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Assay Detail

CHEMBL650318

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

Binding
Binding affinity against AT1 in human hepatoma cell line, PLC-PRF-5
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.
Le Bourdonnec B, Meulon E, Yous S, Goossens JF, Houssin R, Hénichart JP.
J Med Chem (2000) 43 : 2685 -2697
PubMed 10893306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.02 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1513 IRBESARTAN 4.0 1 8.70
CHEMBL91113 1 8.00
CHEMBL90872 1 7.89
CHEMBL315444 1 7.60
CHEMBL90483 1 7.60
CHEMBL313392 1 7.50
CHEMBL315873 1 7.50
CHEMBL92225 1 7.40
CHEMBL88924 1 7.38
CHEMBL90411 1 6.80
CHEMBL90999 1 6.42
CHEMBL327594 1 6.40
CHEMBL88471 1 6.40
CHEMBL90187 1 5.70
CHEMBL90887 1 5.50
CHEMBL90885 1 5.48
CHEMBL328484 1 -
CHEMBL90629 1 -
CHEMBL91069 1 -
CHEMBL90257 1 -
CHEMBL88131 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1513 IRBESARTAN Ki = 2.0 nM 8.70
CHEMBL91113 Ki = 10.0 nM 8.00
CHEMBL90872 Ki = 13.0 nM 7.89
CHEMBL315444 Ki = 25.0 nM 7.60
CHEMBL90483 Ki = 25.0 nM 7.60
CHEMBL313392 Ki = 32.0 nM 7.50
CHEMBL315873 Ki = 32.0 nM 7.50
CHEMBL92225 Ki = 40.0 nM 7.40
CHEMBL88924 Ki = 42.0 nM 7.38
CHEMBL90411 Ki = 158.0 nM 6.80
CHEMBL90999 Ki = 381.0 nM 6.42
CHEMBL327594 Ki = 402.0 nM 6.40
CHEMBL88471 Ki = 398.0 nM 6.40
CHEMBL90187 Ki = 1995.0 nM 5.70
CHEMBL90887 Ki = 3162.0 nM 5.50
CHEMBL90885 Ki = 3301.0 nM 5.48
CHEMBL328484 Ki > 10000.0 nM -
CHEMBL90629 Ki > 10000.0 nM -
CHEMBL91069 Ki > 10000.0 nM -
CHEMBL90257 Ki > 10000.0 nM -
CHEMBL88131 Ki > 10000.0 nM -