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Assay Detail

CHEMBL818813

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

Binding
Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Vasopressin V2 receptor (CHEMBL3766)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 8 6.38 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307483 1 9.11
CHEMBL419667 RELCOVAPTAN 2.0 1 6.54
CHEMBL86577 1 6.44
CHEMBL86949 1 6.00
CHEMBL89552 1 5.91
CHEMBL86667 1 5.74
CHEMBL2112339 1 4.93
CHEMBL296908 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307483 Ki = 0.77 nM 9.11
CHEMBL419667 RELCOVAPTAN Ki = 285.0 nM 6.54
CHEMBL86577 Ki = 364.0 nM 6.44
CHEMBL86949 Ki = 1010.0 nM 6.00
CHEMBL89552 Ki = 1240.0 nM 5.91
CHEMBL86667 Ki = 1840.0 nM 5.74
CHEMBL2112339 Ki = 11700.0 nM 4.93
CHEMBL296908 Ki > 10000.0 nM -