Ligand source activities (1 row/activity)





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90469674 171925 None 8 Rat Functional pEC50 = 10.7 10.7 3 3
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 171925 None 8 Rat Functional pEC50 = 10.7 10.7 3 3
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 1331 None 29 Rat Functional pEC50 = 10.5 10.5 6 4
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 1331 None 29 Rat Functional pEC50 = 10.5 10.5 6 4
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 1331 None 29 Rat Functional pEC50 = 10.5 10.5 6 4
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
27991.0 1331 None 29 Rat Functional pEC50 = 10.5 10.5 6 4
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 1331 None 29 Rat Functional pEC50 = 10.5 10.5 6 4
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 1331 None 29 Rat Functional pEC50 = 10.5 10.5 6 4
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 1331 None 29 Rat Functional pEC50 = 10.5 10.5 6 4
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 168602 None 15 Human Functional pEC50 = 10.3 10.3 478 3
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 168602 None 15 Human Functional pEC50 = 10.3 10.3 478 3
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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
644077.0 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 173968 None 3 Rat Functional pEC50 = 10.3 10.3 5 3
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 173968 None 3 Rat Functional pEC50 = 10.3 10.3 5 3
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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
644077.0 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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
644077.0 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 3976 None 29 Human Functional pEC50 = 10.3 10.3 -12 6
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 171925 None 8 Human Functional pEC50 = 10.2 10.2 -3 3
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 171925 None 8 Human Functional pEC50 = 10.2 10.2 -3 3
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 171013 None 0 Human Functional pEC50 = 10.1 10.1 724 3
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 171013 None 0 Human Functional pEC50 = 10.1 10.1 724 3
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 172363 None 0 Human Functional pEC50 = 10.1 10.1 812 2
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 172363 None 0 Human Functional pEC50 = 10.1 10.1 812 2
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 170976 None 0 Human Functional pEC50 = 10 10.0 1778 2
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 170976 None 0 Human Functional pEC50 = 10 10.0 1778 2
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 171520 None 0 Human Functional pEC50 = 10 10.0 1412 2
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 171520 None 0 Human Functional pEC50 = 10 10.0 1412 2
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 173495 None 0 Human Functional pEC50 = 10 10.0 2290 3
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 173495 None 0 Human Functional pEC50 = 10 10.0 2290 3
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 173693 None 0 Human Functional pEC50 = 10 10.0 1584 2
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 173693 None 0 Human Functional pEC50 = 10 10.0 1584 2
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 175694 None 0 Human Functional pEC50 = 10 10.0 2630 2
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 175694 None 0 Human Functional pEC50 = 10 10.0 2630 2
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 173839 None 0 Human Functional pEC50 = 10.0 10.0 363 2
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 173839 None 0 Human Functional pEC50 = 10.0 10.0 363 2
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 174201 None 0 Human Functional pEC50 = 9.9 9.9 1174 2
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 174201 None 0 Human Functional pEC50 = 9.9 9.9 1174 2
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 173666 None 0 Human Functional pEC50 = 9.9 9.9 2691 2
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 173666 None 0 Human Functional pEC50 = 9.9 9.9 2691 2
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 172162 None 0 Human Functional pEC50 = 9.8 9.8 562 2
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 172162 None 0 Human Functional pEC50 = 9.8 9.8 562 2
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 170294 None 0 Human Functional pEC50 = 9.7 9.7 3388 2
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 170294 None 0 Human Functional pEC50 = 9.7 9.7 3388 2
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 171314 None 0 Human Functional pEC50 = 9.7 9.7 630 2
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 171314 None 0 Human Functional pEC50 = 9.7 9.7 630 2
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 173954 None 0 Human Functional pEC50 = 9.7 9.7 794 2
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 173954 None 0 Human Functional pEC50 = 9.7 9.7 794 2
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 1331 None 29 Human Functional pEC50 = 9.7 9.7 -6 4
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 1331 None 29 Human Functional pEC50 = 9.7 9.7 -6 4
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 1331 None 29 Human Functional pEC50 = 9.7 9.7 -6 4
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
27991.0 1331 None 29 Human Functional pEC50 = 9.7 9.7 -6 4
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 1331 None 29 Human Functional pEC50 = 9.7 9.7 -6 4
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 1331 None 29 Human Functional pEC50 = 9.7 9.7 -6 4
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 1331 None 29 Human Functional pEC50 = 9.7 9.7 -6 4
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 175328 None 0 Human Functional pEC50 = 9.7 9.7 645 2
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 175328 None 0 Human Functional pEC50 = 9.7 9.7 645 2
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 171051 None 0 Human Functional pEC50 = 9.7 9.7 575 2
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 171051 None 0 Human Functional pEC50 = 9.7 9.7 575 2
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 172312 None 0 Human Functional pEC50 = 9.7 9.7 1513 2
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 172312 None 0 Human Functional pEC50 = 9.7 9.7 1513 2
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 170420 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 170420 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 173269 None 0 Human Functional pEC50 = 9.7 9.7 954 2
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 173269 None 0 Human Functional pEC50 = 9.7 9.7 954 2
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 175439 None 0 Human Functional pEC50 = 9.7 9.7 501 2
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 175439 None 0 Human Functional pEC50 = 9.7 9.7 501 2
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 170771 None 0 Human Functional pEC50 = 9.6 9.6 2089 2
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 170771 None 0 Human Functional pEC50 = 9.6 9.6 2089 2
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 173630 None 0 Human Functional pEC50 = 9.6 9.6 2089 2
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 173630 None 0 Human Functional pEC50 = 9.6 9.6 2089 2
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 173968 None 3 Human Functional pEC50 = 9.6 9.6 -5 3
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 173968 None 3 Human Functional pEC50 = 9.6 9.6 -5 3
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 174157 None 0 Human Functional pEC50 = 9.6 9.6 741 2
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 174157 None 0 Human Functional pEC50 = 9.6 9.6 741 2
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 174619 None 0 Human Functional pEC50 = 9.6 9.6 588 2
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 174619 None 0 Human Functional pEC50 = 9.6 9.6 588 2
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 170785 None 0 Human Functional pEC50 = 9.6 9.6 1288 2
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 170785 None 0 Human Functional pEC50 = 9.6 9.6 1288 2
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 174715 None 0 Human Functional pEC50 = 9.6 9.6 169 2
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 174715 None 0 Human Functional pEC50 = 9.6 9.6 169 2
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 171512 None 0 Human Functional pEC50 = 9.5 9.5 524 2
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 171512 None 0 Human Functional pEC50 = 9.5 9.5 524 2
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 174266 None 0 Human Functional pEC50 = 9.5 9.5 588 2
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 174266 None 0 Human Functional pEC50 = 9.5 9.5 588 2
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 174698 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 174698 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 169901 None 0 Human Functional pEC50 = 9.5 9.5 331 2
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 169901 None 0 Human Functional pEC50 = 9.5 9.5 331 2
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 169861 None 0 Human Functional pEC50 = 9.5 9.5 457 2
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 169861 None 0 Human Functional pEC50 = 9.5 9.5 457 2
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 173626 None 0 Human Functional pEC50 = 9.5 9.5 457 3
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 173626 None 0 Human Functional pEC50 = 9.5 9.5 457 3
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 173482 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 173482 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 170304 None 0 Human Functional pEC50 = 9.5 9.5 758 2
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 170304 None 0 Human Functional pEC50 = 9.5 9.5 758 2
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 169645 None 0 Human Functional pEC50 = 9.5 9.5 630 2
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 169645 None 0 Human Functional pEC50 = 9.5 9.5 630 2
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 173263 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 173263 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 172900 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 172900 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 174509 None 0 Human Functional pEC50 = 9.4 9.4 2089 2
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 174509 None 0 Human Functional pEC50 = 9.4 9.4 2089 2
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 211472 None 20 Human Functional pEC50 = 9.4 9.4 -1 5
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 169714 None 0 Human Functional pEC50 = 9.4 9.4 1288 2
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 169714 None 0 Human Functional pEC50 = 9.4 9.4 1288 2
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 211472 None 20 Human Functional pEC50 = 9.4 9.4 -1 5
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 4004 None 22 Human Functional pEC50 = 9.2 9.2 3 4
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 4004 None 22 Human Functional pEC50 = 9.2 9.2 3 4
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 4004 None 22 Human Functional pEC50 = 9.2 9.2 3 4
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 4004 None 22 Human Functional pEC50 = 9.1 9.1 3 4
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 4004 None 22 Human Functional pEC50 = 9.1 9.1 3 4
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 4004 None 22 Human Functional pEC50 = 9.1 9.1 3 4
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 202255 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 202255 None 0 Human Functional pEC50 = 9.0 9.0 - 1
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 204170 None 0 Human Functional pEC50 = 9 9.0 - 1
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 204170 None 0 Human Functional pEC50 = 9 9.0 - 1
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 202164 None 0 Human Functional pEC50 = 9 9.0 - 1
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 202164 None 0 Human Functional pEC50 = 9 9.0 - 1
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 202320 None 0 Human Functional pEC50 = 9 9.0 - 1
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 202320 None 0 Human Functional pEC50 = 9 9.0 - 1
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 12581 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 12581 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 12581 None 0 Human Functional pEC50 = 8.9 8.9 - 1
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 211473 None 0 Human Functional pEC50 = 8.9 8.9 -18 4
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 211473 None 0 Human Functional pEC50 = 8.9 8.9 -18 4
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 73886 None 0 Human Functional pEC50 = 8.8 8.8 43 3
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 73886 None 0 Human Functional pEC50 = 8.8 8.8 43 3
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 194595 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 194595 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 194595 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 194595 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 194595 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 194595 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 188460 None 0 Human Functional pEC50 = 8 8.0 - 1
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 188460 None 0 Human Functional pEC50 = 8 8.0 - 1
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 189026 None 0 Human Functional pEC50 = 8 8.0 - 1
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 189026 None 0 Human Functional pEC50 = 8 8.0 - 1
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 176848 None 0 Human Functional pEC50 = 7 7.0 - 1
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 176848 None 0 Human Functional pEC50 = 7 7.0 - 1
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 189952 None 0 Human Functional pEC50 = 7 7.0 - 1
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 189952 None 0 Human Functional pEC50 = 7 7.0 - 1
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 180446 None 0 Human Functional pEC50 = 6 6.0 - 1
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 180446 None 0 Human Functional pEC50 = 6 6.0 - 1
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 12585 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 12585 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 12585 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 161575 None 0 Human Functional pEC50 = 5.0 5.0 -309 4
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 161575 None 0 Human Functional pEC50 = 5.0 5.0 -309 4
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 174694 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 174694 None 0 Human Functional pEC50 = 7.0 7.0 - 1
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 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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
165708555.0 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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
16681432.0 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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
495 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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 797 None 33 Human Functional pEC50 = 6.0 6.0 -173 5
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 12582 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 12582 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 12582 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 211441 None 0 Human Functional pEC50 = 6.0 6.0 -61 3
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 211441 None 0 Human Functional pEC50 = 6.0 6.0 -61 3
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 211482 None 0 Human Functional pEC50 = 6.9 6.9 -218 4
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 211487 None 0 Human Functional pEC50 = 5.9 5.9 -1513 4
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 180617 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 180617 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 190894 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 190894 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 211482 None 0 Human Functional pEC50 = 6.9 6.9 -218 4
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 64641 None 0 Human Functional pEC50 = 5.9 5.9 -17 3
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 64641 None 0 Human Functional pEC50 = 5.9 5.9 -17 3
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 211486 None 0 Human Functional pEC50 = 5.9 5.9 -93 3
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 211487 None 0 Human Functional pEC50 = 5.9 5.9 -1513 4
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 64641 None 0 Human Functional pEC50 = 5.9 5.9 -17 3
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 64641 None 0 Human Functional pEC50 = 5.9 5.9 -17 3
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 211486 None 0 Human Functional pEC50 = 5.9 5.9 -93 3
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 66086 None 0 Human Functional pEC50 = 7.9 7.9 -74 2
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 66086 None 0 Human Functional pEC50 = 7.9 7.9 -74 2
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 174695 None 0 Rat Functional pEC50 = 7.9 7.9 -6 2
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 174695 None 0 Rat Functional pEC50 = 7.9 7.9 -6 2
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 173519 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 173519 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 211446 None 0 Human Functional pEC50 = 6.9 6.9 -512 5
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 211446 None 0 Human Functional pEC50 = 6.9 6.9 -512 5
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 211447 None 0 Human Functional pEC50 = 6.9 6.9 -1348 5
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 174348 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 174348 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 176857 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 176857 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 176858 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 176858 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 193333 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 193333 None 0 Human Functional pEC50 = 6.9 6.9 - 1
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 211447 None 0 Human Functional pEC50 = 6.9 6.9 -1348 5
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 179336 None 0 Rat Functional pEC50 = 7.8 7.8 -3 2
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 179336 None 0 Rat Functional pEC50 = 7.8 7.8 -3 2
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 177007 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 177007 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 190697 None 33 Rat Functional pEC50 = 6.8 6.8 -6 2
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 190697 None 33 Rat Functional pEC50 = 6.8 6.8 -6 2
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 211476 None 6 Human Functional pEC50 = 6.8 6.8 -1258 4
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 211476 None 6 Human Functional pEC50 = 6.8 6.8 -1258 4
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 180925 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 180925 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 64654 None 0 Human Functional pEC50 = 5.8 5.8 -602 4
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 64654 None 0 Human Functional pEC50 = 5.8 5.8 -602 4
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 211443 None 0 Human Functional pEC50 = 5.8 5.8 -4786 4
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 64654 None 0 Human Functional pEC50 = 5.8 5.8 -602 4
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 64654 None 0 Human Functional pEC50 = 5.8 5.8 -602 4
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 64642 None 0 Human Functional pEC50 = 6.8 6.8 -13 3
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 64642 None 0 Human Functional pEC50 = 6.8 6.8 -13 3
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 211443 None 0 Human Functional pEC50 = 5.8 5.8 -4786 4
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 64824 None 0 Human Functional pEC50 = 5.8 5.8 -1513 3
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 64824 None 0 Human Functional pEC50 = 5.8 5.8 -1513 3
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 64642 None 0 Human Functional pEC50 = 6.8 6.8 -13 3
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 64642 None 0 Human Functional pEC50 = 6.8 6.8 -13 3
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 180445 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 180445 None 0 Human Functional pEC50 = 5.8 5.8 - 1
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 64824 None 0 Human Functional pEC50 = 5.8 5.8 -1513 3
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 64824 None 0 Human Functional pEC50 = 5.8 5.8 -1513 3
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 174693 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 174693 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 176856 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 176856 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 211449 None 0 Human Functional pEC50 = 6.7 6.7 -234 4
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 2956 None 18 Human Functional pEC50 = 6.7 6.7 -1 2
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 2956 None 18 Human Functional pEC50 = 6.7 6.7 -1 2
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 2956 None 18 Human Functional pEC50 = 6.7 6.7 -1 2
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 2956 None 18 Human Functional pEC50 = 6.7 6.7 -1 2
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 161458 None 0 Human Functional pEC50 = 4.7 4.7 -1348 4
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 161458 None 0 Human Functional pEC50 = 4.7 4.7 -1348 4
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 211449 None 0 Human Functional pEC50 = 6.7 6.7 -234 4
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 174695 None 0 Human Functional pEC50 = 8.7 8.7 6 2
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 174695 None 0 Human Functional pEC50 = 8.7 8.7 6 2
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 177095 None 0 Human Functional pEC50 = 8.6 8.6 17 2
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 177095 None 0 Human Functional pEC50 = 8.6 8.6 17 2
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 202400 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 202400 None 0 Human Functional pEC50 = 8.6 8.6 - 1
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 179043 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 179043 None 0 Human Functional pEC50 = 7.7 7.7 - 1
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 211483 None 0 Human Functional pEC50 = 6.7 6.7 -323 4
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 211483 None 0 Human Functional pEC50 = 6.7 6.7 -323 4
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 64821 None 0 Human Functional pEC50 = 6.7 6.7 -34 4
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 64821 None 0 Human Functional pEC50 = 6.7 6.7 -34 4
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 2983 None 40 Human Functional pEC50 = 6.7 6.7 -25 5
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 2983 None 40 Human Functional pEC50 = 6.7 6.7 -25 5
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 2983 None 40 Human Functional pEC50 = 6.7 6.7 -25 5
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 2983 None 40 Human Functional pEC50 = 6.7 6.7 -25 5
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
439302.0 2983 None 40 Human Functional pEC50 = 6.7 6.7 -25 5
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 2983 None 40 Human Functional pEC50 = 6.7 6.7 -25 5
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 2983 None 40 Human Functional pEC50 = 6.7 6.7 -25 5
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 177080 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 177080 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 64821 None 0 Human Functional pEC50 = 6.7 6.7 -34 4
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 64821 None 0 Human Functional pEC50 = 6.7 6.7 -34 4
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 66085 None 0 Human Functional pEC50 = 6.7 6.7 -204 2
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 66085 None 0 Human Functional pEC50 = 6.7 6.7 -204 2
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 179615 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 179615 None 0 Human Functional pEC50 = 6.7 6.7 - 1
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 179613 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 179613 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 137987 None 19 Human Functional pEC50 = 5.6 5.6 -48 4
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 137987 None 19 Human Functional pEC50 = 5.6 5.6 -48 4
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 190697 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 190697 None 33 Human Functional pEC50 = 7.6 7.6 6 2
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 211481 None 0 Human Functional pEC50 = 5.6 5.6 -131 4
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 211481 None 0 Human Functional pEC50 = 5.6 5.6 -131 4
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 211448 None 0 Human Functional pEC50 = 6.6 6.6 -1621 5
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 211448 None 0 Human Functional pEC50 = 6.6 6.6 -1621 5
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 64646 None 0 Human Functional pEC50 = 5.6 5.6 -645 3
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 64646 None 0 Human Functional pEC50 = 5.6 5.6 -645 3
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 64822 None 0 Human Functional pEC50 = 5.6 5.6 -67 3
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 64822 None 0 Human Functional pEC50 = 5.6 5.6 -67 3
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 64646 None 0 Human Functional pEC50 = 5.6 5.6 -645 3
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 64646 None 0 Human Functional pEC50 = 5.6 5.6 -645 3
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 64822 None 0 Human Functional pEC50 = 5.6 5.6 -67 3
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 64822 None 0 Human Functional pEC50 = 5.6 5.6 -67 3
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 66081 None 13 Human Functional pEC50 = 6.6 6.6 -102 2
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 66081 None 13 Human Functional pEC50 = 6.6 6.6 -102 2
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 179363 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 179363 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 176851 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 176851 None 0 Human Functional pEC50 = 6.6 6.6 - 1
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 3577 None 12 Human Functional pEC50 = 5.6 5.6 -4786 5
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 211445 None 0 Human Functional pEC50 = 6.6 6.6 -2238 5
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 2983 None 40 Human Functional pEC50 = 7.5 7.5 -25 5
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 2983 None 40 Human Functional pEC50 = 7.5 7.5 -25 5
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 2983 None 40 Human Functional pEC50 = 7.5 7.5 -25 5
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 2983 None 40 Human Functional pEC50 = 7.5 7.5 -25 5
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
439302.0 2983 None 40 Human Functional pEC50 = 7.5 7.5 -25 5
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 2983 None 40 Human Functional pEC50 = 7.5 7.5 -25 5
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 2983 None 40 Human Functional pEC50 = 7.5 7.5 -25 5
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 211445 None 0 Human Functional pEC50 = 6.5 6.5 -2238 5
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 12738 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 12738 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 12738 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 177053 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 177053 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 174699 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 174699 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 64823 None 0 Human Functional pEC50 = 5.5 5.5 -144 3
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 64823 None 0 Human Functional pEC50 = 5.5 5.5 -144 3
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 64823 None 0 Human Functional pEC50 = 5.5 5.5 -144 3
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 64823 None 0 Human Functional pEC50 = 5.5 5.5 -144 3
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 66082 None 0 Human Functional pEC50 = 7.5 7.5 -9 2
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 66082 None 0 Human Functional pEC50 = 7.5 7.5 -9 2
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 211484 None 0 Human Functional pEC50 = 6.5 6.5 -151 4
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 211484 None 0 Human Functional pEC50 = 6.5 6.5 -151 4
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 176976 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 176976 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 161655 None 0 Human Functional pEC50 = 5.4 5.4 -33 4
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 161655 None 0 Human Functional pEC50 = 5.4 5.4 -33 4
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 189970 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 189970 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 211451 None 0 Human Functional pEC50 = 5.4 5.4 -2691 4
