17785 1 None - 0 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 17785 1 None - 0 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 114390 9 None - 0 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 114390 9 None - 0 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 82373 0 None 64 3 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 82373 0 None 64 3 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 82373 0 None 64 3 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 156092 0 None - 1 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 156092 0 None - 1 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
2168 3974 38 None -4 9 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 None None None None 10.1016/s0960-894x(99)00041-4
2810 3974 38 None -4 9 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 None None None None 10.1016/s0960-894x(99)00041-4
644077 3974 38 None -4 9 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 None None None None 10.1016/s0960-894x(99)00041-4
CHEMBL373742 3974 38 None -4 9 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 None None None None 10.1016/s0960-894x(99)00041-4
DB00067 3974 38 None -4 9 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 None None None None 10.1016/s0960-894x(99)00041-4
2168 3974 38 None -7 9 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 None None None None 10.1021/jm00028a008
2810 3974 38 None -7 9 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 None None None None 10.1021/jm00028a008
644077 3974 38 None -7 9 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 None None None None 10.1021/jm00028a008
CHEMBL373742 3974 38 None -7 9 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 None None None None 10.1021/jm00028a008
DB00067 3974 38 None -7 9 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 None None None None 10.1021/jm00028a008
CHEMBL265119 210634 0 None - 1 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 None None None 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 79690 0 None -257 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 79690 0 None -257 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
118718752 115389 0 None -26 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 115389 0 None -26 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 82372 0 None 38 2 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 82372 0 None 38 2 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 213080 0 None - 1 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 None None None 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 115391 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 115391 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 160773 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 160773 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 118590 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 118590 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 209885 0 None -3 3 Rat 7.8 pKd = 7.8 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL None None None 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 63328 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 63328 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 82374 0 None 234 3 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 82374 0 None 234 3 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 82374 0 None 234 3 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 82375 0 None - 1 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 82375 0 None - 1 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 82375 0 None - 1 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 210800 0 None - 1 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 None None None 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 78354 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 78354 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 141465 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 141465 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 96842 0 None - 1 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 96842 0 None - 1 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 209970 10 None -3 3 Rat 7.6 pKd = 7.6 Binding
Antidiuretic activity at V2 receptorAntidiuretic activity at V2 receptor
ChEMBL None None None 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
118718751 115388 0 None -213 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 115388 0 None -213 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 168892 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 168892 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 96716 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 96716 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 118591 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 118591 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 161833 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 161833 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 115343 0 None -173 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 115343 0 None -173 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 115344 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 115344 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 115347 1 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 115347 1 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 168803 0 None - 1 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 168803 0 None - 1 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 161904 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 161904 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 167711 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
CHEMBL3416754 167711 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 167711 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 115346 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 115346 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 51171 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 51171 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 206383 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 206383 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 212794 0 None - 1 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 None None None 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 115386 0 None -5 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 115386 0 None -5 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 155699 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 155699 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 167655 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
CHEMBL3416753 167655 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 167655 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 160696 0 None - 1 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 160696 0 None - 1 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 78368 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 78368 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 115390 0 None -2 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 115390 0 None -2 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 97010 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 97010 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 161682 0 None - 1 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 161682 0 None - 1 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 112560 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 112560 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
CHEMBL217517 209374 0 None - 1 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 None None None 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
CHEMBL2371674 210105 0 None - 1 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 None None None 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
44321206 96801 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 96801 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 137394 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 137394 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
44419026 168497 17 None 1230 2 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 168497 17 None 1230 2 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
2181 1330 42 None 6 7 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 None None None None 10.1021/jm060928n
2182 1330 42 None 6 7 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 None None None None 10.1021/jm060928n
27991 1330 42 None 6 7 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 None None None None 10.1021/jm060928n
5311065 1330 42 None 6 7 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 None None None None 10.1021/jm060928n
CHEMBL1429 1330 42 None 6 7 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 None None None None 10.1021/jm060928n
CHEMBL264448 1330 42 None 6 7 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 None None None None 10.1021/jm060928n
DB00035 1330 42 None 6 7 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 None None None None 10.1021/jm060928n
44419025 84294 0 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 84294 0 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
151171 1163 50 None -1 6 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
216322 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 188817 0 None - 1 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 188817 0 None - 1 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 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
443894 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
2168 3974 38 None -4 9 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 None None None None 10.1021/jm060928n
2810 3974 38 None -4 9 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 None None None None 10.1021/jm060928n
644077 3974 38 None -4 9 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 None None None None 10.1021/jm060928n
CHEMBL373742 3974 38 None -4 9 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 None None None None 10.1021/jm060928n
DB00067 3974 38 None -4 9 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 None None None None 10.1021/jm060928n
CHEMBL2371605 210103 0 None - 1 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 None None None 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
10411308 201232 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 201232 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 201232 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 201232 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 201232 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 201232 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
135413562 2203 15 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 2203 15 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 2203 15 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 210102 0 None - 1 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 None None None 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
2205 4121 6 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 4121 6 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 4121 6 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
16051933 138128 4 None -3 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
CHEMBL376685 138128 4 None -3 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 138128 4 None -3 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 82375 0 None - 1 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 82375 0 None - 1 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 82375 0 None - 1 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
2198 3418 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 3418 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 3418 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 96491 0 None - 1 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 96491 0 None - 1 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
44375638 168846 0 None 6 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 168846 0 None 6 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 210984 0 None - 1 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 None None None 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 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
443894 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
44382370 141548 0 None 3 2 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(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(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
CHEMBL384776 141548 0 None 3 2 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(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(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
2205 4121 6 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 4121 6 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 4121 6 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 4121 6 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 4121 6 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 4121 6 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 84294 0 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 84294 0 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
2168 3974 38 None -15 9 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 None None None None 10.1021/jm1016208
2810 3974 38 None -15 9 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 None None None None 10.1021/jm1016208
644077 3974 38 None -15 9 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 None None None None 10.1021/jm1016208
CHEMBL373742 3974 38 None -15 9 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 None None None None 10.1021/jm1016208
DB00067 3974 38 None -15 9 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 None None None None 10.1021/jm1016208
CHEMBL408474 212713 0 None - 1 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 None None None 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
2168 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
2810 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
644077 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
CHEMBL373742 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
DB00067 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
