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Assay Detail

CHEMBL817919

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Vasopressin V2 receptor (CHEMBL1790)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor.
Kakefuda A, Suzuki T, Tobe T, Tsukada J, Tahara A, Sakamoto S, Tsukamoto S.
J Med Chem (2002) 45 : 2589 -2598
PubMed 12036368 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 5.55 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307483 1 8.92
CHEMBL419667 RELCOVAPTAN 2.0 1 6.75
CHEMBL86577 1 6.23
CHEMBL86949 1 6.01
CHEMBL89552 1 5.75
CHEMBL86667 1 5.72
CHEMBL87351 1 5.61
CHEMBL87887 1 5.61
CHEMBL432375 1 5.35
CHEMBL86384 1 5.31
CHEMBL86936 1 5.18
CHEMBL87455 1 5.16
CHEMBL315232 1 5.13
CHEMBL315251 1 5.09
CHEMBL316093 1 5.07
CHEMBL313451 1 5.05
CHEMBL315524 1 4.99
CHEMBL329209 1 4.99
CHEMBL89177 1 4.96
CHEMBL314908 1 4.84
CHEMBL2112339 1 4.84
CHEMBL296908 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307483 Ki = 1.19 nM 8.92
CHEMBL419667 RELCOVAPTAN Ki = 178.0 nM 6.75
CHEMBL86577 Ki = 585.0 nM 6.23
CHEMBL86949 Ki = 979.0 nM 6.01
CHEMBL89552 Ki = 1780.0 nM 5.75
CHEMBL86667 Ki = 1920.0 nM 5.72
CHEMBL87351 Ki = 2460.0 nM 5.61
CHEMBL87887 Ki = 2470.0 nM 5.61
CHEMBL432375 Ki = 4430.0 nM 5.35
CHEMBL86384 Ki = 4850.0 nM 5.31
CHEMBL86936 Ki = 6650.0 nM 5.18
CHEMBL87455 Ki = 6930.0 nM 5.16
CHEMBL315232 Ki = 7370.0 nM 5.13
CHEMBL315251 Ki = 8170.0 nM 5.09
CHEMBL316093 Ki = 8520.0 nM 5.07
CHEMBL313451 Ki = 8890.0 nM 5.05
CHEMBL315524 Ki = 10200.0 nM 4.99
CHEMBL329209 Ki = 10200.0 nM 4.99
CHEMBL89177 Ki = 11100.0 nM 4.96
CHEMBL314908 Ki = 14300.0 nM 4.84
CHEMBL2112339 Ki = 14400.0 nM 4.84
CHEMBL296908 Ki > 10000.0 nM -