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 211451 None 0 Human Functional pEC50 = 5.4 5.4 -2691 4
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 176977 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 176977 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 211489 None 0 Human Functional pEC50 = 6.4 6.4 -407 4
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 211489 None 0 Human Functional pEC50 = 6.4 6.4 -407 4
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 211460 None 0 Human Functional pEC50 = 6.4 6.4 -1202 5
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 177101 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 177101 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 211460 None 0 Human Functional pEC50 = 6.4 6.4 -1202 5
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 161671 None 0 Human Functional pEC50 = 5.4 5.4 -114 4
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 161671 None 0 Human Functional pEC50 = 5.4 5.4 -114 4
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 163810 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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 163810 None 0 Human Functional pEC50 = 8.4 8.4 2 3
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 211475 None 0 Human Functional pEC50 = 8.4 8.4 -17 4
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 211475 None 0 Human Functional pEC50 = 8.4 8.4 -17 4
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 182771 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 182771 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 179336 None 0 Human Functional pEC50 = 8.4 8.4 3 2
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 179336 None 0 Human Functional pEC50 = 8.4 8.4 3 2
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 189826 None 0 Human Functional pEC50 = 8.3 8.3 13 2
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 189826 None 0 Human Functional pEC50 = 8.3 8.3 13 2
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 189193 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 189193 None 0 Human Functional pEC50 = 7.4 7.4 - 1
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 2326 None 17 Human Functional pEC50 = 7.4 7.4 -9 4
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 2326 None 17 Human Functional pEC50 = 7.4 7.4 -9 4
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 2326 None 17 Human Functional pEC50 = 7.4 7.4 -9 4
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 2326 None 17 Human Functional pEC50 = 7.4 7.4 -9 4
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 177095 None 0 Rat Functional pEC50 = 7.4 7.4 -17 2
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 177095 None 0 Rat Functional pEC50 = 7.4 7.4 -17 2
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 189427 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 189427 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 211485 None 0 Human Functional pEC50 = 6.3 6.3 -42 3
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 174700 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 174700 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 211485 None 0 Human Functional pEC50 = 6.3 6.3 -42 3
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 179489 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 179489 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 65298 None 2 Rat Functional pEC50 = 7.3 7.3 1 2
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 65298 None 2 Rat Functional pEC50 = 7.3 7.3 1 2
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 64653 None 0 Human Functional pEC50 = 5.3 5.3 -1348 3
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 64653 None 0 Human Functional pEC50 = 5.3 5.3 -1348 3
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 64653 None 0 Human Functional pEC50 = 5.3 5.3 -1348 3
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 64653 None 0 Human Functional pEC50 = 5.3 5.3 -1348 3
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 65298 None 2 Human Functional pEC50 = 7.2 7.2 -1 2
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 65298 None 2 Human Functional pEC50 = 7.2 7.2 -1 2
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 182300 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 182300 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 182300 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 182300 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 12614 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 12614 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 12614 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 12699 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 12699 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 12699 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 189826 None 0 Rat Functional pEC50 = 7.2 7.2 -13 2
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 189826 None 0 Rat Functional pEC50 = 7.2 7.2 -13 2
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 2326 None 17 Human Functional pEC50 = 6.2 6.2 -9 4
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 2326 None 17 Human Functional pEC50 = 6.2 6.2 -9 4
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 2326 None 17 Human Functional pEC50 = 6.2 6.2 -9 4
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 2326 None 17 Human Functional pEC50 = 6.2 6.2 -9 4
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 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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
165708555.0 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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
16681432.0 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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
495 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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 797 None 33 Human Functional pEC50 = 5.2 5.2 -173 5
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 177099 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 177099 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 211477 None 0 Human Functional pEC50 = 7.1 7.1 -144 4
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 211444 None 0 Human Functional pEC50 = 6.1 6.1 -24 3
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 211444 None 0 Human Functional pEC50 = 6.1 6.1 -24 3
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 211477 None 0 Human Functional pEC50 = 7.1 7.1 -144 4
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 190021 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 190021 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 211488 None 0 Human Functional pEC50 = 6.1 6.1 -3019 4
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 211488 None 0 Human Functional pEC50 = 6.1 6.1 -3019 4
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 2983 None 40 Human Functional pEC50 = 6.1 6.1 -25 5
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 2983 None 40 Human Functional pEC50 = 6.1 6.1 -25 5
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 2983 None 40 Human Functional pEC50 = 6.1 6.1 -25 5
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 2983 None 40 Human Functional pEC50 = 6.1 6.1 -25 5
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
439302.0 2983 None 40 Human Functional pEC50 = 6.1 6.1 -25 5
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 2983 None 40 Human Functional pEC50 = 6.1 6.1 -25 5
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 2983 None 40 Human Functional pEC50 = 6.1 6.1 -25 5
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 174345 None 1 Human Functional pEC50 = 7.1 7.1 - 1
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 174345 None 1 Human Functional pEC50 = 7.1 7.1 - 1
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 177079 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 177079 None 0 Human Functional pEC50 = 6.1 6.1 - 1
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 180970 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 180970 None 0 Human Functional pEC50 = 7.1 7.1 - 1
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 122996 None 20 Human Functional pEC50 = 6.1 6.1 -107 3
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 122996 None 20 Human Functional pEC50 = 6.1 6.1 -107 3
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 211474 None 0 Human Functional pEC50 = 8.0 8.0 -64 3
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 211474 None 0 Human Functional pEC50 = 8.0 8.0 -64 3
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 189950 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 189950 None 0 Human Functional pEC50 = 6.0 6.0 - 1
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 211455 None 0 Human Functional pEC50 = 6.0 6.0 -1548 5
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 211455 None 0 Human Functional pEC50 = 6.0 6.0 -1548 5
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 211469 None 0 Human Functional pEC50 = 6.0 6.0 -691 4
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 211469 None 0 Human Functional pEC50 = 6.0 6.0 -691 4
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 203691 None 0 Human Functional pIC50 = 9.2 9.2 2 3
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 203691 None 0 Human Functional pIC50 = 9.2 9.2 2 3
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 168496 None 0 Human Functional pIC50 = 9.0 9.0 39 3
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 168496 None 0 Human Functional pIC50 = 9.0 9.0 39 3
Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
ChEMBL 462 5 1 3 6.0 Cc1ccccc1OCC(=O)Nc1ccc(C(=O)N2CCCCc3cc(Cl)ccc32)c(C)c1 10.1021/jm000108p
121301508 176323 None 5 Human Functional pIC50 = 8.8 8.8 2 4
Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
CHEMBL4594444 176323 None 5 Human Functional pIC50 = 8.8 8.8 2 4
Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).Assay with bioluminescence detection (AVPR). (The vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence).
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
11432362 94190 None 0 Human Functional pIC50 = 7 7.0 -1 2
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 94190 None 0 Human Functional pIC50 = 7 7.0 -1 2
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 107357 None 0 Human Functional pIC50 = 7 7.0 -7 2
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 107357 None 0 Human Functional pIC50 = 7 7.0 -7 2
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 116845 None 0 Human Functional pIC50 = 7 7.0 4 2
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 116845 None 0 Human Functional pIC50 = 7 7.0 4 2
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 111022 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
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 111022 None 0 Human Functional pIC50 = 7.0 7.0 -2 2
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 154993 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
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 154993 None 0 Human Functional pIC50 = 6.0 6.0 -3 2
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 1164 None 41 Human Functional pIC50 = 8.0 8.0 -3 2
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
151171.0 1164 None 41 Human Functional pIC50 = 8.0 8.0 -3 2
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 1164 None 41 Human Functional pIC50 = 8.0 8.0 -3 2
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 1164 None 41 Human Functional pIC50 = 8.0 8.0 -3 2
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 1164 None 41 Human Functional pIC50 = 8.0 8.0 -3 2
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 1164 None 41 Human Functional pIC50 = 8.0 8.0 -3 2
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 1164 None 41 Human Functional pIC50 = 8.0 8.0 -3 2
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 94247 None 0 Human Functional pIC50 = 8.0 8.0 2 2
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 94247 None 0 Human Functional pIC50 = 8.0 8.0 2 2
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 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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
216237.0 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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
443894.0 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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 3843 None 51 Human Functional pIC50 = 8.0 8.0 66 11
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 154710 None 0 Human Functional pIC50 = 6.9 6.9 -2 2
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 154710 None 0 Human Functional pIC50 = 6.9 6.9 -2 2
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 163810 None 0 Human Functional pIC50 = 7.9 7.9 2 3
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 163810 None 0 Human Functional pIC50 = 7.9 7.9 2 3
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 94150 None 0 Human Functional pIC50 = 6.9 6.9 91 2
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 94150 None 0 Human Functional pIC50 = 6.9 6.9 91 2
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 169011 None 0 Human Functional pIC50 = 6.8 6.8 -5 2
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 169011 None 0 Human Functional pIC50 = 6.8 6.8 -5 2
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 202388 None 41 Human Functional pIC50 = 5.8 5.8 -20 2
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 202388 None 41 Human Functional pIC50 = 5.8 5.8 -20 2
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 191948 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 191948 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 164260 None 0 Human Functional pIC50 = 6.8 6.8 -7 2
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 164260 None 0 Human Functional pIC50 = 6.8 6.8 -7 2
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 154894 None 0 Human Functional pIC50 = 5.8 5.8 -2 2
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 154894 None 0 Human Functional pIC50 = 5.8 5.8 -2 2
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 94330 None 0 Human Functional pIC50 = 6.7 6.7 -6 2
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 94330 None 0 Human Functional pIC50 = 6.7 6.7 -6 2
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 109264 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
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 109264 None 0 Human Functional pIC50 = 7.7 7.7 -1 2
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 173934 None 0 Human Functional pIC50 = 4.7 4.7 -489 4
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 173934 None 0 Human Functional pIC50 = 4.7 4.7 -489 4
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 192510 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 192510 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 175942 None 0 Human Functional pIC50 = 4.6 4.6 -125 4
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 175942 None 0 Human Functional pIC50 = 4.6 4.6 -125 4
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 175008 None 0 Human Functional pIC50 = 4.6 4.6 -851 4
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 175008 None 0 Human Functional pIC50 = 4.6 4.6 -851 4
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 202388 None 41 Human Functional pIC50 = 5.6 5.6 -20 2
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 202388 None 41 Human Functional pIC50 = 5.6 5.6 -20 2
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 94248 None 8 Rat Functional pIC50 = 7.5 7.5 -2 4
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 94248 None 8 Rat Functional pIC50 = 7.5 7.5 -2 4
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 18966 None 0 Human Functional pIC50 = 7.5 7.5 24 2
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 18966 None 0 Human Functional pIC50 = 7.5 7.5 24 2
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 116685 None 0 Human Functional pIC50 = 7.5 7.5 91 2
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 116685 None 0 Human Functional pIC50 = 7.5 7.5 91 2
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 107473 None 0 Human Functional pIC50 = 7.5 7.5 -6 2
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 107473 None 0 Human Functional pIC50 = 7.5 7.5 -6 2
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 176222 None 16 Human Functional pIC50 = 4.5 4.5 -2137 4
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 176222 None 16 Human Functional pIC50 = 4.5 4.5 -2137 4
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 57550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 57550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 163447 None 0 Human Functional pIC50 = 6.5 6.5 -1 2
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 163447 None 0 Human Functional pIC50 = 6.5 6.5 -1 2
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 154819 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 154819 None 0 Human Functional pIC50 = 7.4 7.4 -1 2
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 63057 None 0 Human Functional pIC50 = 7.4 7.4 -3 4
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 63057 None 0 Human Functional pIC50 = 7.4 7.4 -3 4
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 118518 None 0 Human Functional pIC50 = 7.4 7.4 58 2
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 118518 None 0 Human Functional pIC50 = 7.4 7.4 58 2
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 154893 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
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 154893 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levelsAntagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
ChEMBL 542 5 2 3 7.0 O=C(O)C1=CC2(CC1)CCN(C(=O)c1ccc(NC(=O)c3ccccc3-c3ccccc3)cc1)c1ccccc1C2 10.1016/j.bmcl.2007.09.059
216237 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
216237.0 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
2226 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
4110 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
443894 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
443894.0 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
CHEMBL344159 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
DB06212 3843 None 51 Human Functional pIC50 = 8.4 8.4 66 11
GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2GPCR PRESTO-Tango dose-response in antagonist mode with target: AVPR2
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.6019/CHEMBL5442687
25132666 94582 None 0 Human Functional pIC50 = 7.4 7.4 1 2
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 94582 None 0 Human Functional pIC50 = 7.4 7.4 1 2
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 115320 None 0 Human Functional pIC50 = 7.4 7.4 47 2
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 115320 None 0 Human Functional pIC50 = 7.4 7.4 47 2
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 117075 None 0 Human Functional pIC50 = 7.4 7.4 44 2
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 117075 None 0 Human Functional pIC50 = 7.4 7.4 44 2
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 154709 None 0 Human Functional pIC50 = 6.4 6.4 -1 2
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 154709 None 0 Human Functional pIC50 = 6.4 6.4 -1 2
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 108243 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
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 108243 None 0 Human Functional pIC50 = 6.4 6.4 -2 2
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 66085 None 0 Human Functional pIC50 = 5.4 5.4 -204 2
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 66085 None 0 Human Functional pIC50 = 5.4 5.4 -204 2
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 4969 None 0 Human Functional pIC50 = 7.3 7.3 1 2
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 4969 None 0 Human Functional pIC50 = 7.3 7.3 1 2
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 5369 None 0 Human Functional pIC50 = 7.3 7.3 -1 2
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 5369 None 0 Human Functional pIC50 = 7.3 7.3 -1 2
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 2332 None 49 Human Functional pIC50 = 8.3 8.3 -4 5
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 2332 None 49 Human Functional pIC50 = 8.3 8.3 -4 5
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 2332 None 49 Human Functional pIC50 = 8.3 8.3 -4 5
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 2332 None 49 Human Functional pIC50 = 8.3 8.3 -4 5
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 94248 None 8 Human Functional pIC50 = 7.3 7.3 -3 4
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 94248 None 8 Human Functional pIC50 = 7.3 7.3 -3 4
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 63058 None 1 Human Functional pIC50 = 6.2 6.2 -26 4
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 63058 None 1 Human Functional pIC50 = 6.2 6.2 -26 4
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 57479 None 0 Human Functional pIC50 = 7.2 7.2 -37 3
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 57479 None 0 Human Functional pIC50 = 7.2 7.2 -37 3
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 165647 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 165647 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 66086 None 0 Human Functional pIC50 = 6.2 6.2 -74 2
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 66086 None 0 Human Functional pIC50 = 6.2 6.2 -74 2
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 94551 None 0 Human Functional pIC50 = 6.1 6.1 -7 2
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 94551 None 0 Human Functional pIC50 = 6.1 6.1 -7 2
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 171631 None 0 Human Functional pIC50 = 5.1 5.1 -794 4
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 171631 None 0 Human Functional pIC50 = 5.1 5.1 -794 4
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 6729 None 0 Human Functional pIC50 = 6.1 6.1 -20 2
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 6729 None 0 Human Functional pIC50 = 6.1 6.1 -20 2
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 66081 None 13 Human Functional pIC50 = 5.1 5.1 -102 2
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 66081 None 13 Human Functional pIC50 = 5.1 5.1 -102 2
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 4969 None 0 Human Functional pIC50 = 8.1 8.1 1 2
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 4969 None 0 Human Functional pIC50 = 8.1 8.1 1 2
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 192578 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 192578 None 0 Human Functional pIC50 = 8.0 8.0 - 1
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 2332 None 49 Human Functional pIC50 = 7.0 7.0 -4 5
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 190235 None 1 Human Functional pIC50 = 7.0 7.0 - 1
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 190235 None 1 Human Functional pIC50 = 7.0 7.0 - 1
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 160159 None 0 Rat Functional pKd = 8.0 8.0 - 0
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 160159 None 0 Rat Functional pKd = 8.0 8.0 - 0
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 79720 None 0 Pig Functional pKd = 7 7.0 - 0
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 79720 None 0 Pig Functional pKd = 7 7.0 - 0
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 212836 None 0 Rat Functional pKd = 7 7.0 - 0
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 97112 None 0 Rat Functional pKd = 7.9 7.9 - 0
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 97112 None 0 Rat Functional pKd = 7.9 7.9 - 0
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 156088 None 0 Rat Functional pKd = 7.8 7.8 - 0
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 156088 None 0 Rat Functional pKd = 7.8 7.8 - 0
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 212299 None 0 Rat Functional pKd = 7.8 7.8 - 0
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 212301 None 0 Rat Functional pKd = 7.7 7.7 - 0
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 212300 None 0 Rat Functional pKd = 7.7 7.7 - 0
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 97378 None 0 Rat Functional pKd = 6.6 6.6 - 0
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 97378 None 0 Rat Functional pKd = 6.6 6.6 - 0
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 212839 None 0 Rat Functional pKd = 7.4 7.4 - 0
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 160735 None 0 Rat Functional pKd = 7.2 7.2 - 0
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 160735 None 0 Rat Functional pKd = 7.2 7.2 - 0
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 212835 None 0 Rat Functional pKd = 7.2 7.2 - 0
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 212837 None 0 Rat Functional pKd = 5.2 5.2 - 0
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 157654 None 0 Rat Functional pKd = 8.1 8.1 - 0
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 157654 None 0 Rat Functional pKd = 8.1 8.1 - 0
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 168330 None 0 Pig Functional pKi = 8.9 8.9 - 0
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 168330 None 0 Pig Functional pKi = 8.9 8.9 - 0
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 212667 None 0 Pig Functional pKi = 8.8 8.8 - 0
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 186934 None 0 Human Functional pKi = 6 6.0 - 0
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 186934 None 0 Human Functional pKi = 6 6.0 - 0
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 178688 None 0 Human Functional pKi = 7.0 7.0 - 0
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 178688 None 0 Human Functional pKi = 7.0 7.0 - 0
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 112624 None 0 Human Functional pKi = 8.0 8.0 - 0
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 112624 None 0 Human Functional pKi = 8.0 8.0 - 0
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 201567 None 0 Human Functional pKi = 5.9 5.9 - 0
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 201567 None 0 Human Functional pKi = 5.9 5.9 - 0
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 111625 None 0 Human Functional pKi = 7.9 7.9 - 0
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 111625 None 0 Human Functional pKi = 7.9 7.9 - 0
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 209902 None 0 Human Functional pKi = 7.9 7.9 - 0
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 209902 None 0 Human Functional pKi = 7.9 7.9 - 0
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 175990 None 0 Human Functional pKi = 5.9 5.9 - 0
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 175990 None 0 Human Functional pKi = 5.9 5.9 - 0
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 132637 None 0 Pig Functional pKi = 7.9 7.9 - 0
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 132637 None 0 Pig Functional pKi = 7.9 7.9 - 0
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 112583 None 0 Human Functional pKi = 7.8 7.8 - 0
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 112583 None 0 Human Functional pKi = 7.8 7.8 - 0
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 209850 None 0 Human Functional pKi = 7.8 7.8 - 0
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 209850 None 0 Human Functional pKi = 7.8 7.8 - 0
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 178687 None 0 Human Functional pKi = 6.8 6.8 - 0
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 178687 None 0 Human Functional pKi = 6.8 6.8 - 0
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 13003 None 0 Human Functional pKi = 7.8 7.8 - 0
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 13003 None 0 Human Functional pKi = 7.8 7.8 - 0
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 13003 None 0 Human Functional pKi = 7.8 7.8 - 0
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 78378 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78378 None 0 Human Functional pKi = 6.8 6.8 - 0
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 78378 None 0 Human Functional pKi = 6.8 6.8 - 0
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 168109 None 0 Human Functional pKi = 8.7 8.7 - 0
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 168109 None 0 Human Functional pKi = 8.7 8.7 - 0
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 209803 None 0 Human Functional pKi = 8.7 8.7 - 0
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 209803 None 0 Human Functional pKi = 8.7 8.7 - 0
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 128268 None 0 Pig Functional pKi = 8.6 8.6 - 0
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 128268 None 0 Pig Functional pKi = 8.6 8.6 - 0
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 158538 None 0 Pig Functional pKi = 8.6 8.6 - 0
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 158538 None 0 Pig Functional pKi = 8.6 8.6 - 0
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 89513 None 0 Pig Functional pKi = 8.5 8.5 - 0
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 89513 None 0 Pig Functional pKi = 8.5 8.5 - 0
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 111489 None 0 Human Functional pKi = 7.7 7.7 - 0
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 111489 None 0 Human Functional pKi = 7.7 7.7 - 0
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 112632 None 0 Human Functional pKi = 7.7 7.7 - 0
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 112632 None 0 Human Functional pKi = 7.7 7.7 - 0
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 2332 None 49 Human Functional pKi = 7.6 7.6 -4 5
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 2332 None 49 Human Functional pKi = 7.6 7.6 -4 5
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 2332 None 49 Human Functional pKi = 7.6 7.6 -4 5
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 2332 None 49 Human Functional pKi = 7.6 7.6 -4 5