44325703 111401 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 111401 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
2168 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
2810 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
644077 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
CHEMBL373742 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
DB00067 3974 38 None -15 9 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 None None None None 10.1021/jm3006146
CHEMBL2369831 209696 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 None None None 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 117475 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 117475 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
44297505 165855 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 165855 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 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
443894 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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 141717 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 141717 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 207342 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 207342 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 82374 0 None 234 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 82374 0 None 234 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 82374 0 None 234 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 179460 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 179460 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 191179 0 None - 1 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 191179 0 None - 1 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 192368 0 None - 1 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 192368 0 None - 1 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 209902 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 None None None 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 210044 0 None - 1 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 None None None 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 165424 0 None - 1 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 165424 0 None - 1 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 207283 0 None - 1 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 207283 0 None - 1 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 207286 0 None - 1 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 207286 0 None - 1 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 169258 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 169258 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 163638 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 163638 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 161612 19 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 161612 19 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
10303620 206274 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 206274 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 107036 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 107036 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 112313 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 112313 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 7027 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 7027 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 137240 0 None -104 5 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 137240 0 None -104 5 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 7029 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 7029 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 209707 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 None None None 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 7030 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 7030 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 192385 0 None - 1 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 192385 0 None - 1 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 214741 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 None None None Cc1ccc2c(c1)CC(O)Cc1nnc([C@H]3CC[C@H](Oc4ccccn4)CC3)n1-2 10.1021/acs.jmedchem.1c00863
CHEMBL2369835 209698 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 None None None 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
44520864 172635 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 172635 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 174416 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 174416 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 181854 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 181854 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 189604 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 189604 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 192611 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 192611 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 12472 0 None - 1 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 12472 0 None - 1 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
CHEMBL455418 12472 0 None - 1 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 12693 0 None - 1 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 12693 0 None - 1 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
CHEMBL505517 12693 0 None - 1 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 190124 1 None - 1 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 190124 1 None - 1 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 116995 0 None - 1 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 116995 0 None - 1 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 161441 0 None - 1 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 161441 0 None - 1 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 206858 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 206858 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 207441 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 207441 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 208898 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 None None None 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 33843 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 33843 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 119412 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 119412 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 206628 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 206628 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 209700 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 None None None 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 137220 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 137220 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 164592 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 164592 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 209695 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 None None None 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 7356 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 7356 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
10208389 78629 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 78629 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 189123 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 189123 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 190572 0 None - 1 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 190572 0 None - 1 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 191433 0 None - 1 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 191433 0 None - 1 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 191877 0 None - 1 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 191877 0 None - 1 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
44294575 82112 0 None - 1 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 82112 0 None - 1 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
44294542 96481 0 None - 1 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(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(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
CHEMBL262423 96481 0 None - 1 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(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(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 82385 0 None - 1 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 82385 0 None - 1 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 96907 17 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 96907 17 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 572 32 None -1288249 4 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 572 32 None -1288249 4 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 572 32 None -1288249 4 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 572 32 None -1288249 4 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 6733 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 6733 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 163841 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 163841 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
46890152 6751 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 6751 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 206683 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 206683 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 118598 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 118598 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 72105 0 None -316 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 72105 0 None -316 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 174827 10 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 174827 10 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
44520849 201711 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 201711 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 191837 0 None - 1 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 191837 0 None - 1 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 191486 0 None - 1 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 191486 0 None - 1 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 167836 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 167836 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 112305 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 112305 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 160426 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 160426 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 93315 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 93315 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 7301 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 7301 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 118601 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 118601 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 19390 0 None - 1 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 19390 0 None - 1 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 137394 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 137394 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 7252 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 7252 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
168272611 190384 0 None - 1 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 190384 0 None - 1 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 204965 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 204965 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 97285 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 97285 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 209699 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 None None None 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 179618 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 179618 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 12575 0 None - 1 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 12575 0 None - 1 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
CHEMBL479918 12575 0 None - 1 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 12579 0 None - 1 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 12579 0 None - 1 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
CHEMBL480104 12579 0 None - 1 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 199706 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 199706 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 199797 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 199797 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 82378 0 None - 1 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 82378 0 None - 1 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 82375 0 None - 1 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 82375 0 None - 1 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 82375 0 None - 1 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 63206 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 63206 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 156219 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 156219 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 73647 0 None -831 4 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 73647 0 None -831 4 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
10929819 106942 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 106942 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 78629 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 78629 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 6725 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 6725 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 78345 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
CHEMBL2093899 78345 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 78345 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 207287 0 None - 1 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 207287 0 None - 1 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 93315 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 93315 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 208896 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 None None None 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 208896 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 None None None 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 2981 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
