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Assay Detail

CHEMBL1670311

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

Functional
Antagonist activity at angiotensin AT1 receptor in rabbit aorta assessed as reduction of angiotensin 2-induced contractile response
6
Total Activities
5
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
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 4 9.04 10.09
Kb 1 - -
IC50 1 9.26 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE 2 10.09
CHEMBL332897 1 9.26
CHEMBL87778 1 8.86
CHEMBL352257 1 8.82
CHEMBL340315 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL907 CARBOXYLIC ACID METABOLITE Kd = 0.08128 nM 10.09
CHEMBL332897 IC50 = 0.55 nM 9.26
CHEMBL87778 Kd = 1.38 nM 8.86
CHEMBL352257 Kd = 1.514 nM 8.82
CHEMBL340315 Kd = 3.981 nM 8.40
CHEMBL907 CARBOXYLIC ACID METABOLITE Kb = 0.1 nM -