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 209769 None 0 Human Functional pKi = 7.6 7.6 - 0
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 209769 None 0 Human Functional pKi = 7.6 7.6 - 0
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 127972 None 0 Pig Functional pKi = 7.6 7.6 - 0
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 127972 None 0 Pig Functional pKi = 7.6 7.6 - 0
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 8265 None 0 Human Functional pKi = 5.6 5.6 - 0
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 8265 None 0 Human Functional pKi = 5.6 5.6 - 0
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 8436 None 0 Human Functional pKi = 5.6 5.6 - 0
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 8436 None 0 Human Functional pKi = 5.6 5.6 - 0
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 175991 None 0 Human Functional pKi = 6.6 6.6 - 0
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 175991 None 0 Human Functional pKi = 6.6 6.6 - 0
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 203509 None 0 Human Functional pKi = 5.6 5.6 - 0
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 203509 None 0 Human Functional pKi = 5.6 5.6 - 0
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 7998 None 0 Human Functional pKi = 5.6 5.6 - 0
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 7998 None 0 Human Functional pKi = 5.6 5.6 - 0
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 112219 None 0 Human Functional pKi = 8.5 8.5 - 0
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 112219 None 0 Human Functional pKi = 8.5 8.5 - 0
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 212675 None 0 Pig Functional pKi = 8.5 8.5 - 0
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 212670 None 0 Pig Functional pKi = 8.4 8.4 - 0
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 141637 None 0 Pig Functional pKi = 8.4 8.4 - 0
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 141637 None 0 Pig Functional pKi = 8.4 8.4 - 0
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 112801 None 0 Human Functional pKi = 6.5 6.5 - 0
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 112801 None 0 Human Functional pKi = 6.5 6.5 - 0
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 3420 None 2 Human Functional pKi = 8.4 8.4 - 0
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 3420 None 2 Human Functional pKi = 8.4 8.4 - 0
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 3420 None 2 Human Functional pKi = 8.4 8.4 - 0
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 210270 None 0 Human Functional pKi = 7.4 7.4 - 0
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 210270 None 0 Human Functional pKi = 7.4 7.4 - 0
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 210367 None 0 Human Functional pKi = 7.4 7.4 - 0
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 210367 None 0 Human Functional pKi = 7.4 7.4 - 0
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 158944 None 0 Pig Functional pKi = 7.4 7.4 - 0
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 158944 None 0 Pig Functional pKi = 7.4 7.4 - 0
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 106666 None 0 Human Functional pKi = 8.3 8.3 - 0
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 106666 None 0 Human Functional pKi = 8.3 8.3 - 0
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 89501 None 0 Pig Functional pKi = 8.2 8.2 - 0
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 89501 None 0 Pig Functional pKi = 8.2 8.2 - 0
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 178686 None 0 Human Functional pKi = 6.3 6.3 - 0
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 178686 None 0 Human Functional pKi = 6.3 6.3 - 0
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 189833 None 0 Human Functional pKi = 6.3 6.3 - 0
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 189833 None 0 Human Functional pKi = 6.3 6.3 - 0
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 111466 None 0 Human Functional pKi = 8.2 8.2 - 0
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 111466 None 0 Human Functional pKi = 8.2 8.2 - 0
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 168951 None 0 Pig Functional pKi = 8.2 8.2 - 0
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 168951 None 0 Pig Functional pKi = 8.2 8.2 - 0
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 175499 None 0 Human Functional pKi = 7.2 7.2 - 0
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 175499 None 0 Human Functional pKi = 7.2 7.2 - 0
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 193086 None 0 Human Functional pKi = 5.2 5.2 - 0
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 193086 None 0 Human Functional pKi = 5.2 5.2 - 0
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 112370 None 0 Human Functional pKi = 7.2 7.2 - 0
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 112370 None 0 Human Functional pKi = 7.2 7.2 - 0
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 164372 None 0 Human Functional pKi = 7.2 7.2 - 0
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 164372 None 0 Human Functional pKi = 7.2 7.2 - 0
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 2983 None 40 Human Functional pEC50 = 8.2 8.2 -25 5
NoneNone
Drug Central None None None None None
2174 2983 None 40 Human Functional pEC50 = 8.2 8.2 -25 5
NoneNone
Drug Central None None None None None
2176 2983 None 40 Human Functional pEC50 = 8.2 8.2 -25 5
NoneNone
Drug Central None None None None None
439302 2983 None 40 Human Functional pEC50 = 8.2 8.2 -25 5
NoneNone
Drug Central None None None None None
439302.0 2983 None 40 Human Functional pEC50 = 8.2 8.2 -25 5
NoneNone
Drug Central None None None None None
CHEMBL395429 2983 None 40 Human Functional pEC50 = 8.2 8.2 -25 5
NoneNone
Drug Central None None None None None
DB00107 2983 None 40 Human Functional pEC50 = 8.2 8.2 -25 5
NoneNone
Drug Central None None None None None
5280343 188382 None 69 Human Functional pIC50 = 8.3 8.3 -31 12
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 188382 None 69 Human Functional pIC50 = 8.3 8.3 -31 12
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 188382 None 69 Human Functional pIC50 = 8.3 8.3 -31 12
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 4781 None 63 Human Functional pIC50 = 8.3 8.3 -16 44
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 4781 None 63 Human Functional pIC50 = 8.3 8.3 -16 44
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 205667 None 50 Human Functional pIC50 = 8.2 8.2 -2 4
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 205667 None 50 Human Functional pIC50 = 8.2 8.2 -2 4
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 205667 None 50 Human Functional pIC50 = 8.2 8.2 -2 4
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 4004 None 22 Human Functional pIC50 = 7.1 7.1 3 4
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621
5311500 4004 None 22 Human Functional pIC50 = 7.1 7.1 3 4
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621
CHEMBL363910 4004 None 22 Human Functional pIC50 = 7.1 7.1 3 4
UnclassifiedUnclassified
Guide to Pharmacology 402 2 0 4 4.8 Cc1ccn(n1)c1ccc(c(c1)Cl)C(=O)N1Cc2cccn2Cc2c1cccc2 16297621




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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3686 94720 None 64 Human Binding pAC50 = 5.0 5.0 - 0
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 94720 None 64 Human Binding pAC50 = 5.0 5.0 - 0
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 11852 None 18 Human Binding pAC50 = 4.9 4.9 - 12
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 11852 None 18 Human Binding pAC50 = 4.9 4.9 - 12
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 11852 None 18 Human Binding pAC50 = 4.9 4.9 - 12
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 11852 None 18 Human Binding pAC50 = 4.9 4.9 - 12
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 31229 None 62 Human Binding pAC50 = 4.9 4.9 - 0
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 31229 None 62 Human Binding pAC50 = 4.9 4.9 - 0
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 3779 None 53 Human Binding pAC50 = 4.8 4.8 - 13
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 3779 None 53 Human Binding pAC50 = 4.8 4.8 - 13
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 3779 None 53 Human Binding pAC50 = 4.8 4.8 - 13
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 3779 None 53 Human Binding pAC50 = 4.8 4.8 - 13
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 3779 None 53 Human Binding pAC50 = 4.8 4.8 - 13
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 111644 None 40 Human Binding pAC50 = 4.8 4.8 - 0
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 111644 None 40 Human Binding pAC50 = 4.8 4.8 - 0
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 120312 None 42 Human Binding pAC50 = 4.8 4.8 - 0
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 120312 None 42 Human Binding pAC50 = 4.8 4.8 - 0
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 3860 None 43 Human Binding pAC50 = 4.7 4.7 - 29
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 3860 None 43 Human Binding pAC50 = 4.7 4.7 - 29
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 3860 None 43 Human Binding pAC50 = 4.7 4.7 - 29
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
5566.0 3860 None 43 Human Binding pAC50 = 4.7 4.7 - 29
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 3860 None 43 Human Binding pAC50 = 4.7 4.7 - 29
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 3860 None 43 Human Binding pAC50 = 4.7 4.7 - 29
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 3860 None 43 Human Binding pAC50 = 4.7 4.7 - 29
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 938 None 48 Human Binding pAC50 = 4.7 4.7 - 15
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
156419.0 938 None 48 Human Binding pAC50 = 4.7 4.7 - 15
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 938 None 48 Human Binding pAC50 = 4.7 4.7 - 15
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
647 938 None 48 Human Binding pAC50 = 4.7 4.7 - 15
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 938 None 48 Human Binding pAC50 = 4.7 4.7 - 15
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 938 None 48 Human Binding pAC50 = 4.7 4.7 - 15
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 207985 None 33 Human Binding pAC50 = 4.7 4.7 - 25
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 207985 None 33 Human Binding pAC50 = 4.7 4.7 - 25
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 207985 None 33 Human Binding pAC50 = 4.7 4.7 - 25
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 3806 None 35 Human Binding pAC50 = 4.7 4.7 - 25
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 3806 None 35 Human Binding pAC50 = 4.7 4.7 - 25
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 3806 None 35 Human Binding pAC50 = 4.7 4.7 - 25
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
941651.0 3806 None 35 Human Binding pAC50 = 4.7 4.7 - 25
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 3806 None 35 Human Binding pAC50 = 4.7 4.7 - 25
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 3806 None 35 Human Binding pAC50 = 4.7 4.7 - 25
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 3773 None 26 Human Binding pAC50 = 4.7 4.7 - 19
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 3773 None 26 Human Binding pAC50 = 4.7 4.7 - 19
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 3773 None 26 Human Binding pAC50 = 4.7 4.7 - 19
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 100270 None 65 Human Binding pAC50 = 4.7 4.7 - 0
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 100270 None 65 Human Binding pAC50 = 4.7 4.7 - 0
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 63562 None 59 Human Binding pAC50 = 4.7 4.7 - 0
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 63562 None 59 Human Binding pAC50 = 4.7 4.7 - 0
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 1664 None 37 Human Binding pAC50 = 4.6 4.6 - 32
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 1664 None 37 Human Binding pAC50 = 4.6 4.6 - 32
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
3396.0 1664 None 37 Human Binding pAC50 = 4.6 4.6 - 32
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 1664 None 37 Human Binding pAC50 = 4.6 4.6 - 32
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 1664 None 37 Human Binding pAC50 = 4.6 4.6 - 32
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 1664 None 37 Human Binding pAC50 = 4.6 4.6 - 32
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 3125 None 49 Human Binding pAC50 = 4.6 4.6 - 29
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
16362.0 3125 None 49 Human Binding pAC50 = 4.6 4.6 - 29
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 3125 None 49 Human Binding pAC50 = 4.6 4.6 - 29
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 3125 None 49 Human Binding pAC50 = 4.6 4.6 - 29
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 3125 None 49 Human Binding pAC50 = 4.6 4.6 - 29
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 3125 None 49 Human Binding pAC50 = 4.6 4.6 - 29
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 None 60 Human Binding pAC50 = 4.6 4.6 - 28
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 None 60 Human Binding pAC50 = 4.6 4.6 - 28
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 None 60 Human Binding pAC50 = 4.6 4.6 - 28
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
2170.0 403 None 60 Human Binding pAC50 = 4.6 4.6 - 28
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 None 60 Human Binding pAC50 = 4.6 4.6 - 28
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 None 60 Human Binding pAC50 = 4.6 4.6 - 28
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 55132 None 30 Human Binding pAC50 = 4.6 4.6 - 0
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 55132 None 30 Human Binding pAC50 = 4.6 4.6 - 0
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 198991 None 63 Human Binding pAC50 = 4.6 4.6 - 30
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 198991 None 63 Human Binding pAC50 = 4.6 4.6 - 30
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 3590 None 59 Human Binding pAC50 = 4.6 4.6 - 48
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 3590 None 59 Human Binding pAC50 = 4.6 4.6 - 48
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 3590 None 59 Human Binding pAC50 = 4.6 4.6 - 48
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 3590 None 59 Human Binding pAC50 = 4.6 4.6 - 48
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 3590 None 59 Human Binding pAC50 = 4.6 4.6 - 48
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 None 47 Human Binding pAC50 = 4.6 4.6 - 31
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 None 47 Human Binding pAC50 = 4.6 4.6 - 31
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
2157.0 398 None 47 Human Binding pAC50 = 4.6 4.6 - 31
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 None 47 Human Binding pAC50 = 4.6 4.6 - 31
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 None 47 Human Binding pAC50 = 4.6 4.6 - 31
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 None 47 Human Binding pAC50 = 4.6 4.6 - 31
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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
189562.0 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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
71301.0 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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
9844194.0 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 2757 None 41 Human Binding pAC50 = 4.5 4.5 - 4
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 137055 None 20 Human Binding pAC50 = 4.5 4.5 - 0
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 137055 None 20 Human Binding pAC50 = 4.5 4.5 - 0
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 137055 None 20 Human Binding pAC50 = 4.5 4.5 - 0
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 2483 None 21 Human Binding pAC50 = 4.5 4.5 - 2
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 2483 None 21 Human Binding pAC50 = 4.5 4.5 - 2
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 2483 None 21 Human Binding pAC50 = 4.5 4.5 - 2
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 2483 None 21 Human Binding pAC50 = 4.5 4.5 - 2
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 17999 None 26 Human Binding pAC50 = 4.5 4.5 - 5
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 17999 None 26 Human Binding pAC50 = 4.5 4.5 - 5
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 14508 None 49 Human Binding pAC50 = 4.4 4.4 - 0
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 14508 None 49 Human Binding pAC50 = 4.4 4.4 - 0
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 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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
5311010.0 518 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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
68613.0 518 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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 None 30 Human Binding pAC50 = 5.4 5.4 -660 5
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 207729 None 57 Human Binding pAC50 = 5.4 5.4 - 0
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 207729 None 57 Human Binding pAC50 = 5.4 5.4 - 0
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 207729 None 57 Human Binding pAC50 = 5.4 5.4 - 0
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 207729 None 57 Human Binding pAC50 = 5.4 5.4 - 0
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 207729 None 57 Human Binding pAC50 = 5.4 5.4 - 0
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 207729 None 57 Human Binding pAC50 = 5.4 5.4 - 0
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 207729 None 57 Human Binding pAC50 = 5.4 5.4 - 0
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 194838 None 50 Human Binding pAC50 = 5.3 5.3 - 0
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 194838 None 50 Human Binding pAC50 = 5.3 5.3 - 0
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 14498 None 13 Human Binding pAC50 = 5.2 5.2 - 0
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 14498 None 13 Human Binding pAC50 = 5.2 5.2 - 0
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 14498 None 13 Human Binding pAC50 = 5.2 5.2 - 0
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 14498 None 13 Human Binding pAC50 = 5.2 5.2 - 0
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 12618 None 11 Human Binding pAC50 = 5.1 5.1 - 0
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 12618 None 11 Human Binding pAC50 = 5.1 5.1 - 0
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 35070 None 5 Human Binding pAC50 = 5 5.0 - 0
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 35070 None 5 Human Binding pAC50 = 5 5.0 - 0
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 35070 None 5 Human Binding pAC50 = 5 5.0 - 0
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 3976 None 29 Human Binding pEC50 = 10.3 10.3 -15 9
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 3976 None 29 Human Binding pEC50 = 10.3 10.3 -15 9
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 3976 None 29 Human Binding pEC50 = 10.3 10.3 -15 9
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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
644077.0 3976 None 29 Human Binding pEC50 = 10.3 10.3 -15 9
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 3976 None 29 Human Binding pEC50 = 10.3 10.3 -15 9
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 3976 None 29 Human Binding pEC50 = 10.3 10.3 -15 9
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 1331 None 29 Human Binding pEC50 = 9.7 9.7 -12 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 1331 None 29 Human Binding pEC50 = 9.7 9.7 -12 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 1331 None 29 Human Binding pEC50 = 9.7 9.7 -12 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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
27991.0 1331 None 29 Human Binding pEC50 = 9.7 9.7 -12 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 1331 None 29 Human Binding pEC50 = 9.7 9.7 -12 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 1331 None 29 Human Binding pEC50 = 9.7 9.7 -12 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 1331 None 29 Human Binding pEC50 = 9.7 9.7 -12 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115809 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115809 None 0 Human Binding pEC50 = 8.7 8.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115817 None 0 Human Binding pEC50 = 7 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115817 None 0 Human Binding pEC50 = 7 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115820 None 0 Human Binding pEC50 = 7 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115820 None 0 Human Binding pEC50 = 7 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115924 None 0 Human Binding pEC50 = 7 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115924 None 0 Human Binding pEC50 = 7 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 64576 None 0 Human Binding pEC50 = 7 7.0 - 0
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 64576 None 0 Human Binding pEC50 = 7 7.0 - 0
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 115913 None 0 Human Binding pEC50 = 6 6.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115913 None 0 Human Binding pEC50 = 6 6.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115816 None 0 Human Binding pEC50 = 8.0 8.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115816 None 0 Human Binding pEC50 = 8.0 8.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115911 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115911 None 0 Human Binding pEC50 = 7.0 7.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115903 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115903 None 0 Human Binding pEC50 = 6.0 6.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 123882 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 123882 None 0 Human Binding pEC50 = 6.0 6.0 - 0
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 115910 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115910 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 169606 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 169606 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 115904 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115904 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 126270 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 126270 None 0 Human Binding pEC50 = 5.9 5.9 - 0
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 115914 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115914 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115921 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115921 None 0 Human Binding pEC50 = 6.9 6.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115899 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115899 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115900 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115900 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115922 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115922 None 0 Human Binding pEC50 = 5.9 5.9 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115906 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115906 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115923 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115923 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115919 None 0 Human Binding pEC50 = 5.8 5.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115919 None 0 Human Binding pEC50 = 5.8 5.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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
165708555.0 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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
16681432.0 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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
495 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 797 None 33 Human Binding pEC50 = 6.8 6.8 -1 2
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115828 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115828 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115908 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115908 None 0 Human Binding pEC50 = 7.8 7.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115827 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115827 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115831 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115831 None 0 Human Binding pEC50 = 6.8 6.8 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 66296 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 66296 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 66382 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 66382 None 0 Human Binding pEC50 = 5.8 5.8 - 0
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 65247 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 65247 None 0 Human Binding pEC50 = 6.7 6.7 - 0
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 115909 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115909 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115917 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115917 None 0 Human Binding pEC50 = 6.7 6.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115912 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115912 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115898 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115898 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 123902 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 123902 None 0 Human Binding pEC50 = 6.6 6.6 - 0
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 115926 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115926 None 0 Human Binding pEC50 = 6.6 6.6 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115578 None 0 Human Binding pEC50 = 5.6 5.6 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115578 None 0 Human Binding pEC50 = 5.6 5.6 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 169078 None 10 Human Binding pEC50 = 8.5 8.5 - 1
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 169078 None 10 Human Binding pEC50 = 8.5 8.5 - 1
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115823 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115823 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115927 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115927 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115925 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115925 None 0 Human Binding pEC50 = 5.5 5.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115920 None 5 Human Binding pEC50 = 6.5 6.5 - 1
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115920 None 5 Human Binding pEC50 = 6.5 6.5 - 1
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115821 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115821 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115808 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115808 None 0 Human Binding pEC50 = 7.5 7.5 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115915 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115915 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 2230 None 35 Human Binding pEC50 = 4.4 4.4 -10000 5
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 2230 None 35 Human Binding pEC50 = 4.4 4.4 -10000 5
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 2230 None 35 Human Binding pEC50 = 4.4 4.4 -10000 5
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 115829 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115829 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 4004 None 22 Human Binding pEC50 = 7.4 7.4 3 3
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 4004 None 22 Human Binding pEC50 = 7.4 7.4 3 3
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 4004 None 22 Human Binding pEC50 = 7.4 7.4 3 3
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 115806 None 0 Human Binding pEC50 = 8.4 8.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115806 None 0 Human Binding pEC50 = 8.4 8.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115812 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115812 None 0 Human Binding pEC50 = 7.4 7.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115813 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115813 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115814 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115814 None 0 Human Binding pEC50 = 6.4 6.4 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115832 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115832 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115905 None 0 Human Binding pEC50 = 6.3 6.3 - 1
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115905 None 0 Human Binding pEC50 = 6.3 6.3 - 1
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115902 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115902 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115918 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115918 None 0 Human Binding pEC50 = 7.3 7.3 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115818 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115818 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115833 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115833 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 170951 None 0 Human Binding pEC50 = 6.2 6.2 - 0
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 170951 None 0 Human Binding pEC50 = 6.2 6.2 - 0