2174 2981 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
2176 2981 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
439302 2981 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
CHEMBL395429 2981 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
DB00107 2981 58 None -831 8 Human 5.8 pKi = 5.8 Binding
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
54585227 61185 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 61185 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
44520856 189025 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 189025 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 12576 0 None - 1 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 12576 0 None - 1 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
CHEMBL479919 12576 0 None - 1 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 199862 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 199862 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 82386 0 None - 1 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 82386 0 None - 1 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 157238 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 157238 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 164440 1 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 164440 1 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 5223 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 5223 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 208892 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 None None None 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
CHEMBL339118 211615 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 None None None 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 96807 0 None -120226 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 96807 0 None -120226 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
10444 2324 14 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
139030525 2324 14 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 2324 14 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 2324 14 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 66617 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
CHEMBL1794053 66617 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 66617 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
44325377 111586 0 None - 1 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 111586 0 None - 1 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 159540 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 159540 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 12448 0 None - 1 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 12448 0 None - 1 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
CHEMBL448269 12448 0 None - 1 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 6849 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 6849 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 7094 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 7094 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
2200 3309 46 None -177 6 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
3482 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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
DB13929 3309 46 None -177 6 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 206683 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 206683 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 157380 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 157380 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 182026 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 182026 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 12675 0 None - 1 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 12675 0 None - 1 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
CHEMBL500371 12675 0 None - 1 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 190637 0 None - 1 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 190637 0 None - 1 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 207126 0 None - 1 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 207126 0 None - 1 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 108008 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 108008 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 73649 4 None -190 4 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 73649 4 None -190 4 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 118595 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 118595 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 73649 4 None -190 4 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 73649 4 None -190 4 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
CHEMBL52176 215596 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 None None None 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 90678 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 90678 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 6671 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 6671 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 118595 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 118595 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 206225 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 206225 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 82376 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 82376 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 7295 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 7295 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 7299 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 7299 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 191931 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 191931 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 194485 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
CHEMBL487164 194485 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 194485 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 155762 0 None - 1 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 155762 0 None - 1 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 206225 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 206225 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
CHEMBL2369829 209694 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 None None None 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
172997 2330 57 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 2330 57 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 2330 57 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 2330 57 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 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
443894 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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 14106 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 14106 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
44325345 111560 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 111560 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 112154 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 112154 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 117475 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 117475 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
44520853 185517 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 185517 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 12447 0 None - 1 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 12447 0 None - 1 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
CHEMBL448195 12447 0 None - 1 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 174589 0 None - 1 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 174589 0 None - 1 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 214224 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 None None None O[C@@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
44520884 12450 0 None - 1 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 12450 0 None - 1 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
CHEMBL448942 12450 0 None - 1 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 2225 18 None -54 6 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 2225 18 None -54 6 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 2225 18 None -54 6 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 190586 33 None - 1 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 190586 33 None - 1 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 6584 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 6584 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 103084 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 103084 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 6917 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 6917 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 7201 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 7201 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 118594 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 118594 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
10119966 185386 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 185386 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 12695 0 None - 1 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 12695 0 None - 1 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
CHEMBL506111 12695 0 None - 1 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 161614 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 161614 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
44520870 186951 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 186951 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 12732 0 None - 1 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 12732 0 None - 1 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
CHEMBL516757 12732 0 None - 1 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 208897 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 None None None 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
54584267 61183 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 61183 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 204998 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 204998 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 190511 0 None - 1 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 190511 0 None - 1 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
2181 1330 42 None -14 7 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 None None None None 10.1021/jm030611c
2182 1330 42 None -14 7 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 None None None None 10.1021/jm030611c
27991 1330 42 None -14 7 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 None None None None 10.1021/jm030611c
5311065 1330 42 None -14 7 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 None None None None 10.1021/jm030611c
CHEMBL1429 1330 42 None -14 7 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 None None None None 10.1021/jm030611c
CHEMBL264448 1330 42 None -14 7 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 None None None None 10.1021/jm030611c
DB00035 1330 42 None -14 7 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 None None None None 10.1021/jm030611c
46890153 6848 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 6848 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 163791 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 163791 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 6854 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 6854 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
CHEMBL2369845 209706 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 None None None 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 209701 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 None None None 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 136603 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 136603 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 102014 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 102014 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 97187 0 None -1071 4 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 12 14 -2.6 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(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
CHEMBL268306 97187 0 None -1071 4 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 12 14 -2.6 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(N)N)C(=O)NCC(N)=O)NC(=O)[C@@H](CC(N)=O)NC1=O 10.1021/jm030611c
5034737 206341 12 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 206341 12 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 206418 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 206418 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 6449 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 6449 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 182663 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 182663 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 207906 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 207906 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 82383 0 None - 1 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 82383 0 None - 1 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 210312 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 None None None 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 17002 13 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 17002 13 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 17002 13 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 17002 13 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 180557 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 180557 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
