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Assay Detail

CHEMBL876759

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

Binding
In vitro binding affinity towards Angiotensin II receptor, type 1 of human hepatoma cell line PLC-PRF-5
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Comparison of 3D structures and AT(1) binding properties of pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones with parent antihypertensive drug irbesartan.
Le Bourdonnec B, Cauvin C, Meulon E, Yous S, Goossens JF, Durant F, Houssin R, Hénichart JP.
J Med Chem (2002) 45 : 4794 -4798
PubMed 12361407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.81 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1513 IRBESARTAN 4.0 1 8.70
CHEMBL358359 1 7.85
CHEMBL315444 1 7.60
CHEMBL146275 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1513 IRBESARTAN Ki = 2.0 nM 8.70
CHEMBL358359 Ki = 14.0 nM 7.85
CHEMBL315444 Ki = 25.0 nM 7.60
CHEMBL146275 Ki = 80.0 nM 7.10