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 115896 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115896 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115830 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115830 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115811 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115811 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115822 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115822 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115810 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115810 None 0 Human Binding pEC50 = 6.2 6.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 2983 None 40 Human Binding pEC50 = 8.1 8.1 -831 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 2983 None 40 Human Binding pEC50 = 8.1 8.1 -831 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 2983 None 40 Human Binding pEC50 = 8.1 8.1 -831 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 2983 None 40 Human Binding pEC50 = 8.1 8.1 -831 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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
439302.0 2983 None 40 Human Binding pEC50 = 8.1 8.1 -831 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 2983 None 40 Human Binding pEC50 = 8.1 8.1 -831 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 2983 None 40 Human Binding pEC50 = 8.1 8.1 -831 8
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 203691 None 0 Human Binding pEC50 = 8.1 8.1 2 3
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 203691 None 0 Human Binding pEC50 = 8.1 8.1 2 3
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 115901 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115901 None 0 Human Binding pEC50 = 7.2 7.2 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115916 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115916 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115907 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115907 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115928 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115928 None 0 Human Binding pEC50 = 6.1 6.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115815 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115815 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115826 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115826 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115819 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115819 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115825 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115825 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115824 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115824 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 122996 None 20 Human Binding pEC50 = 6.1 6.1 - 8
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 122996 None 20 Human Binding pEC50 = 6.1 6.1 - 8
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 122996 None 20 Human Binding pEC50 = 6.1 6.1 - 8
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 122996 None 20 Human Binding pEC50 = 6.1 6.1 - 8
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 115897 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115897 None 0 Human Binding pEC50 = 7.1 7.1 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 127357 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 127357 None 0 Human Binding pEC50 = 6.1 6.1 - 0
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 115807 None 0 Human Binding pEC50 = 8 8.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 115807 None 0 Human Binding pEC50 = 8 8.0 - 0
Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by 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 4535 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 4535 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 2332 None 49 Rat Binding pIC50 = 9.3 9.3 - 2
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 2332 None 49 Rat Binding pIC50 = 9.3 9.3 - 2
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 2332 None 49 Rat Binding pIC50 = 9.3 9.3 - 2
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 2332 None 49 Rat Binding pIC50 = 9.3 9.3 - 2
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 105476 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 105476 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 163574 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 163574 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 187450 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 187450 None 0 Human Binding pIC50 = 9.2 9.2 - 0
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 57479 None 0 Rat Binding pIC50 = 9 9.0 - 0
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 57479 None 0 Rat Binding pIC50 = 9 9.0 - 0
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 146840 None 0 Human Binding pIC50 = 9 9.0 - 0
Cellular in Vitro Assay: On the 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 146840 None 0 Human Binding pIC50 = 9 9.0 - 0
Cellular in Vitro Assay: On the 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 177123 None 0 Rat Binding pIC50 = 9 9.0 - 0
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 177123 None 0 Rat Binding pIC50 = 9 9.0 - 0
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 104542 None 0 Human Binding pIC50 = 9 9.0 - 0
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 104542 None 0 Human Binding pIC50 = 9 9.0 - 0
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 2332 None 49 Human Binding pIC50 = 9 9.0 64 2
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 2332 None 49 Human Binding pIC50 = 9 9.0 64 2
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 2332 None 49 Human Binding pIC50 = 9 9.0 64 2
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 2332 None 49 Human Binding pIC50 = 9 9.0 64 2
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 161832 None 0 Rat Binding pIC50 = 9 9.0 - 0
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 161832 None 0 Rat Binding pIC50 = 9 9.0 - 0
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 130757 None 0 Human Binding pIC50 = 9 9.0 - 0
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 130757 None 0 Human Binding pIC50 = 9 9.0 - 0
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 102085 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
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 102085 None 0 Rat Binding pIC50 = 9.0 9.0 - 0
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 119731 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
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 119731 None 0 Rat Binding pIC50 = 8.9 8.9 - 0
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 2332 None 49 Human Binding pIC50 = 8.9 8.9 64 2
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 57435 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 57435 None 0 Human Binding pIC50 = 8.9 8.9 - 0
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 151892 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Cellular In Vitro Assay: On the 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 151892 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Cellular In Vitro Assay: On the 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 52667 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
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 52667 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
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 148637 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Cellular In Vitro Assay: On the 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 148637 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Cellular In Vitro Assay: On the 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 206231 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 206231 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 206231 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
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 206231 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
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 101775 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
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 101775 None 0 Rat Binding pIC50 = 8.8 8.8 - 0
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 120167 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 120167 None 0 Human Binding pIC50 = 8.8 8.8 - 0
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 101969 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
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 101969 None 0 Rat Binding pIC50 = 8.7 8.7 - 0
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 207854 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 207854 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 208027 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 208027 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 108243 None 0 Human Binding pIC50 = 8 8.0 - 0
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 108243 None 0 Human Binding pIC50 = 8 8.0 - 0
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 146761 None 0 Human Binding pIC50 = 8 8.0 - 0
Cellular in Vitro Assay: On the 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 146761 None 0 Human Binding pIC50 = 8 8.0 - 0
Cellular in Vitro Assay: On the 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 5173 None 0 Human Binding pIC50 = 8 8.0 4 2
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 5173 None 0 Human Binding pIC50 = 8 8.0 4 2
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 60460 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 60460 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 60820 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 60820 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 61799 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 61799 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 131425 None 0 Human Binding pIC50 = 8 8.0 - 0
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 131425 None 0 Human Binding pIC50 = 8 8.0 - 0
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 206746 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 206746 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 115185 None 0 Human Binding pIC50 = 7 7.0 - 0
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 115185 None 0 Human Binding pIC50 = 7 7.0 - 0
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 151868 None 0 Human Binding pIC50 = 7 7.0 - 0
Cellular In Vitro Assay: On the 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 151868 None 0 Human Binding pIC50 = 7 7.0 - 0
Cellular In Vitro Assay: On the 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 128739 None 0 Rat Binding pIC50 = 7 7.0 - 0
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 128739 None 0 Rat Binding pIC50 = 7 7.0 - 0
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 132423 None 0 Rat Binding pIC50 = 7 7.0 - 0
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 132423 None 0 Rat Binding pIC50 = 7 7.0 - 0
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 12791 None 0 Rat Binding pIC50 = 6 6.0 - 0
Displacement of [3H]-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 12791 None 0 Rat Binding pIC50 = 6 6.0 - 0
Displacement of [3H]-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 14037 None 0 Rat Binding pIC50 = 6 6.0 - 0
Displacement of [3H]-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 14037 None 0 Rat Binding pIC50 = 6 6.0 - 0
Displacement of [3H]-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 89960 None 0 Human Binding pIC50 = 6 6.0 - 0
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 89960 None 0 Human Binding pIC50 = 6 6.0 - 0
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 90221 None 0 Human Binding pIC50 = 6 6.0 - 0
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 90221 None 0 Human Binding pIC50 = 6 6.0 - 0
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 119311 None 0 Human Binding pIC50 = 6 6.0 - 0
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 119311 None 0 Human Binding pIC50 = 6 6.0 - 0
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 18906 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 18906 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 18964 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 18964 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 19391 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 19391 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 21176 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 21176 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 21525 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 21525 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 116835 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 116835 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 117121 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 117121 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 168655 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 168655 None 0 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 98369 None 0 Rat Binding pIC50 = 4 4.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 98369 None 0 Rat Binding pIC50 = 4 4.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 211994 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 107357 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 107357 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 164260 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 164260 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 150153 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Cellular In Vitro Assay: On the 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 150153 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Cellular In Vitro Assay: On the 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 145705 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Cellular in Vitro Assay: On the 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 145705 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Cellular in Vitro Assay: On the 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 165647 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 165647 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 146740 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 146740 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 11730 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 11730 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 11730 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 142542 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Cellular In Vitro Assay: On the 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 142542 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Cellular In Vitro Assay: On the 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 113568 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-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 113568 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-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 94150 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 94150 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 214061 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
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 146287 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Cellular In Vitro Assay: On the 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 146287 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Cellular In Vitro Assay: On the 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 211694 None 0 Rat Binding pIC50 = 6.0 6.0 - 2
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 98848 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
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 98848 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
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 18883 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 18883 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 117339 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 117339 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 120309 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
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 120309 None 0 Pig Binding pIC50 = 5.0 5.0 - 0
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 211141 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
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 214062 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
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 22126 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 22126 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 99238 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
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 99238 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 21389 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 21389 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 145985 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular In Vitro Assay: On the 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 145985 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular In Vitro Assay: On the 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 153817 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular In Vitro Assay: On the 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 153817 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular In Vitro Assay: On the 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 2606 None 50 Rat Binding pIC50 = 7.9 7.9 -1 8
Displacement of [3H]-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 2606 None 50 Rat Binding pIC50 = 7.9 7.9 -1 8
Displacement of [3H]-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 2606 None 50 Rat Binding pIC50 = 7.9 7.9 -1 8
Displacement of [3H]-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 2606 None 50 Rat Binding pIC50 = 7.9 7.9 -1 8
Displacement of [3H]-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 57531 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 57531 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 120102 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 120102 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 26547 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 26547 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 151884 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Cellular in Vitro Assay: On the 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 151884 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Cellular in Vitro Assay: On the 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 11727 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-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 11727 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-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 212350 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
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 18903 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 18903 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 21134 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 21134 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 78528 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 78528 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 89483 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 89483 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 151715 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular In Vitro Assay: On the 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 151715 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular In Vitro Assay: On the 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 147125 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular in Vitro Assay: On the 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 147125 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Cellular in Vitro Assay: On the 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 13919 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 13919 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 110435 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 110435 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 57467 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 57467 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 102588 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 102588 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 102791 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 102791 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 26598 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 26598 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 116074 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 116074 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 107526 None 0 Human Binding pIC50 = 7.9 7.9 1 2
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 107526 None 0 Human Binding pIC50 = 7.9 7.9 1 2
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 78902 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 78902 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 120102 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 120102 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 211693 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
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 98668 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
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 98668 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
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 163042 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
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 163042 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
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 18977 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 18977 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 18872 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 18872 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 19055 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 19055 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 116867 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 116867 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 116991 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 116991 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 117555 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 117555 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 113051 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 113051 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 114124 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 114124 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]-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 120107 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 120107 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 207070 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 207070 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 154893 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 154893 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 206358 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 206358 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 207070 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 207070 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 56695 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 56695 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 13966 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]-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 13966 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]-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 56163 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 56163 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 113575 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-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 113575 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]-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 214065 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
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 118530 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 118530 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 118618 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 118618 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 164428 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 164428 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of radioligand [3H]-AVP binding 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 18966 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 18966 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 160861 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Cellular in Vitro Assay: On the 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 160861 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Cellular in Vitro Assay: On the 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 57317 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 57317 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 102278 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
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 102278 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
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 108058 None 0 Human Binding pIC50 = 7.8 7.8 - 1
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 108058 None 0 Human Binding pIC50 = 7.8 7.8 - 1
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 118245 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 118245 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 118245 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 118245 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 151014 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Cellular In Vitro Assay: On the 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 151014 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Cellular In Vitro Assay: On the 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 13854 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-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 13854 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-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 119995 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 119995 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 214091 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 99660 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
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 99660 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
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 117085 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 117085 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 118530 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 118530 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 133629 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 133629 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 21493 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 21493 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 116712 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 116712 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 4781 None 63 Human Binding pIC50 = 4.8 4.8 - 34
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 4781 None 63 Human Binding pIC50 = 4.8 4.8 - 34
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 188382 None 69 Human Binding pIC50 = 4.8 4.8 -147 32
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 188382 None 69 Human Binding pIC50 = 4.8 4.8 -147 32
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 188382 None 69 Human Binding pIC50 = 4.8 4.8 -147 32
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 188382 None 69 Human Binding pIC50 = 4.8 4.8 -147 32
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 188382 None 69 Human Binding pIC50 = 4.8 4.8 -147 32
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 188382 None 69 Human Binding pIC50 = 4.8 4.8 -147 32
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 4781 None 63 Human Binding pIC50 = 4.8 4.8 - 34
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 4781 None 63 Human Binding pIC50 = 4.8 4.8 - 34
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 4246 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 4246 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 115320 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 115320 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 109264 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 109264 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 153267 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Cellular in Vitro Assay: On the 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 153267 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Cellular in Vitro Assay: On the 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 104785 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
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 104785 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
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 27195 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 27195 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 188189 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 188189 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 78900 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 78900 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
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 11879 None 1 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]-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 11879 None 1 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]-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 214067 None 0 Rat Binding pIC50 = 5.8 5.8 - 2
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 21457 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 21457 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 117109 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 117109 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 98672 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
