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Assay Detail

CHEMBL815443

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Binding
Evaluated for the binding affinity towards vasopressin (V1A) receptor in rat liver membrane using [3H]AVP as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vasopressin V1a receptor (CHEMBL2868)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
Kakefuda A, Tsukada J, Kusayama T, Tahara A, Tsukamoto S.
Bioorg Med Chem Lett (2002) 12 : 229 -232
PubMed 11755361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.84 9.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310921 1 9.99
CHEMBL307483 1 9.21
CHEMBL306718 1 8.53
CHEMBL77105 1 8.30
CHEMBL307269 1 8.24
CHEMBL75489 1 8.12
CHEMBL74593 1 8.06
CHEMBL1794053 GW407323A 1 7.11
CHEMBL307487 1 6.47
CHEMBL76498 1 6.31
CHEMBL76763 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310921 Ki = 0.102 nM 9.99
CHEMBL307483 Ki = 0.62 nM 9.21
CHEMBL306718 Ki = 2.93 nM 8.53
CHEMBL77105 Ki = 4.97 nM 8.30
CHEMBL307269 Ki = 5.71 nM 8.24
CHEMBL75489 Ki = 7.59 nM 8.12
CHEMBL74593 Ki = 8.77 nM 8.06
CHEMBL1794053 GW407323A Ki = 78.6 nM 7.11
CHEMBL307487 Ki = 335.0 nM 6.47
CHEMBL76498 Ki = 491.0 nM 6.31
CHEMBL76763 Ki = 1140.0 nM 5.94