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Assay Detail

CHEMBL4146907

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

Binding
Displacement of [125I-Sar1-Ile8]-Ang2 from human angiotensin 2 receptor type 1 receptor expressed in HEK293 cells after 1 hr by gamma counting analysis
6
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL227)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Integration of multi-scale molecular modeling approaches with experiments for the in silico guided design and discovery of novel hERG-Neutral antihypertensive oxazalone and imidazolone derivatives and analysis of their potential restrictive effects on cell proliferation.
Durdagi S, Aksoydan B, Erol I, Kantarcioglu I, Ergun Y, Bulut G, Acar M, Avsar T, Liapakis G, Karageorgos V, Salmas RE, Sergi B, Alkhatib S, Turan G, Yigit BN, Cantasir K, Kurt B, Kilic T.
Eur J Med Chem (2018) 145 : 273 -290
PubMed 29329002 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 7.30 8.87
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4160691 1 8.87
CHEMBL1069 VALSARTAN 4.0 1 8.52
CHEMBL1016 CANDESARTAN 3.0 1 7.98
CHEMBL4175147 2 6.50
CHEMBL4164514 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4160691 Ki = 1.35 nM 8.87
CHEMBL1069 VALSARTAN Ki = 3.0 nM 8.52
CHEMBL1016 CANDESARTAN Ki = 10.4 nM 7.98
CHEMBL4175147 Ki = 317.0 nM 6.50
CHEMBL4164514 Ki = 24838.0 nM 4.61
CHEMBL4175147 Inhibition - % -