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 98672 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
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 114602 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-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 114602 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-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 120055 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 120055 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 150865 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Cellular In Vitro Assay: On the 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 150865 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Cellular In Vitro Assay: On the 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 114863 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]-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 114863 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]-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 206740 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
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 206740 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
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 215014 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
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 96871 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 96871 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 117091 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 117091 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 168554 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 168554 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 74205 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
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 74205 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
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 2224 None 5 Rat Binding pIC50 = 4.8 4.8 - 2
Inhibition of radioligand [3H]-AVP binding 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 2224 None 5 Rat Binding pIC50 = 4.8 4.8 - 2
Inhibition of radioligand [3H]-AVP binding 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 2224 None 5 Rat Binding pIC50 = 4.8 4.8 - 2
Inhibition of radioligand [3H]-AVP binding 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 163447 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 163447 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 14113 None 0 Rat Binding pIC50 = 7.8 7.8 - 3
Displacement of [3H]-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 14113 None 0 Rat Binding pIC50 = 7.8 7.8 - 3
Displacement of [3H]-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 115191 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 115191 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 94330 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 94330 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 26670 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 26670 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 119363 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 119363 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 113867 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-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 113867 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]-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 119955 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 119955 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 4322 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 4322 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 119489 None 3 Human Binding pIC50 = 6.8 6.8 - 1
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 119489 None 3 Human Binding pIC50 = 6.8 6.8 - 1
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 13767 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]-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 13767 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Displacement of [3H]-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 18876 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 18876 None 0 Rat Binding pIC50 = 5.8 5.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 116929 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 116929 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of radioligand [3H]-AVP binding 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 75077 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 75077 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 53173 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 53173 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 101461 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 101461 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 115292 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 115292 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 107546 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 107546 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 12880 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 12880 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 57551 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 57551 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 13796 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]-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 13796 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]-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 117009 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 117009 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 118109 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 118109 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 211702 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
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 149959 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Cellular In Vitro Assay: On the 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 149959 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Cellular In Vitro Assay: On the 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 145281 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Cellular in Vitro Assay: On the 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 145281 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Cellular in Vitro Assay: On the 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 151770 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Cellular in Vitro Assay: On the 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 151770 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Cellular in Vitro Assay: On the 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 104952 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 104952 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 105506 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 105506 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 120155 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 120155 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 132643 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 132643 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 208015 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 208015 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 57424 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 57424 None 0 Human Binding pIC50 = 8.7 8.7 - 0
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 2332 None 49 Rat Binding pIC50 = 8.6 8.6 - 2
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 53166 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
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 53166 None 0 Rat Binding pIC50 = 8.6 8.6 - 0
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 119973 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 119973 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 52667 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 52667 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 21602 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 21602 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 111022 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 111022 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 13469 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-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 13469 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-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 57479 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 57479 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 130756 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 130756 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 131417 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 131417 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 168605 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 168605 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 60460 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 60460 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 167691 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 167691 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 15388 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 15388 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 113127 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 113127 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 60459 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 60459 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 169399 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 169399 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 60820 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 60820 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 211993 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 72500 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 72500 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 118530 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 118530 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 21129 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 21129 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 187551 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 187551 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 11037 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 11037 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]-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 57402 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 57402 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 115490 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 115490 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 13640 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]-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 13640 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Displacement of [3H]-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 18970 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 18970 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 20718 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 20718 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 116967 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 116967 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 18911 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 18911 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 143805 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Cellular in Vitro Assay: On the 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 143805 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Cellular in Vitro Assay: On the 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 12859 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-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 12859 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-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 206746 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 206746 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
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 30639 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 30639 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 120233 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 120233 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 22327 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 22327 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of radioligand [3H]-AVP binding 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 13434 None 2 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]-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 13434 None 2 Rat Binding pIC50 = 4.7 4.7 - 0
Displacement of [3H]-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 107473 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 107473 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 145630 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 145630 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 149166 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 149166 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 151955 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 151955 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 2956 None 18 Rat Binding pIC50 = 6.6 6.6 - 2
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 2956 None 18 Rat Binding pIC50 = 6.6 6.6 - 2
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 2956 None 18 Rat Binding pIC50 = 6.6 6.6 - 2
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 2956 None 18 Rat Binding pIC50 = 6.6 6.6 - 2
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 53392 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 53392 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 78908 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 78908 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 2218 None 2 Rat Binding pIC50 = 5.6 5.6 -208 4
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 2218 None 2 Rat Binding pIC50 = 5.6 5.6 -208 4
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 2218 None 2 Rat Binding pIC50 = 5.6 5.6 -208 4
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 98957 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 98957 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 99598 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 99598 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 98653 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 98653 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 120233 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 120233 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 110474 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 110474 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 188003 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 188003 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 78909 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 78909 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 78910 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 78910 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 78813 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 78813 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 155776 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 155776 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 3976 None 29 Human Binding pIC50 = 6.6 6.6 -15 9
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 3976 None 29 Human Binding pIC50 = 6.6 6.6 -15 9
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 3976 None 29 Human Binding pIC50 = 6.6 6.6 -15 9
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
644077.0 3976 None 29 Human Binding pIC50 = 6.6 6.6 -15 9
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 3976 None 29 Human Binding pIC50 = 6.6 6.6 -15 9
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 3976 None 29 Human Binding pIC50 = 6.6 6.6 -15 9
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 110330 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 110330 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 103730 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 103730 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 13171 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-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 13171 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]-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 135409 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 135409 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 72809 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 72809 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 116759 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 116759 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 168733 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 168733 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 4781 None 63 Human Binding pIC50 = 5.6 5.6 - 34
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 4781 None 63 Human Binding pIC50 = 5.6 5.6 - 34
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 108066 None 0 Human Binding pIC50 = 7.6 7.6 14 2
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 108066 None 0 Human Binding pIC50 = 7.6 7.6 14 2
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 20823 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 20823 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 116756 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 116756 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 144868 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 144868 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 11924 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 11924 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 114979 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 114979 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 78904 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 78904 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 117117 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 117117 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 4781 None 63 Human Binding pIC50 = 5.6 5.6 - 34
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 4781 None 63 Human Binding pIC50 = 5.6 5.6 - 34
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 107318 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 107318 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 153032 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 153032 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Cellular In Vitro Assay: On the 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 14135 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 14135 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]-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 5227 None 0 Human Binding pIC50 = 7.6 7.6 5 2
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 5227 None 0 Human Binding pIC50 = 7.6 7.6 5 2
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 21412 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 21412 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Inhibition of radioligand [3H]-AVP binding 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 71745 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 71745 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
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 11926 None 0 Rat Binding pIC50 = 7.5 7.5 - 2
Displacement of [3H]-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 11926 None 0 Rat Binding pIC50 = 7.5 7.5 - 2
Displacement of [3H]-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 12090 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 12090 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 12946 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 12946 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 113128 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 113128 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 101394 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 101394 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 4452 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 4452 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 206739 None 1 Rat Binding pIC50 = 7.5 7.5 - 0
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 206739 None 1 Rat Binding pIC50 = 7.5 7.5 - 0
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 207015 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 207015 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 187453 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 187453 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 78903 None 0 Rat Binding pIC50 = 6.5 6.5 - 1
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 78903 None 0 Rat Binding pIC50 = 6.5 6.5 - 1
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 117338 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 117338 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 75319 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 75319 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 148028 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Cellular in Vitro Assay: On the 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 148028 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Cellular in Vitro Assay: On the 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 101563 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 101563 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 131425 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 131425 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 167691 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 167691 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 53197 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 53197 None 0 Rat Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 163404 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 150717 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Cellular In Vitro Assay: On the 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 150717 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Cellular In Vitro Assay: On the 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 3976 None 29 Pig Binding pIC50 = 8.5 8.5 - 9
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 3976 None 29 Pig Binding pIC50 = 8.5 8.5 - 9
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 3976 None 29 Pig Binding pIC50 = 8.5 8.5 - 9
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
644077.0 3976 None 29 Pig Binding pIC50 = 8.5 8.5 - 9
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 3976 None 29 Pig Binding pIC50 = 8.5 8.5 - 9
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 3976 None 29 Pig Binding pIC50 = 8.5 8.5 - 9
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 120067 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 120067 None 0 Human Binding pIC50 = 8.5 8.5 - 0
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 109253 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 109253 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 60451 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 60451 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 60581 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 60581 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 60581 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 60581 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 130756 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 130756 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 131417 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 131417 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 144626 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Cellular in Vitro Assay: On the 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 144626 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Cellular in Vitro Assay: On the 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 114447 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-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 114447 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]-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 165845 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 165845 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 2606 None 50 Rat Binding pIC50 = 6.5 6.5 -1 8
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 2606 None 50 Rat Binding pIC50 = 6.5 6.5 -1 8
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 2606 None 50 Rat Binding pIC50 = 6.5 6.5 -1 8
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 2606 None 50 Rat Binding pIC50 = 6.5 6.5 -1 8
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 60491 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 60491 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 77135 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
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 77135 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
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 18959 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 18959 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 20649 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 20649 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 22127 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 22127 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 78810 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 78810 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 116877 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 116877 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 168553 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 168553 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 73545 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
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 73545 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
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 28396 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 28396 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 78901 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 78901 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 60554 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 60554 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 211365 None 0 Rat Binding pIC50 = 5.5 5.5 - 2
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 154361 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Cellular In Vitro Assay: On the 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 154361 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Cellular In Vitro Assay: On the 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 164133 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 164133 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]-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 118947 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 118947 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 18901 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 18901 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 189930 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 189930 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 102311 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 102311 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 2956 None 18 Human Binding pIC50 = 6.5 6.5 8 2
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 2956 None 18 Human Binding pIC50 = 6.5 6.5 8 2
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 2956 None 18 Human Binding pIC50 = 6.5 6.5 8 2
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 2956 None 18 Human Binding pIC50 = 6.5 6.5 8 2
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 211127 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 117338 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 117338 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 89881 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 89881 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 94248 None 8 Human Binding pIC50 = 7.5 7.5 - 0
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 94248 None 8 Human Binding pIC50 = 7.5 7.5 - 0
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 24870 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 24870 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 56163 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 56163 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 163558 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 163558 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Inhibition of radioligand [3H]-AVP binding 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 63058 None 1 Human Binding pIC50 = 6.5 6.5 - 0
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 63058 None 1 Human Binding pIC50 = 6.5 6.5 - 0
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 169553 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 169553 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 116738 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 116738 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 78905 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 78905 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 90714 None 1 Rat Binding pIC50 = 6.5 6.5 - 4
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 90714 None 1 Rat Binding pIC50 = 6.5 6.5 - 4
