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Assay Detail

CHEMBL650154

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

Binding
Binding affinity towards Angiotensin receptor from rabbit aorta
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094256)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
Mantlo NB, Chakravarty PK, Ondeyka DL, Siegl PK, Chang RS, Lotti VJ, Faust KA, Chen TB, Schorn TW, Sweet CS.
J Med Chem (1991) 34 : 2919 -2922
PubMed 1895308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.82 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2369937 1 9.70
CHEMBL315104 1 9.52
CHEMBL7550 L-158809 1 9.52
CHEMBL98907 1 9.30
CHEMBL296725 1 9.00
CHEMBL99991 1 8.70
CHEMBL317360 1 8.22
CHEMBL99751 1 8.10
CHEMBL191 LOSARTAN 4.0 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2369937 IC50 = 0.2 nM 9.70
CHEMBL315104 IC50 = 0.3 nM 9.52
CHEMBL7550 L-158809 IC50 = 0.3 nM 9.52
CHEMBL98907 IC50 = 0.5 nM 9.30
CHEMBL296725 IC50 = 1.0 nM 9.00
CHEMBL99991 IC50 = 2.0 nM 8.70
CHEMBL317360 IC50 = 6.0 nM 8.22
CHEMBL99751 IC50 = 8.0 nM 8.10
CHEMBL191 LOSARTAN IC50 = 50.0 nM 7.30