168270081 190052 0 None - 1 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 190052 0 None - 1 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 162097 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 162097 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 82372 0 None 38 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 82372 0 None 38 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 210906 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 None None None 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
44520866 181638 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 181638 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 117039 0 None - 1 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 117039 0 None - 1 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
44351440 168810 0 None - 1 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 168810 0 None - 1 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 155714 0 None - 1 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 155714 0 None - 1 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 2229 20 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 2229 20 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 2229 20 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
145978570 163817 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 163817 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 96421 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 96421 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
2200 3309 46 None -288 6 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
3482 3309 46 None -288 6 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 3309 46 None -288 6 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 3309 46 None -288 6 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
DB13929 3309 46 None -288 6 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
135916070 200971 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 200971 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 200971 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 200971 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 2759 33 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 2759 33 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 2759 33 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 2759 33 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 118475 4 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 118475 4 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 6672 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 6672 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 155724 0 None -28 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 155724 0 None -28 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 1163 50 None -2 6 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
216322 1163 50 None -2 6 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 1163 50 None -2 6 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 1163 50 None -2 6 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 1163 50 None -2 6 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 1163 50 None -2 6 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
44419029 96908 0 None -77 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 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 96908 0 None -77 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 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 141598 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 141598 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 111925 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 111925 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 112518 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 112518 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 162097 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 162097 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 137220 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 137220 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 180817 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 180817 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 209903 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 None None None 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 96876 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 96876 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 12996 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 12996 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
CHEMBL539285 12996 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 112557 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 112557 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 168004 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 168004 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 207389 0 None - 1 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 207389 0 None - 1 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 137395 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 137395 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 192360 4 None - 1 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 192360 4 None - 1 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
44294542 96481 0 None - 1 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(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(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
CHEMBL262423 96481 0 None - 1 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(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(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
44294542 96481 0 None - 1 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(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(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
CHEMBL262423 96481 0 None - 1 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(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(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
46890612 6902 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 6902 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 108000 0 None - 1 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 108000 0 None - 1 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 96756 0 None - 1 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 96756 0 None - 1 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 63207 0 None - 1 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 63207 0 None - 1 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 189983 0 None - 1 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 189983 0 None - 1 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 190049 0 None - 1 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 190049 0 None - 1 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 118601 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 118601 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 208899 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 None None None 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 61184 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 61184 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 138420 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 138420 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
2168 3974 38 None -15 9 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 None None None None 10.1016/j.bmc.2018.03.019
2810 3974 38 None -15 9 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 None None None None 10.1016/j.bmc.2018.03.019
644077 3974 38 None -15 9 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 None None None None 10.1016/j.bmc.2018.03.019
CHEMBL373742 3974 38 None -15 9 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 None None None None 10.1016/j.bmc.2018.03.019
DB00067 3974 38 None -15 9 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 None None None None 10.1016/j.bmc.2018.03.019
44335345 5169 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 5169 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
CHEMBL2372927 210313 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 None None None 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 2759 33 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 2759 33 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 2759 33 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 2759 33 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 2759 33 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 2759 33 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 2759 33 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 2759 33 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
44520867 182024 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 182024 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 104790 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 104790 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 518 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
3008 518 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
5311010 518 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
68613 518 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
CHEMBL378642 518 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
CHEMBL382301 518 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
DB09059 518 46 None -660 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human vasopressin V2 receptorBinding affinity to human vasopressin V2 receptor
ChEMBL None None None None 10.1016/j.bmcl.2007.11.008
CHEMBL52813 215703 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 None None None 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 164142 0 None - 1 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 164142 0 None - 1 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 164124 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 164124 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 6585 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 6585 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 208897 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 None None None 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 199264 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 199264 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 191038 0 None - 1 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 191038 0 None - 1 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 2981 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
2174 2981 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
2176 2981 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
439302 2981 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
CHEMBL395429 2981 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
DB00107 2981 58 None -831 8 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human Vasopressin V2 receptorBinding affinity towards human Vasopressin V2 receptor
ChEMBL None None None None 10.1021/jm010526+
44361522 121693 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 121693 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 35012 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 35012 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
46890184 6533 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 6533 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 209704 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 None None None 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 118595 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 118595 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
10187283 206211 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 206211 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 164275 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 164275 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 96492 0 None - 1 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 96492 0 None - 1 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 215716 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 None None None 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 73654 0 None -131 4 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 73654 0 None -131 4 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 2228 48 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 2228 48 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 2228 48 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 2228 48 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 2228 48 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 2228 48 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 2228 48 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 2228 48 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 2228 48 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 163713 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 163713 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 4115 5 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 4115 5 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 4115 5 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
168282087 190755 0 None - 1 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 190755 0 None - 1 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 7151 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 7151 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 138420 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 138420 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 4002 22 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 4002 22 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 4002 22 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 208895 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 None None None 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 208893 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 None None None 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
11634973 75337 15 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 75337 15 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 82379 0 None - 1 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 82379 0 None - 1 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