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 150569 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Cellular in Vitro Assay: On the 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 150569 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Cellular in Vitro Assay: On the 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 120270 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 120270 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 20697 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 20697 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 188382 None 69 Human Binding pIC50 = 4.4 4.4 -147 32
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 188382 None 69 Human Binding pIC50 = 4.4 4.4 -147 32
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 188382 None 69 Human Binding pIC50 = 4.4 4.4 -147 32
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 119995 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 119995 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 168496 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 168496 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 107295 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 107295 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 61027 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
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 61027 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
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 214076 None 0 Rat Binding pIC50 = 5.4 5.4 -19 2
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 19568 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 19568 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 4969 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 4969 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 5369 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 5369 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 17794 None 2 Rat Binding pIC50 = 6.4 6.4 - 0
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 17794 None 2 Rat Binding pIC50 = 6.4 6.4 - 0
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 140807 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 140807 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 4487 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 4487 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 140660 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 140660 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 98925 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
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 98925 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
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 87041 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 87041 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 188382 None 69 Human Binding pIC50 = 4.4 4.4 -147 32
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 188382 None 69 Human Binding pIC50 = 4.4 4.4 -147 32
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 188382 None 69 Human Binding pIC50 = 4.4 4.4 -147 32
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 188215 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 188215 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 103079 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 103079 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 208090 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 208090 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 119963 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 119963 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 206692 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 206692 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 101967 None 4 Rat Binding pIC50 = 8.4 8.4 - 0
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 101967 None 4 Rat Binding pIC50 = 8.4 8.4 - 0
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 103079 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 103079 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 206692 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 206692 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 206837 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 206837 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 4956 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 4956 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 169626 None 0 Human Binding pIC50 = 8.4 8.4 14 2
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 169626 None 0 Human Binding pIC50 = 8.4 8.4 14 2
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 62326 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 62326 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 206837 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 206837 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 115191 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 115191 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 163599 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 163599 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 101675 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 101675 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 145117 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Cellular In Vitro Assay: On the 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 145117 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Cellular In Vitro Assay: On the 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 104542 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 104542 None 0 Rat Binding pIC50 = 8.4 8.4 - 0
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 142458 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Cellular In Vitro Assay: On the 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 142458 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Cellular In Vitro Assay: On the 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 102228 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 102228 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 151909 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Cellular In Vitro Assay: On the 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 151909 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Cellular In Vitro Assay: On the 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 148005 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Cellular In Vitro Assay: On the 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 148005 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Cellular In Vitro Assay: On the 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 12388 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-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 12388 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-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 12820 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-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 12820 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-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 87041 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 87041 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 12439 None 8 Rat Binding pIC50 = 4.4 4.4 - 0
Displacement of [3H]-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 12439 None 8 Rat Binding pIC50 = 4.4 4.4 - 0
Displacement of [3H]-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 215701 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
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 10519 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]-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 10519 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Displacement of [3H]-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 73290 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
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 73290 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
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 117004 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 117004 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 140433 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 140433 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 206686 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 206686 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
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 12527 None 4 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-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 12527 None 4 Rat Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]-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 18923 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 18923 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 18965 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 18965 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 211366 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
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 10163 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]-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 10163 None 0 Rat Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]-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 120216 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 120216 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 154894 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 154894 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 172733 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 172733 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 204588 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
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 204588 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
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 63058 None 1 Rat Binding pIC50 = 6.4 6.4 - 0
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 63058 None 1 Rat Binding pIC50 = 6.4 6.4 - 0
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 149215 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Cellular In Vitro Assay: On the 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 149215 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Cellular In Vitro Assay: On the 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 117344 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 117344 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 21471 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 21471 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of radioligand [3H]-AVP binding 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 87041 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 87041 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 181039 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 181039 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 168682 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 168682 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 18912 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 18912 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 75945 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 75945 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 148500 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Cellular in Vitro Assay: On the 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 148500 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Cellular in Vitro Assay: On the 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 101370 None 1 Rat Binding pIC50 = 6.3 6.3 - 0
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 101370 None 1 Rat Binding pIC50 = 6.3 6.3 - 0
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 116870 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 116870 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 117039 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 117039 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 18534 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 18534 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 73886 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 73886 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 149643 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Cellular in Vitro Assay: On the 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 149643 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Cellular in Vitro Assay: On the 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 151934 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Cellular in Vitro Assay: On the 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 151934 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Cellular in Vitro Assay: On the 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 102791 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 102791 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 63057 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 63057 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 102228 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 102228 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
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 119364 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 119364 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 2332 None 49 Human Binding pIC50 = 8.3 8.3 64 2
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 167941 None 0 Human Binding pIC50 = 8.3 8.3 1 2
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 167941 None 0 Human Binding pIC50 = 8.3 8.3 1 2
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 60554 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 60554 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 120287 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 120287 None 0 Human Binding pIC50 = 8.3 8.3 - 0
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 152218 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Cellular In Vitro Assay: On the 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 152218 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Cellular In Vitro Assay: On the 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 27217 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 27217 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 12457 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]-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 12457 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]-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 57550 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 57550 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 62126 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 62126 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 61799 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 61799 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 62126 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 62126 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 2606 None 50 Human Binding pIC50 = 6.3 6.3 1 8
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 2606 None 50 Human Binding pIC50 = 6.3 6.3 1 8
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 2606 None 50 Human Binding pIC50 = 6.3 6.3 1 8
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 2606 None 50 Human Binding pIC50 = 6.3 6.3 1 8
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 206807 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
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 206807 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
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 87041 None 0 Human Binding pIC50 = 4.3 4.3 - 0
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 87041 None 0 Human Binding pIC50 = 4.3 4.3 - 0
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 27391 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 27391 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 72064 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 72064 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 78906 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 78906 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 20514 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 20514 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 115285 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 115285 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 115563 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 115563 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 122679 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 122679 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 211365 None 0 Rat Binding pIC50 = 5.3 5.3 - 2
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 117122 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 117122 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 94190 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 94190 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 114326 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-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 114326 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]-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 206925 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 206925 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 116878 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 116878 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 118163 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 118163 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 168064 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
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 168064 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
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 167600 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 167600 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
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 120143 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 120143 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 4367 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 4367 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 116406 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 116406 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 116589 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 116589 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 118016 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 118016 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 118535 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 118535 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of radioligand [3H]-AVP binding 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 78911 None 1 Rat Binding pIC50 = 6.2 6.2 - 2
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 78911 None 1 Rat Binding pIC50 = 6.2 6.2 - 2
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 168343 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 168343 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 2227 None 17 Rat Binding pIC50 = 6.2 6.2 -54 7
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 2227 None 17 Rat Binding pIC50 = 6.2 6.2 -54 7
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 2227 None 17 Rat Binding pIC50 = 6.2 6.2 -54 7
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 11820 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 11820 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 71806 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 71806 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 56273 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 56273 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 107411 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 107411 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 129718 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 129718 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 161832 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 161832 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 186829 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 186829 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 60451 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 60451 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 61027 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 61027 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 118341 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 118341 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 205667 None 50 Human Binding pIC50 = 5.2 5.2 - 1
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 205667 None 50 Human Binding pIC50 = 5.2 5.2 - 1
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 205667 None 50 Human Binding pIC50 = 5.2 5.2 - 1
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 114170 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 114170 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 116920 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 116920 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 99524 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
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 99524 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
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 117078 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 117078 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 22071 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 22071 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 22330 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 22330 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 188382 None 69 Human Binding pIC50 = 5.2 5.2 -147 32
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 188382 None 69 Human Binding pIC50 = 5.2 5.2 -147 32
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 188382 None 69 Human Binding pIC50 = 5.2 5.2 -147 32
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 205667 None 50 Human Binding pIC50 = 5.2 5.2 - 1
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 205667 None 50 Human Binding pIC50 = 5.2 5.2 - 1
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 205667 None 50 Human Binding pIC50 = 5.2 5.2 - 1
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 110710 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]-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 110710 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]-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 12896 None 4 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 12896 None 4 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 117428 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 117428 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 113396 None 4 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 113396 None 4 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 116129 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 116129 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 117116 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 117116 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 206227 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 206227 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 20704 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 20704 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 116993 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 116993 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 149803 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Cellular In Vitro Assay: On the 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 149803 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Cellular In Vitro Assay: On the 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 4693 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 4693 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 22063 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 22063 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 118155 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 118155 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 103110 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 103110 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 11849 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]-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 11849 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [3H]-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 18974 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 18974 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of radioligand [3H]-AVP binding 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 120068 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 120068 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 216122 None 2 Rat Binding pIC50 = 6.2 6.2 - 2
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 117075 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 117075 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 118518 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 118518 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 120171 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 120171 None 0 Human Binding pIC50 = 8.2 8.2 - 0
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 206752 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 206752 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 108648 None 0 Human Binding pIC50 = 8.2 8.2 4 2
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 108648 None 0 Human Binding pIC50 = 8.2 8.2 4 2
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 130757 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 130757 None 0 Rat Binding pIC50 = 8.2 8.2 - 0
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 101894 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 101894 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 165641 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 165641 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 118946 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 118946 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 146986 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 146986 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 152508 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Cellular in Vitro Assay: On the 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 152508 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Cellular in Vitro Assay: On the 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 114489 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-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 114489 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-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 169220 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 169220 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 128716 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 128716 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 188382 None 69 Human Binding pIC50 = 5.2 5.2 -147 32
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 188382 None 69 Human Binding pIC50 = 5.2 5.2 -147 32
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 188382 None 69 Human Binding pIC50 = 5.2 5.2 -147 32
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 118541 None 4 Rat Binding pIC50 = 4.2 4.2 -77 6
Inhibition of radioligand [3H]-AVP binding 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 118541 None 4 Rat Binding pIC50 = 4.2 4.2 -77 6
Inhibition of radioligand [3H]-AVP binding 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 114596 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-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 114596 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]-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 169011 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 169011 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 120068 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 120068 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 10091 None 7 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 10091 None 7 Rat Binding pIC50 = 5.2 5.2 - 0
Displacement of [3H]-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 99079 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
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 99079 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
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 168101 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 168101 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 211696 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 99102 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
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 99102 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
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 167987 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 167987 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 117434 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 117434 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 211703 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
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 117281 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 117281 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 118293 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 118293 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 211701 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 118540 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 118540 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 154709 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 154709 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 113196 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-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 113196 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Displacement of [3H]-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 12960 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]-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 12960 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]-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 114876 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-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 114876 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-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 103865 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 103865 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 205770 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 205770 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 12712 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 12712 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 21548 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 21548 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 205667 None 50 Human Binding pIC50 = 6.1 6.1 - 1
