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Assay Detail

CHEMBL974599

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Functional
Antagonist activity at vasopressin V1a receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Vasopressin V1a receptor (CHEMBL1889)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and optimization of potent, selective antagonists of Oxytocin.
Brown A, Brown L, Ellis D, Puhalo N, Smith CR, Wallace O, Watson L.
Bioorg Med Chem Lett (2008) 18 : 4278 -4281
PubMed 18639455 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.36 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL467154 1 7.55
CHEMBL512257 1 7.36
CHEMBL467186 1 6.88
CHEMBL467545 1 6.70
CHEMBL467185 1 6.57
CHEMBL467378 1 6.41
CHEMBL511215 1 6.37
CHEMBL467184 1 6.28
CHEMBL466762 1 6.13
CHEMBL511265 1 5.91
CHEMBL511917 1 5.62
CHEMBL512105 1 5.49
CHEMBL469005 1 5.37
CHEMBL467546 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL467154 Ki = 28.0 nM 7.55
CHEMBL512257 Ki = 44.0 nM 7.36
CHEMBL467186 Ki = 132.0 nM 6.88
CHEMBL467545 Ki = 202.0 nM 6.70
CHEMBL467185 Ki = 270.0 nM 6.57
CHEMBL467378 Ki = 388.0 nM 6.41
CHEMBL511215 Ki = 432.0 nM 6.37
CHEMBL467184 Ki = 525.0 nM 6.28
CHEMBL466762 Ki = 732.0 nM 6.13
CHEMBL511265 Ki = 1220.0 nM 5.91
CHEMBL511917 Ki = 2410.0 nM 5.62
CHEMBL512105 Ki = 3230.0 nM 5.49
CHEMBL469005 Ki = 4300.0 nM 5.37
CHEMBL467546 Ki - -