CHEMBL2370640 209901 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 None None None 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 106608 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 106608 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 112559 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 112559 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 192399 0 None - 1 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 192399 0 None - 1 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 209903 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 None None None 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 212713 0 None - 1 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 None None None 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
73348509 89418 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 89418 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 194485 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
CHEMBL487164 194485 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 194485 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 194485 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
CHEMBL487164 194485 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 194485 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 89418 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 89418 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 159741 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 159741 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 96491 0 None - 1 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 96491 0 None - 1 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 7423 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 7423 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
44314382 102992 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 102992 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 96619 0 None - 1 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 96619 0 None - 1 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 6995 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 6995 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 137242 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 137242 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 7424 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 7424 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
CHEMBL2369848 209708 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 None None None 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 168053 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 168053 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 204838 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 204838 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 96575 0 None -147 5 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 96575 0 None -147 5 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 161447 0 None -562 5 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 161447 0 None -562 5 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 210900 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 None None None 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 61186 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 61186 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 158832 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 158832 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 210043 0 None - 1 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 None None None 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 163515 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 163515 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 214227 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 None None None OC1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
53349364 166687 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 166687 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 7028 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 7028 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 210905 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 None None None 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 206181 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 206181 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 171713 0 None - 1 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 171713 0 None - 1 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 61181 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 61181 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
16051933 138128 4 None -25 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
CHEMBL376685 138128 4 None -25 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 138128 4 None -25 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 111424 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 111424 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 112567 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 112567 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
44317966 155650 0 None - 1 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 155650 0 None - 1 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 179372 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 179372 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 209901 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 None None None 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 82373 0 None 64 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 82373 0 None 64 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 82373 0 None 64 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 162097 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 162097 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 162097 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 162097 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 209702 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 None None None 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 4002 22 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 4002 22 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 4002 22 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 4002 22 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 4002 22 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 4002 22 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 17022 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 17022 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 210314 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 None None None 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 77582 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 77582 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 164077 13 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 164077 13 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 137393 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 137393 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
168288721 191392 0 None - 1 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 191392 0 None - 1 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 164783 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 164783 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 107468 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 107468 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 61182 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 61182 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
44520869 186932 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 186932 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 7349 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 7349 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 158058 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 158058 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 82377 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 82377 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 208894 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 None None None 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 2216 1 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 None None None None 10.1021/jm00169a001
9810632 2216 1 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 None None None None 10.1021/jm00169a001
CHEMBL127686 2216 1 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 None None None None 10.1021/jm00169a001
168280173 190781 0 None - 1 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 190781 0 None - 1 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 208898 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 None None None 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 210884 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 None None None 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 205523 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 205523 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 7129 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 7129 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 183510 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 183510 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 183510 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 183510 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 118475 4 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 118475 4 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 209697 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 None None None 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
CHEMBL1790547 208895 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 None None None 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 73648 0 None -100 5 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 73648 0 None -100 5 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 206211 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 206211 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
2249 2225 18 None -162 6 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 2225 18 None -162 6 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 2225 18 None -162 6 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 2225 18 None -162 6 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 2225 18 None -162 6 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 2225 18 None -162 6 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 12609 0 None - 1 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 12609 0 None - 1 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
CHEMBL485761 12609 0 None - 1 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 96876 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 96876 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
44294575 82112 0 None - 1 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 82112 0 None - 1 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 201087 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 201087 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 82112 0 None - 1 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 82112 0 None - 1 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
44351278 117280 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 117280 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 117280 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 117280 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 155762 0 None - 1 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 155762 0 None - 1 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 189912 0 None - 1 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 189912 0 None - 1 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 112736 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 112736 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 7251 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 7251 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 6835 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 6835 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 84302 0 None -316 5 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 84302 0 None -316 5 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 2981 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
2174 2981 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
2176 2981 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
439302 2981 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
CHEMBL395429 2981 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
DB00107 2981 58 None -63 8 Rat 7.2 pKi = 7.2 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
ChEMBL None None None None 10.1021/jm00171a003
168281109 191142 0 None - 1 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 191142 0 None - 1 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 62370 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 62370 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
CHEMBL2369842 209705 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 None None None 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 6853 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 6853 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 1076 1 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 1076 1 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 1076 1 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 1076 1 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 1076 1 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 1076 1 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 62374 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 62374 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 190509 0 None - 1 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 190509 0 None - 1 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 190082 0 None - 1 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 190082 0 None - 1 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 166687 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 166687 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 191056 0 None - 1 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 191056 0 None - 1 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 207809 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 207809 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 191573 0 None - 1 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 191573 0 None - 1 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