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 205667 None 50 Human Binding pIC50 = 6.1 6.1 - 1
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 205667 None 50 Human Binding pIC50 = 6.1 6.1 - 1
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 116685 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 116685 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 116845 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 116845 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 4969 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 4969 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 63057 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 63057 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 151838 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular in Vitro Assay: On the 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 151838 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular in Vitro Assay: On the 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 120122 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 120122 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 208160 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 208160 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 154819 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 154819 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 61794 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 61794 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 62326 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 62326 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 150499 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 150499 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 101517 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 101517 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 106740 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 106740 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 104952 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 104952 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 149117 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 149117 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 146223 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 146223 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular In Vitro Assay: On the 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 168741 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 168741 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 30986 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 30986 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 4004 None 22 Human Binding pIC50 = 7.1 7.1 3 3
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 4004 None 22 Human Binding pIC50 = 7.1 7.1 3 3
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 4004 None 22 Human Binding pIC50 = 7.1 7.1 3 3
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 61794 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 61794 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 128716 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 128716 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 168605 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 168605 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 4004 None 22 Human Binding pIC50 = 7.1 7.1 3 3
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 4004 None 22 Human Binding pIC50 = 7.1 7.1 3 3
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 4004 None 22 Human Binding pIC50 = 7.1 7.1 3 3
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 205667 None 50 Human Binding pIC50 = 6.1 6.1 - 1
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 205667 None 50 Human Binding pIC50 = 6.1 6.1 - 1
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 205667 None 50 Human Binding pIC50 = 6.1 6.1 - 1
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 100862 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 100862 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 211695 None 2 Rat Binding pIC50 = 6.1 6.1 - 2
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 116503 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 116503 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 110569 None 6 Rat Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]-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 110569 None 6 Rat Binding pIC50 = 5.1 5.1 - 0
Displacement of [3H]-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 218195 None 0 Rat Binding pIC50 = 4.1 4.1 -23 2
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 13941 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-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 13941 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]-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 203008 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 203008 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
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 99561 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
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 99561 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
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 18878 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 18878 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 21483 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 21483 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 102346 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 102346 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 206820 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 206820 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 168624 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 168624 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 73953 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
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 73953 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
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 22126 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 22126 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of radioligand [3H]-AVP binding 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 74973 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 74973 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
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 118245 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 118245 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 144970 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular in Vitro Assay: On the 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 144970 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Cellular in Vitro Assay: On the 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 101151 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 101151 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 118245 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 118245 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 129718 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 129718 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 97147 None 0 Pig Binding pIC50 = 8.0 8.0 - 0
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 97147 None 0 Pig Binding pIC50 = 8.0 8.0 - 0
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 74380 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 74380 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 211695 None 2 Rat Binding pIC50 = 6.0 6.0 - 2
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 154710 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 154710 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 21332 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 21332 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 117021 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 117021 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 73968 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 73968 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 118451 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 118451 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 22455 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 22455 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 14576 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-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 14576 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]-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 140363 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 140363 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 18895 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 18895 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Inhibition of radioligand [3H]-AVP binding 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 17794 None 2 Human Binding pIC50 = 6.0 6.0 - 0
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 17794 None 2 Human Binding pIC50 = 6.0 6.0 - 0
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 114456 None 7 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]-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 114456 None 7 Rat Binding pIC50 = 6.0 6.0 - 0
Displacement of [3H]-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 82407 None 0 Human Binding pKd = 8.9 8.9 64 3
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 82407 None 0 Human Binding pKd = 8.9 8.9 64 3
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 82407 None 0 Human Binding pKd = 8.9 8.9 64 3
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 156185 None 0 Bovine Binding pKd = 8.9 8.9 - 1
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 156185 None 0 Bovine Binding pKd = 8.9 8.9 - 1
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 3976 None 29 Rat Binding pKd = 8.8 8.8 -4 9
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 3976 None 29 Rat Binding pKd = 8.8 8.8 -4 9
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 3976 None 29 Rat Binding pKd = 8.8 8.8 -4 9
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
644077.0 3976 None 29 Rat Binding pKd = 8.8 8.8 -4 9
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 3976 None 29 Rat Binding pKd = 8.8 8.8 -4 9
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 3976 None 29 Rat Binding pKd = 8.8 8.8 -4 9
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 3976 None 29 Bovine Binding pKd = 8.8 8.8 -7 9
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 3976 None 29 Bovine Binding pKd = 8.8 8.8 -7 9
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 3976 None 29 Bovine Binding pKd = 8.8 8.8 -7 9
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
644077.0 3976 None 29 Bovine Binding pKd = 8.8 8.8 -7 9
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 3976 None 29 Bovine Binding pKd = 8.8 8.8 -7 9
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 3976 None 29 Bovine Binding pKd = 8.8 8.8 -7 9
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 213095 None 0 Bovine Binding pKd = 8 8.0 - 1
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 79723 None 0 Pig Binding pKd = 7 7.0 -257 2
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 79723 None 0 Pig Binding pKd = 7 7.0 -257 2
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 115455 None 0 Rat Binding pKd = 6 6.0 -26 3
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 115455 None 0 Rat Binding pKd = 6 6.0 -26 3
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 82406 None 0 Human Binding pKd = 8.0 8.0 38 2
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 82406 None 0 Human Binding pKd = 8.0 8.0 38 2
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 215542 None 0 Bovine Binding pKd = 7.0 7.0 - 1
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 115457 None 0 Rat Binding pKd = 5.9 5.9 -43 3
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 115457 None 0 Rat Binding pKd = 5.9 5.9 -43 3
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 160869 None 0 Bovine Binding pKd = 6.9 6.9 -8 2
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 160869 None 0 Bovine Binding pKd = 6.9 6.9 -8 2
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 118656 None 0 Human Binding pKd = 6.9 6.9 -77 3
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 118656 None 0 Human Binding pKd = 6.9 6.9 -77 3
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 212346 None 0 Rat Binding pKd = 7.8 7.8 -3 3
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 63350 None 0 Bovine Binding pKd = 6.7 6.7 1 2
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 63350 None 0 Bovine Binding pKd = 6.7 6.7 1 2
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 82408 None 0 Human Binding pKd = 8.6 8.6 234 3
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 82408 None 0 Human Binding pKd = 8.6 8.6 234 3
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 82408 None 0 Human Binding pKd = 8.6 8.6 234 3
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 82409 None 0 Human Binding pKd = 8.6 8.6 - 1
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 82409 None 0 Human Binding pKd = 8.6 8.6 - 1
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 82409 None 0 Human Binding pKd = 8.6 8.6 - 1
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 213261 None 0 Bovine Binding pKd = 7.7 7.7 - 1
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 78387 None 0 Rat Binding pKd = 5.6 5.6 -6 2
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 78387 None 0 Rat Binding pKd = 5.6 5.6 -6 2
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 141554 None 0 Bovine Binding pKd = 6.6 6.6 -1 2
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 141554 None 0 Bovine Binding pKd = 6.6 6.6 -1 2
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 96897 None 0 Bovine Binding pKd = 6.6 6.6 - 1
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 96897 None 0 Bovine Binding pKd = 6.6 6.6 - 1
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 212431 None 10 Rat Binding pKd = 7.6 7.6 -3 3
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 115454 None 0 Rat Binding pKd = 5.5 5.5 -213 3
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 115454 None 0 Rat Binding pKd = 5.5 5.5 -213 3
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 168997 None 0 Bovine Binding pKd = 7.5 7.5 -1 2
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 168997 None 0 Bovine Binding pKd = 7.5 7.5 -1 2
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 96771 None 0 Rat Binding pKd = 8.5 8.5 1 2
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 96771 None 0 Rat Binding pKd = 8.5 8.5 1 2
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 118657 None 0 Human Binding pKd = 7.5 7.5 -21 3
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 118657 None 0 Human Binding pKd = 7.5 7.5 -21 3
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 161929 None 0 Bovine Binding pKd = 6.5 6.5 -38 2
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 161929 None 0 Bovine Binding pKd = 6.5 6.5 -38 2
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 115409 None 0 Rat Binding pKd = 5.5 5.5 -173 3
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 115409 None 0 Rat Binding pKd = 5.5 5.5 -173 3
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 115410 None 0 Rat Binding pKd = 5.5 5.5 -154 3
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 115410 None 0 Rat Binding pKd = 5.5 5.5 -154 3
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 115413 None 1 Rat Binding pKd = 5.5 5.5 -363 3
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 115413 None 1 Rat Binding pKd = 5.5 5.5 -363 3
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 168908 None 0 Bovine Binding pKd = 7.5 7.5 - 1
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 168908 None 0 Bovine Binding pKd = 7.5 7.5 - 1
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 162000 None 0 Bovine Binding pKd = 7.5 7.5 -1 2
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 162000 None 0 Bovine Binding pKd = 7.5 7.5 -1 2
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 167815 None 0 Human Binding pKd = 6.5 6.5 -190 2
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 167815 None 0 Human Binding pKd = 6.5 6.5 -190 2
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 167815 None 0 Human Binding pKd = 6.5 6.5 -190 2
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 115412 None 0 Rat Binding pKd = 5.4 5.4 -186 3
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 115412 None 0 Rat Binding pKd = 5.4 5.4 -186 3
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 51188 None 0 Rat Binding pKd = 6.4 6.4 -52 2
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 51188 None 0 Rat Binding pKd = 6.4 6.4 -52 2
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 208843 None 0 Bovine Binding pKd = 6.4 6.4 -52 2
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 208843 None 0 Bovine Binding pKd = 6.4 6.4 -52 2
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 215256 None 0 Bovine Binding pKd = 7.4 7.4 - 1
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 115452 None 0 Rat Binding pKd = 7.3 7.3 -5 3
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 115452 None 0 Rat Binding pKd = 7.3 7.3 -5 3
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 155791 None 0 Rat Binding pKd = 5.3 5.3 -131 2
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 155791 None 0 Rat Binding pKd = 5.3 5.3 -131 2
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 167757 None 0 Human Binding pKd = 6.3 6.3 -323 2
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 167757 None 0 Human Binding pKd = 6.3 6.3 -323 2
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 167757 None 0 Human Binding pKd = 6.3 6.3 -323 2
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 160792 None 0 Bovine Binding pKd = 7.3 7.3 - 1
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 160792 None 0 Bovine Binding pKd = 7.3 7.3 - 1
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 78401 None 0 Rat Binding pKd = 5.3 5.3 -2 2
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 78401 None 0 Rat Binding pKd = 5.3 5.3 -2 2
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 115456 None 0 Rat Binding pKd = 7.3 7.3 -2 3
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 115456 None 0 Rat Binding pKd = 7.3 7.3 -2 3
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 97065 None 0 Rat Binding pKd = 8.1 8.1 1 3
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 97065 None 0 Rat Binding pKd = 8.1 8.1 1 3
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 161778 None 0 Bovine Binding pKd = 8.1 8.1 - 1
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 161778 None 0 Bovine Binding pKd = 8.1 8.1 - 1
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 112625 None 0 Bovine Binding pKd = 6.1 6.1 -45 2
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 112625 None 0 Bovine Binding pKd = 6.1 6.1 -45 2
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 211835 None 0 Bovine Binding pKd = 8.0 8.0 - 1
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 212566 None 0 Bovine Binding pKd = 8.0 8.0 - 1
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 96856 None 0 Bovine Binding pKd = 7.0 7.0 -13 2
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 96856 None 0 Bovine Binding pKd = 7.0 7.0 -13 2
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 137483 None 0 Rat Binding pKi = 9.7 9.7 -1 8
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 137483 None 0 Rat Binding pKi = 9.7 9.7 -1 8
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 168602 None 15 Rat Binding pKi = 9.6 9.6 1230 2
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 168602 None 15 Rat Binding pKi = 9.6 9.6 1230 2
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 1331 None 29 Rat Binding pKi = 9.5 9.5 1 8
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 1331 None 29 Rat Binding pKi = 9.5 9.5 1 8
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 1331 None 29 Rat Binding pKi = 9.5 9.5 1 8
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
27991.0 1331 None 29 Rat Binding pKi = 9.5 9.5 1 8
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 1331 None 29 Rat Binding pKi = 9.5 9.5 1 8
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 1331 None 29 Rat Binding pKi = 9.5 9.5 1 8
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 1331 None 29 Rat Binding pKi = 9.5 9.5 1 8
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 84330 None 0 Rat Binding pKi = 9.5 9.5 -1 8
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 84330 None 0 Rat Binding pKi = 9.5 9.5 -1 8
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 1164 None 41 Human Binding pKi = 9.4 9.4 -1 6
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
151171.0 1164 None 41 Human Binding pKi = 9.4 9.4 -1 6
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 1164 None 41 Human Binding pKi = 9.4 9.4 -1 6
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 1164 None 41 Human Binding pKi = 9.4 9.4 -1 6
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 1164 None 41 Human Binding pKi = 9.4 9.4 -1 6
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 1164 None 41 Human Binding pKi = 9.4 9.4 -1 6
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 1164 None 41 Human Binding pKi = 9.4 9.4 -1 6
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 188927 None 0 Rat Binding pKi = 9.4 9.4 - 1
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 188927 None 0 Rat Binding pKi = 9.4 9.4 - 1
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 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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
216237.0 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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
443894.0 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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 3843 None 51 Human Binding pKi = 9.4 9.4 2 8
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 3976 None 29 Rat Binding pKi = 9.4 9.4 -4 9
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 3976 None 29 Rat Binding pKi = 9.4 9.4 -4 9
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 3976 None 29 Rat Binding pKi = 9.4 9.4 -4 9
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
644077.0 3976 None 29 Rat Binding pKi = 9.4 9.4 -4 9
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 3976 None 29 Rat Binding pKi = 9.4 9.4 -4 9
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 3976 None 29 Rat Binding pKi = 9.4 9.4 -4 9
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 212564 None 0 Human Binding pKi = 9.3 9.3 - 1
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 203691 None 0 Human Binding pKi = 9.2 9.2 2 3
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 203691 None 0 Human Binding pKi = 9.2 9.2 2 3
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 203691 None 0 Human Binding pKi = 9.2 9.2 2 3
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 203691 None 0 Human Binding pKi = 9.2 9.2 2 3
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 203691 None 0 Human Binding pKi = 9.2 9.2 2 3
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 203691 None 0 Human Binding pKi = 9.2 9.2 2 3
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
121301508 176323 None 5 Human Binding pKi = 9.2 9.2 1 3
Radiometric AVPR2 binding assay (Eurofins #287610)Radiometric AVPR2 binding assay (Eurofins #287610)
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
CHEMBL4594444 176323 None 5 Human Binding pKi = 9.2 9.2 1 3
Radiometric AVPR2 binding assay (Eurofins #287610)Radiometric AVPR2 binding assay (Eurofins #287610)
ChEMBL 542 7 2 9 3.6 C[C@H](O)c1nc(Cn2nc(-c3ccc(Cl)cc3)n(C[C@H](O)C(F)(F)F)c2=O)nn1-c1cccc(Cl)c1 10.6019/CHEMBL5463729
135413562 2205 None 13 Human Binding pKi = 9.2 9.2 -1 5
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 2205 None 13 Human Binding pKi = 9.2 9.2 -1 5
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 2205 None 13 Human Binding pKi = 9.2 9.2 -1 5
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 212563 None 0 Human Binding pKi = 9.2 9.2 - 1
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 4123 None 6 Rat Binding pKi = 9.1 9.1 -3 5
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 4123 None 6 Rat Binding pKi = 9.1 9.1 -3 5
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 4123 None 6 Rat Binding pKi = 9.1 9.1 -3 5
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
2181 1331 None 29 Rat Binding pKi = 9.1 9.1 1 8
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 1331 None 29 Rat Binding pKi = 9.1 9.1 1 8
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 1331 None 29 Rat Binding pKi = 9.1 9.1 1 8
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
27991.0 1331 None 29 Rat Binding pKi = 9.1 9.1 1 8
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 1331 None 29 Rat Binding pKi = 9.1 9.1 1 8
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 1331 None 29 Rat Binding pKi = 9.1 9.1 1 8
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 1331 None 29 Rat Binding pKi = 9.1 9.1 1 8
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
71462477 82409 None 0 Human Binding pKi = 9.1 9.1 - 1
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 82409 None 0 Human Binding pKi = 9.1 9.1 - 1
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 82409 None 0 Human Binding pKi = 9.1 9.1 - 1
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 3420 None 2 Human Binding pKi = 9.1 9.1 46 2
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 3420 None 2 Human Binding pKi = 9.1 9.1 46 2
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 3420 None 2 Human Binding pKi = 9.1 9.1 46 2
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 96546 None 0 Human Binding pKi = 9 9.0 - 1
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 96546 None 0 Human Binding pKi = 9 9.0 - 1
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 168951 None 0 Human Binding pKi = 9 9.0 6 2
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 168951 None 0 Human Binding pKi = 9 9.0 6 2
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 213445 None 0 Human Binding pKi = 9 9.0 - 1
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 3843 None 51 Human Binding pKi = 9 9.0 2 8
Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assayDisplacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
ChEMBL 448 3 2 3 5.7 Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C 10.1021/acs.jmedchem.1c00863
216237.0 3843 None 51 Human Binding pKi = 9 9.0 2 8
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 3843 None 51 Human Binding pKi = 9 9.0 2 8
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 3843 None 51 Human Binding pKi = 9 9.0 2 8
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 3843 None 51 Human Binding pKi = 9 9.0 2 8
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
443894.0 3843 None 51 Human Binding pKi = 9 9.0 2 8
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 3843 None 51 Human Binding pKi = 9 9.0 2 8
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 3843 None 51 Human Binding pKi = 9 9.0 2 8
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 141637 None 0 Human Binding pKi = 9.0 9.0 3 2
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 141637 None 0 Human Binding pKi = 9.0 9.0 3 2
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 4123 None 6 Human Binding pKi = 8.9 8.9 -3 5
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 4123 None 6 Human Binding pKi = 8.9 8.9 -3 5
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 4123 None 6 Human Binding pKi = 8.9 8.9 -3 5
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 4123 None 6 Rat Binding pKi = 8.9 8.9 -3 5
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 4123 None 6 Rat Binding pKi = 8.9 8.9 -3 5
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 4123 None 6 Rat Binding pKi = 8.9 8.9 -3 5
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 84330 None 0 Human Binding pKi = 8.9 8.9 -4 8
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 84330 None 0 Human Binding pKi = 8.9 8.9 -4 8
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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
644077.0 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 215175 None 0 Pig Binding pKi = 8.9 8.9 - 1
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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
644077.0 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 3976 None 29 Human Binding pKi = 8.9 8.9 -15 9
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 111466 None 0 Human Binding pKi = 8.9 8.9 75 2
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 111466 None 0 Human Binding pKi = 8.9 8.9 75 2
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 3976 None 29 Human Binding pKi = 8.8 8.8 -15 9
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 3976 None 29 Human Binding pKi = 8.8 8.8 -15 9
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 3976 None 29 Human Binding pKi = 8.8 8.8 -15 9
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
644077.0 3976 None 29 Human Binding pKi = 8.8 8.8 -15 9
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 3976 None 29 Human Binding pKi = 8.8 8.8 -15 9
