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Assay Detail

CHEMBL885387

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Binding
Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney 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 Kidney
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Vasopressin V2 receptor (CHEMBL3766)
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 6.76 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307483 1 8.92
CHEMBL310921 1 7.47
CHEMBL306718 1 7.38
CHEMBL74593 1 7.13
CHEMBL77105 1 7.03
CHEMBL1794053 GW407323A 1 6.78
CHEMBL75489 1 6.35
CHEMBL307269 1 6.11
CHEMBL76498 1 5.87
CHEMBL307487 1 5.69
CHEMBL76763 1 5.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307483 Ki = 1.19 nM 8.92
CHEMBL310921 Ki = 33.9 nM 7.47
CHEMBL306718 Ki = 41.5 nM 7.38
CHEMBL74593 Ki = 73.4 nM 7.13
CHEMBL77105 Ki = 94.5 nM 7.03
CHEMBL1794053 GW407323A Ki = 168.0 nM 6.78
CHEMBL75489 Ki = 445.0 nM 6.35
CHEMBL307269 Ki = 782.0 nM 6.11
CHEMBL76498 Ki = 1360.0 nM 5.87
CHEMBL307487 Ki = 2040.0 nM 5.69
CHEMBL76763 Ki = 2250.0 nM 5.65