10907482 206273 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 206273 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 190642 0 None - 1 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 190642 0 None - 1 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 61180 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 61180 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 7133 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 7133 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 208892 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 None None None 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 161780 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 161780 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 206355 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 206355 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 14106 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 14106 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 96756 0 None - 1 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 96756 0 None - 1 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 171627 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 171627 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 201232 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 201232 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 11920 0 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 11920 0 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 82384 0 None - 1 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 82384 0 None - 1 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 209902 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 None None None 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 63206 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 63206 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 210045 0 None - 1 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 None None None 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 7355 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 7355 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 164828 1 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 164828 1 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 204758 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 204758 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 208894 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 None None None 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 106992 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 106992 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 208899 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 None None None 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 96907 17 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 96907 17 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 194864 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 194864 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 194864 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 83349 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 83349 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 7300 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 7300 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 164199 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 164199 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 199942 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 199942 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 208893 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 None None None 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 103051 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 103051 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
44325804 207308 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 207308 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 161289 0 None -37 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 161289 0 None -37 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 157137 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 157137 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 159025 0 None - 1 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 159025 0 None - 1 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 161315 0 None - 1 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 161315 0 None - 1 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 209703 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 None None None 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
10873853 106994 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 106994 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 6684 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 6684 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 6896 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 6896 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 2216 1 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 None None None None 10.1021/jm00099a019
9810632 2216 1 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 None None None None 10.1021/jm00099a019
CHEMBL127686 2216 1 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 None None None None 10.1021/jm00099a019
118734336 118598 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 118598 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 6735 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 6735 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
10144208 107126 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 107126 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 118597 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 118597 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 102528 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
CHEMBL2424668 102528 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 102528 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 2981 58 None -63 8 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 None None None None 10.1021/jm00171a003
2174 2981 58 None -63 8 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 None None None None 10.1021/jm00171a003
2176 2981 58 None -63 8 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 None None None None 10.1021/jm00171a003
439302 2981 58 None -63 8 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 None None None None 10.1021/jm00171a003
CHEMBL395429 2981 58 None -63 8 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 None None None None 10.1021/jm00171a003
DB00107 2981 58 None -63 8 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 None None None None 10.1021/jm00171a003
118734335 118596 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 118596 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 106124 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 106124 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
168294720 192467 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 192467 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 108590 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 108590 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 169521 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 169521 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 207176 0 None - 1 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 207176 0 None - 1 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 82374 0 None 234 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 82374 0 None 234 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 82374 0 None 234 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 12439 0 None - 1 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 12439 0 None - 1 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
CHEMBL444956 12439 0 None - 1 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 6683 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 6683 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 12608 0 None - 1 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 12608 0 None - 1 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
CHEMBL485760 12608 0 None - 1 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 210922 0 None - 1 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 None None None 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 96492 0 None - 1 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 96492 0 None - 1 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 182192 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 182192 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 182192 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 182192 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 63208 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 63208 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 214325 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 None None None O[C@H]1Cc2cc(Cl)ccc2-n2c(nnc2[C@H]2CC[C@H](Oc3ccccn3)CC2)C1 10.1021/acs.jmedchem.1c00863
2173 2954 13 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 2954 13 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 2954 13 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 2954 13 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 118592 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 118592 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 201541 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 201541 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 210046 0 None - 1 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 None None None 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 161291 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 161291 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 161291 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
56678446 63212 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 63212 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 118640 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 118640 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 205048 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 205048 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 3319 30 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 3319 30 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 3319 30 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 3319 30 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 2229 20 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 2229 20 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 2229 20 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 206274 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 206274 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 118601 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 118601 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 192359 0 None - 1 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 192359 0 None - 1 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
119369 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 216075 0 None - 9 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 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
146681949 216075 0 None -6 9 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 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
10615 572 32 None -1288249 4 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 572 32 None -1288249 4 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 572 32 None -1288249 4 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 572 32 None -1288249 4 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
2042 2981 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
2174 2981 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
2176 2981 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
439302 2981 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
CHEMBL395429 2981 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
DB00107 2981 58 None -831 8 Human 5.8 pKd None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
216237 3841 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 3841 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 3841 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 3841 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 3841 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 3841 89 3H-AVP 2 5 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
151171 1163 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216322 1163 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 1163 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 1163 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 1163 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 1163 50 3H-Oxytocin -2 6 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216237 3841 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 3841 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 3841 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 3841 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 3841 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 3841 89 3H-AVP 2 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
146681949 216075 0 3H-Oxytocin -1 9 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
146681949 216075 0 3H-AVP -1 9 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
146681949 216075 0 3H-AVP -1 9 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
216237 3841 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
2226 3841 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
4110 3841 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
443894 3841 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
CHEMBL344159 3841 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
DB06212 3841 89 3H-AVP -2 5 Rat 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C None
46783812 216077 0 3H-AVP 6 3 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 1182 19 14 16 -6.7 CC(=O)O.C1CC(N(C1)C(=O)C2CSSCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N.O.O.O None
None 216076 0 3H-Oxytocin -83 3 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 1151 20 12 15 -2.3 COC1=CC=C(C=C1)CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSC3(CCCCC3)CC(=O)N2)C(=O)N4CCCC4C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N)CC5=CC=CC=C5 None
