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Assay Detail

CHEMBL1670350

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

Functional
Antagonist activity at angiotensin AT1 receptor in rabbit aortic strip assessed as inhibition of angiotensin 2-induced contractile response
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Type-1 angiotensin II receptor (CHEMBL3948)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.
Naik P, Murumkar P, Giridhar R, Yadav MR.
Bioorg Med Chem (2010) 18 : 8418 -8456
PubMed 21071232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 8.55 9.20
IC50 2 8.48 10.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48242 1 10.26
CHEMBL433895 1 9.20
CHEMBL123713 1 7.90
CHEMBL1014 CANDESARTAN CILEXETIL 4.0 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48242 IC50 = 0.055 nM 10.26
CHEMBL433895 Kd = 0.631 nM 9.20
CHEMBL123713 Kd = 12.59 nM 7.90
CHEMBL1014 CANDESARTAN CILEXETIL IC50 = 200.0 nM 6.70