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 3976 None 29 Human Binding pKi = 8.8 8.8 -15 9
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 212157 None 1 Human Binding pKi = 8.8 8.8 -1 4
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 117541 None 0 Human Binding pKi = 8.8 8.8 1 2
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 117541 None 0 Human Binding pKi = 8.8 8.8 1 2
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 165952 None 0 Rat Binding pKi = 8.8 8.8 -7 3
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 165952 None 0 Rat Binding pKi = 8.8 8.8 -7 3
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 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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
216237.0 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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
443894.0 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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 3843 None 51 Human Binding pKi = 8.8 8.8 2 8
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 141806 None 0 Rat Binding pKi = 8.7 8.7 -9 4
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 141806 None 0 Rat Binding pKi = 8.7 8.7 -9 4
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 209803 None 0 Human Binding pKi = 8.7 8.7 354 2
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 209803 None 0 Human Binding pKi = 8.7 8.7 354 2
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 82408 None 0 Human Binding pKi = 8.7 8.7 234 3
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 82408 None 0 Human Binding pKi = 8.7 8.7 234 3
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 82408 None 0 Human Binding pKi = 8.7 8.7 234 3
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 179568 None 0 Human Binding pKi = 8 8.0 3 2
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 179568 None 0 Human Binding pKi = 8 8.0 3 2
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 191290 None 0 Human Binding pKi = 8 8.0 - 1
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 191290 None 0 Human Binding pKi = 8 8.0 - 1
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 192479 None 0 Human Binding pKi = 8 8.0 - 1
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 192479 None 0 Human Binding pKi = 8 8.0 - 1
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 212363 None 0 Pig Binding pKi = 8 8.0 -1 2
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 212505 None 0 Pig Binding pKi = 8 8.0 - 1
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 165521 None 0 Human Binding pKi = 8 8.0 - 1
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 165521 None 0 Human Binding pKi = 8 8.0 - 1
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 209743 None 0 Human Binding pKi = 8 8.0 - 1
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 209743 None 0 Human Binding pKi = 8 8.0 - 1
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 209746 None 0 Human Binding pKi = 8 8.0 - 1
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 209746 None 0 Human Binding pKi = 8 8.0 - 1
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 169363 None 0 Rat Binding pKi = 8 8.0 -22 3
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 169363 None 0 Rat Binding pKi = 8 8.0 -22 3
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 163735 None 0 Human Binding pKi = 7 7.0 7 2
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 163735 None 0 Human Binding pKi = 7 7.0 7 2
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 161708 None 18 Rat Binding pKi = 7 7.0 -630 4
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 161708 None 18 Rat Binding pKi = 7 7.0 -630 4
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 208734 None 0 Rat Binding pKi = 6 6.0 -954 4
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 208734 None 0 Rat Binding pKi = 6 6.0 -954 4
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 107094 None 0 Human Binding pKi = 5.0 5.0 -354 2
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 107094 None 0 Human Binding pKi = 5.0 5.0 -354 2
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 112378 None 0 Human Binding pKi = 5.0 5.0 -269 2
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 112378 None 0 Human Binding pKi = 5.0 5.0 -269 2
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 7031 None 0 Human Binding pKi = 6.0 6.0 -93 2
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 7031 None 0 Human Binding pKi = 6.0 6.0 -93 2
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 137329 None 0 Rat Binding pKi = 6.0 6.0 -104 5
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 137329 None 0 Rat Binding pKi = 6.0 6.0 -104 5
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 7033 None 0 Human Binding pKi = 6.0 6.0 -28 2
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 7033 None 0 Human Binding pKi = 6.0 6.0 -28 2
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 212168 None 0 Human Binding pKi = 6.0 6.0 -112 4
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 7034 None 0 Human Binding pKi = 7.0 7.0 -199 2
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 7034 None 0 Human Binding pKi = 7.0 7.0 -199 2
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 192496 None 0 Human Binding pKi = 7.0 7.0 - 1
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 192496 None 0 Human Binding pKi = 7.0 7.0 - 1
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 217231 None 0 Human Binding pKi = 6.0 6.0 -2691 2
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 212159 None 0 Human Binding pKi = 6.0 6.0 -7 4
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 172740 None 0 Human Binding pKi = 8.0 8.0 5 2
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 172740 None 0 Human Binding pKi = 8.0 8.0 5 2
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 174522 None 0 Human Binding pKi = 8.0 8.0 4 2
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 174522 None 0 Human Binding pKi = 8.0 8.0 4 2
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 181962 None 0 Human Binding pKi = 8.0 8.0 3 2
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 181962 None 0 Human Binding pKi = 8.0 8.0 3 2
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 189715 None 0 Human Binding pKi = 8.0 8.0 3 2
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 189715 None 0 Human Binding pKi = 8.0 8.0 3 2
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 192722 None 0 Human Binding pKi = 8.0 8.0 3 2
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 192722 None 0 Human Binding pKi = 8.0 8.0 3 2
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 12478 None 0 Human Binding pKi = 8.0 8.0 - 1
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 12478 None 0 Human Binding pKi = 8.0 8.0 - 1
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 12478 None 0 Human Binding pKi = 8.0 8.0 - 1
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 12699 None 0 Human Binding pKi = 8.0 8.0 - 1
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 12699 None 0 Human Binding pKi = 8.0 8.0 - 1
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 12699 None 0 Human Binding pKi = 8.0 8.0 - 1
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 190235 None 1 Human Binding pKi = 8.0 8.0 - 1
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 190235 None 1 Human Binding pKi = 8.0 8.0 - 1
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 117061 None 0 Pig Binding pKi = 8.0 8.0 - 1
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 117061 None 0 Pig Binding pKi = 8.0 8.0 - 1
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 161537 None 0 Pig Binding pKi = 8.0 8.0 - 1
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 161537 None 0 Pig Binding pKi = 8.0 8.0 - 1
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 209318 None 0 Human Binding pKi = 8.0 8.0 44 2
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 209318 None 0 Human Binding pKi = 8.0 8.0 44 2
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 209902 None 0 Human Binding pKi = 8.0 8.0 562 2
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 209902 None 0 Human Binding pKi = 8.0 8.0 562 2
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 211359 None 0 Rat Binding pKi = 6.0 6.0 -229 2
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 33853 None 1 Rat Binding pKi = 5.0 5.0 -457 5
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 33853 None 1 Rat Binding pKi = 5.0 5.0 -457 5
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 119478 None 0 Rat Binding pKi = 5.0 5.0 -724 5
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 119478 None 0 Rat Binding pKi = 5.0 5.0 -724 5
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 209088 None 0 Human Binding pKi = 5.0 5.0 -1202 2
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 209088 None 0 Human Binding pKi = 5.0 5.0 -1202 2
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 212161 None 0 Human Binding pKi = 5.0 5.0 -6165 4
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 137309 None 0 Human Binding pKi = 6.0 6.0 -2511 8
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 137309 None 0 Human Binding pKi = 6.0 6.0 -2511 8
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 164689 None 0 Human Binding pKi = 5.9 5.9 -7 3
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 164689 None 0 Human Binding pKi = 5.9 5.9 -7 3
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 212156 None 0 Human Binding pKi = 6.9 6.9 -275 4
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 7360 None 0 Human Binding pKi = 5.9 5.9 -1148 2
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 7360 None 0 Human Binding pKi = 5.9 5.9 -1148 2
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 78662 None 0 Rat Binding pKi = 4.9 4.9 -8128 4
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 78662 None 0 Rat Binding pKi = 4.9 4.9 -8128 4
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 189234 None 0 Human Binding pKi = 7.9 7.9 6 2
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 189234 None 0 Human Binding pKi = 7.9 7.9 6 2
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 190683 None 0 Human Binding pKi = 7.9 7.9 - 1
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 190683 None 0 Human Binding pKi = 7.9 7.9 - 1
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 191544 None 0 Human Binding pKi = 7.9 7.9 - 1
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 191544 None 0 Human Binding pKi = 7.9 7.9 - 1
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 191988 None 0 Human Binding pKi = 7.9 7.9 - 1
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 191988 None 0 Human Binding pKi = 7.9 7.9 - 1
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 82145 None 0 Pig Binding pKi = 7.9 7.9 - 1
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 82145 None 0 Pig Binding pKi = 7.9 7.9 - 1
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 96536 None 0 Pig Binding pKi = 7.9 7.9 - 1
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 96536 None 0 Pig Binding pKi = 7.9 7.9 - 1
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 82419 None 0 Human Binding pKi = 7.9 7.9 - 1
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 82419 None 0 Human Binding pKi = 7.9 7.9 - 1
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 96962 None 16 Rat Binding pKi = 7.9 7.9 -10 8
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 96962 None 16 Rat Binding pKi = 7.9 7.9 -10 8
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 None 35 Human Binding pKi = 5.9 5.9 -1288249 4
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 None 35 Human Binding pKi = 5.9 5.9 -1288249 4
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 None 35 Human Binding pKi = 5.9 5.9 -1288249 4
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 None 35 Human Binding pKi = 5.9 5.9 -1288249 4
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 6737 None 0 Human Binding pKi = 5.9 5.9 -47 2
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 6737 None 0 Human Binding pKi = 5.9 5.9 -47 2
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 163938 None 0 Human Binding pKi = 6.9 6.9 -1 3
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 163938 None 0 Human Binding pKi = 6.9 6.9 -1 3
Displacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assayDisplacement of [3H]-AVP from human V2 receptor expressed in CHO cell membranes by radioligand binding assay
ChEMBL 293 3 0 1 4.6 CCCc1ccc(C(=O)N2CCCCc3ccccc32)cc1 10.1021/acs.jmedchem.8b00697
172441826 195060 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccccc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5395776 195060 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1ccccc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
46890152 6755 None 0 Human Binding pKi = 6.9 6.9 -3 2
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 6755 None 0 Human Binding pKi = 6.9 6.9 -3 2
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 209143 None 0 Rat Binding pKi = 5.9 5.9 -1174 4
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 209143 None 0 Rat Binding pKi = 5.9 5.9 -1174 4
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 118664 None 0 Human Binding pKi = 5.9 5.9 -1 2
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 118664 None 0 Human Binding pKi = 5.9 5.9 -1 2
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 72131 None 0 Human Binding pKi = 5.9 5.9 -316 2
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 72131 None 0 Human Binding pKi = 5.9 5.9 -316 2
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 174933 None 7 Human Binding pKi = 4.9 4.9 -2818 4
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 174933 None 7 Human Binding pKi = 4.9 4.9 -2818 4
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 204170 None 0 Human Binding pKi = 7.9 7.9 -1 2
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 204170 None 0 Human Binding pKi = 7.9 7.9 -1 2
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 191948 None 0 Human Binding pKi = 7.9 7.9 - 1
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 191948 None 0 Human Binding pKi = 7.9 7.9 - 1
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 191597 None 0 Human Binding pKi = 7.9 7.9 - 1
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 191597 None 0 Human Binding pKi = 7.9 7.9 - 1
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 167941 None 0 Human Binding pKi = 7.9 7.9 1 2
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 167941 None 0 Human Binding pKi = 7.9 7.9 1 2
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 112370 None 0 Human Binding pKi = 7.9 7.9 64 2
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 112370 None 0 Human Binding pKi = 7.9 7.9 64 2
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 160522 None 0 Human Binding pKi = 7.9 7.9 -2 4
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 160522 None 0 Human Binding pKi = 7.9 7.9 -2 4
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 93370 None 1 Human Binding pKi = 6.9 6.9 -181 6
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 93370 None 1 Human Binding pKi = 6.9 6.9 -181 6
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 7305 None 0 Human Binding pKi = 6.9 6.9 -181 2
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 7305 None 0 Human Binding pKi = 6.9 6.9 -181 2
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 118667 None 0 Human Binding pKi = 6.9 6.9 -22 2
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 118667 None 0 Human Binding pKi = 6.9 6.9 -22 2
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 19399 None 0 Pig Binding pKi = 6.9 6.9 - 1
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 19399 None 0 Pig Binding pKi = 6.9 6.9 - 1
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 137483 None 0 Human Binding pKi = 6.9 6.9 -1023 8
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 137483 None 0 Human Binding pKi = 6.9 6.9 -1023 8
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 7256 None 0 Human Binding pKi = 6.9 6.9 3 2
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 7256 None 0 Human Binding pKi = 6.9 6.9 3 2
Displacement [3H]Arg human recombinant Vasopressin V2 receptorDisplacement [3H]Arg human recombinant Vasopressin V2 receptor
ChEMBL 451 2 0 1 7.9 CC1(C)C[C@@H]2C[C@@](C)(CN2C(=O)c2cc(Cl)c(-c3cccc4ccccc34)cc2Cl)C1 10.1016/j.bmcl.2010.04.068
172452353 196440 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1cccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5424001 196440 None 0 Human Binding pKi = 6.9 6.9 - 1
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 440 3 0 4 7.1 Cc1cccc(/N=N\c2ccc(C(=O)N3Cc4cccn4Cc4ccccc43)c(Cl)c2)c1 10.1021/acs.jmedchem.2c01625
168272611 190495 None 0 Human Binding pKi = 5.9 5.9 - 1
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 190495 None 0 Human Binding pKi = 5.9 5.9 - 1
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 207425 None 0 Rat Binding pKi = 5.9 5.9 -2 2
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 207425 None 0 Rat Binding pKi = 5.9 5.9 -2 2
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 97340 None 0 Human Binding pKi = 6.9 6.9 -1737 4
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 97340 None 0 Human Binding pKi = 6.9 6.9 -1737 4
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 212160 None 0 Human Binding pKi = 5.9 5.9 -2630 4
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 179726 None 0 Human Binding pKi = 7.9 7.9 4 2
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 179726 None 0 Human Binding pKi = 7.9 7.9 4 2
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 12581 None 0 Human Binding pKi = 7.9 7.9 - 1
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 12581 None 0 Human Binding pKi = 7.9 7.9 - 1
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 12581 None 0 Human Binding pKi = 7.9 7.9 - 1
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 12585 None 0 Human Binding pKi = 7.9 7.9 - 1
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 12585 None 0 Human Binding pKi = 7.9 7.9 - 1
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 12585 None 0 Human Binding pKi = 7.9 7.9 - 1
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 202164 None 0 Human Binding pKi = 7.9 7.9 3 2
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 202164 None 0 Human Binding pKi = 7.9 7.9 3 2
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 202255 None 0 Human Binding pKi = 7.9 7.9 1 2
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 202255 None 0 Human Binding pKi = 7.9 7.9 1 2
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 82412 None 0 Human Binding pKi = 7.9 7.9 - 1
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 82412 None 0 Human Binding pKi = 7.9 7.9 - 1
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 82409 None 0 Human Binding pKi = 7.9 7.9 - 1
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 82409 None 0 Human Binding pKi = 7.9 7.9 - 1
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 82409 None 0 Human Binding pKi = 7.9 7.9 - 1
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 63228 None 0 Rat Binding pKi = 6.9 6.9 -91 2
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 63228 None 0 Rat Binding pKi = 6.9 6.9 -91 2
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 156312 None 0 Human Binding pKi = 6.9 6.9 -50 2
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 156312 None 0 Human Binding pKi = 6.9 6.9 -50 2
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 73675 None 0 Human Binding pKi = 5.9 5.9 -141 3
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 73675 None 0 Human Binding pKi = 5.9 5.9 -141 3
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 107000 None 0 Human Binding pKi = 4.8 4.8 -371 2
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 107000 None 0 Human Binding pKi = 4.8 4.8 -371 2
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 78662 None 0 Human Binding pKi = 4.8 4.8 -10000 4
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 78662 None 0 Human Binding pKi = 4.8 4.8 -10000 4
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 6729 None 0 Human Binding pKi = 7.8 7.8 -19 2
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 6729 None 0 Human Binding pKi = 7.8 7.8 -19 2
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 78378 None 0 Human Binding pKi = 7.8 7.8 58 2
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 78378 None 0 Human Binding pKi = 7.8 7.8 58 2
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 78378 None 0 Human Binding pKi = 7.8 7.8 58 2
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 209747 None 0 Human Binding pKi = 7.8 7.8 - 1
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 209747 None 0 Human Binding pKi = 7.8 7.8 - 1
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 93370 None 1 Rat Binding pKi = 6.8 6.8 -213 6
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 93370 None 1 Rat Binding pKi = 6.8 6.8 -213 6
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 211357 None 0 Rat Binding pKi = 5.8 5.8 -50 2
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 211357 None 0 Rat Binding pKi = 5.8 5.8 -50 2
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 2983 None 40 Human Binding pKi = 5.8 5.8 -831 8
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
2174 2983 None 40 Human Binding pKi = 5.8 5.8 -831 8
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
2176 2983 None 40 Human Binding pKi = 5.8 5.8 -831 8
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
439302 2983 None 40 Human Binding pKi = 5.8 5.8 -831 8
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
439302.0 2983 None 40 Human Binding pKi = 5.8 5.8 -831 8
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
CHEMBL395429 2983 None 40 Human Binding pKi = 5.8 5.8 -831 8
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
DB00107 2983 None 40 Human Binding pKi = 5.8 5.8 -831 8
Binding affinity to V2R (unknown origin)Binding affinity to V2R (unknown origin)
ChEMBL None None None None 10.1021/jm501395b
54585227 61207 None 0 Human Binding pKi = 5.8 5.8 -912 4
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 61207 None 0 Human Binding pKi = 5.8 5.8 -912 4
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 189135 None 0 Human Binding pKi = 7.8 7.8 2 2
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 189135 None 0 Human Binding pKi = 7.8 7.8 2 2
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 12582 None 0 Human Binding pKi = 7.8 7.8 - 1
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 12582 None 0 Human Binding pKi = 7.8 7.8 - 1
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 12582 None 0 Human Binding pKi = 7.8 7.8 - 1
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 202320 None 0 Human Binding pKi = 7.8 7.8 2 2
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 202320 None 0 Human Binding pKi = 7.8 7.8 2 2
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 82420 None 0 Human Binding pKi = 7.8 7.8 - 1
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 82420 None 0 Human Binding pKi = 7.8 7.8 - 1
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 157332 None 0 Human Binding pKi = 6.8 6.8 -23 2
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 157332 None 0 Human Binding pKi = 6.8 6.8 -23 2
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 164537 None 0 Human Binding pKi = 6.8 6.8 -3 3
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 164537 None 0 Human Binding pKi = 6.8 6.8 -3 3
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 5227 None 0 Human Binding pKi = 6.8 6.8 5 2
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 5227 None 0 Human Binding pKi = 6.8 6.8 5 2
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 211353 None 0 Rat Binding pKi = 5.8 5.8 -346 2
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 214076 None 0 Rat Binding pKi = 5.8 5.8 -19 2
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 96862 None 0 Rat Binding pKi = 4.8 4.8 -120226 3
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 96862 None 0 Rat Binding pKi = 4.8 4.8 -120226 3
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 2326 None 17 Human Binding pKi = 5.8 5.8 -7 3
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 2326 None 17 Human Binding pKi = 5.8 5.8 -7 3
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 2326 None 17 Human Binding pKi = 5.8 5.8 -7 3
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 2326 None 17 Human Binding pKi = 5.8 5.8 -7 3
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 66640 None 0 Rat Binding pKi = 6.8 6.8 -2 2
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 66640 None 0 Rat Binding pKi = 6.8 6.8 -2 2
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 66640 None 0 Rat Binding pKi = 6.8 6.8 -2 2
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligandEvaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
ChEMBL 491 2 3 5 5.1 Nc1nc(-c2ccc3c(c2)C(=Cc2cc(Br)c(O)c(Br)c2)C(=O)N3)cs1 10.1016/s0960-894x(01)00723-5
172452804 196725 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 458 3 0 4 7.2 Cc1ccc(F)cc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
CHEMBL5430804 196725 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assayDisplacement of conivaptan-red fluorescent probe from SNAP-tagged human vasopressin V2 receptor expressed in HEK293 cells compound pre-illuminated for 10 mins with light at 365 nm and further incubated for 1 hr by HTRF assay
ChEMBL 458 3 0 4 7.2 Cc1ccc(F)cc1/N=N\c1ccc(C(=O)N2Cc3cccn3Cc3ccccc32)c(Cl)c1 10.1021/acs.jmedchem.2c01625
44325377 111651 None 0 Human Binding pKi = 7.8 7.8 - 1
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 111651 None 0 Human Binding pKi = 7.8 7.8 - 1
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 159636 None 0 Human Binding pKi = 6.8 6.8 -26 2
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 159636 None 0 Human Binding pKi = 6.8 6.8 -26 2
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 12454 None 0 Human Binding pKi = 6.8 6.8 - 1
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 12454 None 0 Human Binding pKi = 6.8 6.8 - 1
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 12454 None 0 Human Binding pKi = 6.8 6.8 - 1
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 6853 None 0 Human Binding pKi = 6.8 6.8 -3 2
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 6853 None 0 Human Binding pKi = 6.8 6.8 -3 2
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 7098 None 0 Human Binding pKi = 6.8 6.8 -1 2
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 7098 None 0 Human Binding pKi = 6.8 6.8 -1 2
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 3311 None 35 Human Binding pKi = 6.8 6.8 -177 6
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 3311 None 35 Human Binding pKi = 6.8 6.8 -177 6
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 3311 None 35 Human Binding pKi = 6.8 6.8 -177 6
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 3311 None 35 Human Binding pKi = 6.8 6.8 -177 6
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 3311 None 35 Human Binding pKi = 6.8 6.8 -177 6
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 209143 None 0 Human Binding pKi = 5.8 5.8 -1698 4
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 209143 None 0 Human Binding pKi = 5.8 5.8 -1698 4
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 157474 None 0 Human Binding pKi = 5.8 5.8 -22 2
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 157474 None 0 Human Binding pKi = 5.8 5.8 -22 2
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 182134 None 0 Human Binding pKi = 7.8 7.8 -1 2
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 182134 None 0 Human Binding pKi = 7.8 7.8 -1 2
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 12681 None 0 Human Binding pKi = 7.8 7.8 - 1
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 12681 None 0 Human Binding pKi = 7.8 7.8 - 1
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 12681 None 0 Human Binding pKi = 7.8 7.8 - 1
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 190748 None 0 Human Binding pKi = 7.8 7.8 - 1
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 190748 None 0 Human Binding pKi = 7.8 7.8 - 1
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 209586 None 0 Human Binding pKi = 7.8 7.8 - 1
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 209586 None 0 Human Binding pKi = 7.8 7.8 - 1
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 108066 None 0 Human Binding pKi = 6.8 6.8 14 2
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 108066 None 0 Human Binding pKi = 6.8 6.8 14 2
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 73677 None 3 Human Binding pKi = 5.8 5.8 -112 3
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 73677 None 3 Human Binding pKi = 5.8 5.8 -112 3
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 118661 None 0 Human Binding pKi = 5.8 5.8 -10 2
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 118661 None 0 Human Binding pKi = 5.8 5.8 -10 2
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 73677 None 3 Human Binding pKi = 5.8 5.8 -112 3
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 73677 None 3 Human Binding pKi = 5.8 5.8 -112 3
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 218088 None 0 Rat Binding pKi = 5.8 5.8 -229 2
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 90714 None 1 Human Binding pKi = 6.7 6.7 -34 4
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 90714 None 1 Human Binding pKi = 6.7 6.7 -34 4
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 6675 None 0 Human Binding pKi = 5.7 5.7 -416 2
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 6675 None 0 Human Binding pKi = 5.7 5.7 -416 2
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 118661 None 0 Human Binding pKi = 6.7 6.7 -10 2
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 118661 None 0 Human Binding pKi = 6.7 6.7 -10 2
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 208685 None 0 Rat Binding pKi = 5.7 5.7 -1819 4
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 208685 None 0 Rat Binding pKi = 5.7 5.7 -1819 4
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 82410 None 0 Human Binding pKi = 6.7 6.7 1 2
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