119376 1839 48 3H-VASOPRESSIN -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
247 1839 48 3H-VASOPRESSIN -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
CHEMBL33884 1839 48 3H-VASOPRESSIN -54954 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 7 1 6 1.6 O=C(c1cn(c2c1cccc2)C)OCC1CCN(CC1)CCNS(=O)(=O)C None
135409468 2033 69 3H-VASOPRESSIN -3548 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2033 69 3H-VASOPRESSIN -3548 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2033 69 3H-VASOPRESSIN -3548 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
114904 2952 56 3H-AVP -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
114904 2952 56 3H-Oxytocin -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
2196 2952 56 3H-AVP -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
2196 2952 56 3H-Oxytocin -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
CHEMBL296908 2952 56 3H-AVP -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
CHEMBL296908 2952 56 3H-Oxytocin -446 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 449 7 1 4 3.2 CC(=O)NCCCOc1ccc(cc1)C(=O)N1CCC(CC1)N1C(=O)CCc2c1cccc2 None
128563 3462 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3462 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3462 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3462 33 3H-VASOPRESSIN -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
185 4004 60 3H-VASOPRESSIN -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4004 60 3H-VASOPRESSIN -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4004 60 3H-VASOPRESSIN -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4004 60 3H-VASOPRESSIN -30902 38 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
21830793 91833 10 3H-8-OH-DPAT -66069 45 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91833 10 3H-8-OH-DPAT -66069 45 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
3663 99965 83 3H-VASOPRESSIN -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
CHEMBL286494 99965 83 3H-VASOPRESSIN -288 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 None
44208932 140705 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140705 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
5280343 188273 124 3H-VASOPRESSIN -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188273 124 3H-VASOPRESSIN -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188273 124 3H-VASOPRESSIN -147 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
5281600 203023 92 3H-VASOPRESSIN -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203023 92 3H-VASOPRESSIN -275 33 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
1973 203481 15 3H-AVP -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203481 15 3H-AVP -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203481 15 3H-AVP -3 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
4054 205499 72 3H-VASOPRESSIN -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205499 72 3H-VASOPRESSIN -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205499 72 3H-VASOPRESSIN -1 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
None 215991 0 3H-VASOPRESSIN -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
6971132 216007 0 3H-VASOPRESSIN -2570 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
None 216237 0 3H-VASOPRESSIN -95499 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
None 216309 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216310 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216311 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216312 0 3H-VASOPRESSIN -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216314 0 3H-VASOPRESSIN -1 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216315 0 3H-VASOPRESSIN -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216316 0 3H-VASOPRESSIN -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 216325 0 3H-VASOPRESSIN -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 11 1 4 9.0 CC(C)C(=O)C12C(=O)C(=C(C(C1=O)(CC(C2(C)CCC=C(C)C)CC=C(C)C)CC=C(C)C)O)CC=C(C)C None
4978 216326 0 3H-VASOPRESSIN -16 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 520 1 7 9 4.3 CC1=CC(=C2C3=C1C4=C5C(=C(C=C4CO)O)C(=O)C6=C(C=C(C7=C6C5=C3C8=C7C(=CC(=C8C2=O)O)O)O)O)O None
None 216327 0 3H-VASOPRESSIN -3 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 464 4 8 12 -0.6 C1=CC(=C(C=C1C2=C(C(=C3C(=CC(=O)C=C3O2)O)O)OC4C(C(C(C(O4)CO)O)O)O)O)O None
None 216328 0 3H-VASOPRESSIN -281 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 610 6 10 16 -1.7 CC1C(C(C(C(O1)OCC2C(C(C(C(O2)OC3=C(OC4=CC(=CC(=C4C3=O)O)O)C5=CC(=C(C=C5)O)O)O)O)O)O)O)O None
None 216329 0 3H-VASOPRESSIN -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 448 3 7 11 0.4 CC1C(C(C(C(O1)OC2=C(OC3=CC(=O)C=C(C3=C2O)O)C4=CC(=C(C=C4)O)O)O)O)O None
2042 2981 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2174 2981 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2176 2981 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
439302 2981 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL395429 2981 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00107 2981 58 3H-Oxytocin -63 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2042 2981 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2174 2981 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2176 2981 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
439302 2981 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL395429 2981 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00107 2981 58 3H-AVP -831 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216182 0 3H-Oxytocin -309 4 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 755 14 5 8 1.7 CC(C=C)C(C(=O)N1CCCCC1(C=O)C(=O)N2CCCCC2)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCCN5C(=O)C(CC6=CN=CN6)N None
146681949 216075 0 3H-AVP -1 9 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
None 216183 0 3H-Oxytocin -64 4 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 780 14 4 9 2.2 CCC(C)C(C(=O)N(C(CC1=CNC2=CC=CC=C21)C=O)C(=O)C3CCCN3C(=O)C(CC4=CC=CCC4(C(=O)N5CCNCC5)C(=O)N6CC=CC=C6)NC)N None
151171 1163 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
216322 1163 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
2203 1163 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
732 1163 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
CHEMBL1755 1163 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
DB00872 1163 50 3H-AVP -2 6 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 498 4 2 3 6.5 Cc1[nH]c2c(n1)c1ccccc1N(CC2)C(=O)c1ccc(cc1)NC(=O)c1ccccc1c1ccccc1 None
146681949 216075 0 3H-AVP -1 9 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 1083 19 14 16 -5.4 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
None 216182 0 3H-Oxytocin -309 4 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 755 14 5 8 1.7 CC(C=C)C(C(=O)N1CCCCC1(C=O)C(=O)N2CCCCC2)NC(=O)C(CC3=CNC4=CC=CC=C43)NC(=O)C5CCCN5C(=O)C(CC6=CN=CN6)N None
None 216184 0 3H-Oxytocin -676 4 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 768 14 3 10 2.3 CCC(C)C(C(=O)C1(CCCN1C(=O)C(CC2=NC(N=C2)(C(=O)N3CCCCC3)C(=O)N4CCCCC4)N)C=O)NC(=O)C(CC5=CC6=CC=CC=C6C=C5)N None
None 216076 0 3H-AVP -83 3 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 1151 20 12 15 -2.3 COC1=CC=C(C=C1)CC2C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSC3(CCCCC3)CC(=O)N2)C(=O)N4CCCC4C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N)CC(=O)N)CCC(=O)N)CC5=CC=CC=C5 None
119369 2604 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 2604 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 2604 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 2604 74 3H-AVP -1 8 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
11169 796 37 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 None None None 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
131676677 796 37 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 None None None 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 796 37 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 None None None 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 796 37 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 None None None 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
495 796 37 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 None None None 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 796 37 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 None None None 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 796 37 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 None None None 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
119369 2604 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 2604 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 2604 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 2604 74 3H-Oxytocin -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
119369 2604 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 2604 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 2604 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 2604 74 3H-AVP -1 8 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
133612094 216484 0 None -13 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 CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(CSSCCC(=O)NC(C(=O)N1)CC2=CC=C(C=C2)OCC)C(=O)N3CCCC3C(=O)NC(CCCN)C(=O)NCC(=O)N)CC(=O)N)C(C)O None
2042 2981 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2174 2981 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2176 2981 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
439302 2981 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL395429 2981 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00107 2981 58 3H-AVP -63 8 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2042 2981 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
2174 2981 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
2176 2981 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
439302 2981 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
CHEMBL395429 2981 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
DB00107 2981 58 None -63 8 Rat 8.1 pKi = 8.1 Binding
Binding affinity against Vasopressin receptor in rat liverBinding affinity against Vasopressin receptor in rat liver
Drug Central None None None None None
46783812 216077 0 3H-Oxytocin 6 3 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 1182 19 14 16 -6.7 CC(=O)O.C1CC(N(C1)C(=O)C2CSSCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N.O.O.O None
119369 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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
122172899 217703 0 None -1 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
5311065 217703 0 None -1 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
CHEMBL1429 217703 0 None -1 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
DB00035 217703 0 None -1 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
151171 1163 50 None -2 6 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
216322 1163 50 None -2 6 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 1163 50 None -2 6 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 1163 50 None -2 6 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 1163 50 None -2 6 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 1163 50 None -2 6 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 3841 89 None -2 5 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 3841 89 None -2 5 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 3841 89 None -2 5 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
443894 3841 89 None -2 5 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 3841 89 None -2 5 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 3841 89 None -2 5 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 216075 0 None -1 9 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 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
None 216184 0 3H-Oxytocin -676 4 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 768 14 3 10 2.3 CCC(C)C(C(=O)C1(CCCN1C(=O)C(CC2=NC(N=C2)(C(=O)N3CCCCC3)C(=O)N4CCCCC4)N)C=O)NC(=O)C(CC5=CC6=CC=CC=C6C=C5)N None
216237 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
443894 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
122172899 217703 0 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
5311065 217703 0 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
CHEMBL1429 217703 0 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
DB00035 217703 0 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 NC(=O)CC[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)CCSSC[C@H](NC(=O)[C@H](CC(N)=O)NC1=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CCCNC(N)=N)C(=O)NCC(N)=O None
146681949 216075 0 None -1 9 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 C1CC(N(C1)C(=O)C2CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N2)CC(=O)N)CCC(=O)N)CC3=CC=CC=C3)CC4=CC=C(C=C4)O)N)C(=O)NC(CCCN=C(N)N)C(=O)NCC(=O)N None
119369 2604 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
2197 2604 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
4004 2604 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
CHEMBL420762 2604 74 3H-AVP 1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C None
151171 1163 50 None -1 6 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
216322 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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
133612094 216484 0 3H-AVP -13 5 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 993 18 11 15 -3.0 CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(CSSCCC(=O)NC(C(=O)N1)CC2=CC=C(C=C2)OCC)C(=O)N3CCCC3C(=O)NC(CCCN)C(=O)NCC(=O)N)CC(=O)N)C(C)O None
10444 2324 14 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
139030525 2324 14 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 2324 14 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 2324 14 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 1490 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2184 1490 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1649739
2184 1490 0 None -645 3 Human 5.1 pKi = 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2173 2954 13 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 2954 13 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 2954 13 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 2954 13 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 1345 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2236 1345 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
3080966 1345 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
3080966 1345 0 None - 1 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2172 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2172 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2959 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2959 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
644076 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
644076 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL1200690 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL1200690 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB14642 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
DB14642 2389 0 None -7 3 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
119369 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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 2604 74 None 1 8 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
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2181 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2182 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
27991 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
5311065 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL1429 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL264448 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
DB00035 1330 42 None -14 7 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2169 466 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2169 466 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
68649 466 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
68649 466 0 None -31 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
2168 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
2810 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
644077 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
CHEMBL373742 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10519430
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10780976
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9864265
DB00067 3974 38 None -15 9 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
158348 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 3485 18 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 2330 57 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 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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
443894 3841 89 None 2 5 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 3841 89 None 2 5 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 3841 89 None 2 5 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 1163 50 None -1 6 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
216322 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 1163 50 None -1 6 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 3352 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 3352 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 2952 56 None -1412 7 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 2952 56 None -1412 7 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 2952 56 None -1412 7 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 1352 0 None -794 3 Human 5.2 pKi None 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2209 3088 0 None -707 3 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2213 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2213 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
3008 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
3008 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
5311010 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
5311010 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
68613 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
68613 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
CHEMBL378642 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
CHEMBL378642 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
CHEMBL382301 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
CHEMBL382301 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
DB09059 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
DB09059 518 46 None -660 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14722330
2202 2759 33 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 2759 33 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 2759 33 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 2759 33 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 1354 0 None -3981 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2221 1354 0 None -3981 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2042 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2042 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2042 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2042 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2042 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2042 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2174 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2174 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2174 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2174 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2174 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2174 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2176 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
2176 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2176 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2176 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2176 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2176 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
439302 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
439302 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
439302 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
439302 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
439302 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
439302 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
CHEMBL395429 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
CHEMBL395429 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL395429 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
CHEMBL395429 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
CHEMBL395429 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
CHEMBL395429 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
DB00107 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12660315
DB00107 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
DB00107 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
DB00107 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
DB00107 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
DB00107 2981 58 None -831 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2188 1342 0 None -316 4 Rat 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2186 1341 0 None -630 4 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2195 2909 0 None -794 3 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2204 4115 5 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 4115 5 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 4115 5 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 1340 0 None -707 4 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2210 3089 0 None -398 3 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
119517 1473 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
119517 1473 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2225 1473 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2225 1473 0 None -354 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2208 3087 0 None -281 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2208 3087 0 None -281 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2190 1442 0 None -501 4 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2189 1443 0 None -630 4 Rat 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2185 1491 0 None -501 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2211 3090 0 None -398 3 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2219 1353 0 None -199 4 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11337500
2200 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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
3482 3309 46 None -177 6 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
3482 3309 46 None -177 6 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
3482 3309 46 None -177 6 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
3482 3309 46 None -177 6 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
3482 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 3309 46 None -177 6 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 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10866830
2223 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2223 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
2223 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2223 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
2223 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
6917952 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10866830
6917952 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
6917952 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9264324
6917952 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
6917952 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9459574
6917952 1351 0 None -79 4 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2235 1346 0 None -31 2 Human 6.9 pKi None 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2191 1444 0 None -630 4 Rat 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17300166
2215 1343 0 None -1 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
164712 3104 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2178 3104 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
CHEMBL3272682 3104 0 None -50 3 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2237 1347 0 None -19 2 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2212 3758 0 None -63 3 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2214 1344 0 None -1 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2214 1344 0 None -1 3 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2170 1331 0 None -7 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7774575
2170 1331 0 None -7 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
119369 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 2604 74 None -1 8 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 1349 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
122322 1349 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2217 1349 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
2217 1349 0 None -8 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9884074
2181 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2181 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2182 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2182 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
27991 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
27991 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
5311065 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
5311065 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL1429 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL1429 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
CHEMBL264448 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL264448 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
DB00035 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
DB00035 1330 42 None -14 7 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15084136
2170 1331 0 None 7 3 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2235 1346 0 None 31 2 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
171113 3968 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2180 3968 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
CHEMBL3274309 3968 0 None -3 3 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2237 1347 0 None 19 2 Rat 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2181 1330 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2182 1330 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
27991 1330 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
5311065 1330 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL1429 1330 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
CHEMBL264448 1330 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
DB00035 1330 42 None 6 7 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9792651
2183 1512 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
2183 1512 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
6441676 1512 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12446593
6441676 1512 0 None 3 3 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9322919
2229 3609 0 None - 1 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11012895
216237 3841 89 None -2 5 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 3841 89 None -2 5 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 3841 89 None -2 5 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
443894 3841 89 None -2 5 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 3841 89 None -2 5 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 3841 89 None -2 5 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 4121 6 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 4121 6 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 4121 6 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 3418 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 3418 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 3418 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 1348 0 None -1 2 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10866830
158348 3485 18 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 3485 18 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 3485 18 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 3485 18 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