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Assay Detail

CHEMBL647290

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

Binding
In vivo inhibitory concentration against Angiotensin II receptor, type 1 of rabbit aorta membrane
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Development of angiotensin II antagonists with equipotent affinity for human AT1 and AT2 receptor subtypes.
Glinka TW, de Laszlo SE, Siegl PK, Chang RS, Kivlighn SD, Schorn TS, Faust KA, Chen T, Zingaro GJ, Lotti VJ, Greenlee WJ
Bioorg Med Chem Lett (1994) 4 : 2337 -2342
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 9.13 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL306362 1 9.89
CHEMBL311160 1 9.72
CHEMBL415073 1 9.72
CHEMBL305647 1 9.70
CHEMBL74556 1 9.64
CHEMBL74476 1 9.62
CHEMBL259843 1 9.62
CHEMBL263191 1 9.28
CHEMBL263452 1 9.27
CHEMBL73876 1 9.24
CHEMBL74442 1 9.21
CHEMBL306361 1 9.14
CHEMBL76821 1 9.11
CHEMBL307430 1 9.04
CHEMBL194608 1 8.92
CHEMBL302102 1 8.82
CHEMBL17487 1 8.70
CHEMBL311386 1 8.66
CHEMBL75401 1 8.64
CHEMBL305956 1 8.64
CHEMBL74144 1 8.64
CHEMBL307290 1 8.42
CHEMBL311484 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL306362 IC50 = 0.13 nM 9.89
CHEMBL311160 IC50 = 0.19 nM 9.72
CHEMBL415073 IC50 = 0.19 nM 9.72
CHEMBL305647 IC50 = 0.2 nM 9.70
CHEMBL74556 IC50 = 0.23 nM 9.64
CHEMBL74476 IC50 = 0.24 nM 9.62
CHEMBL259843 IC50 = 0.24 nM 9.62
CHEMBL263191 IC50 = 0.52 nM 9.28
CHEMBL263452 IC50 = 0.54 nM 9.27
CHEMBL73876 IC50 = 0.57 nM 9.24
CHEMBL74442 IC50 = 0.62 nM 9.21
CHEMBL306361 IC50 = 0.73 nM 9.14
CHEMBL76821 IC50 = 0.77 nM 9.11
CHEMBL307430 IC50 = 0.92 nM 9.04
CHEMBL194608 IC50 = 1.2 nM 8.92
CHEMBL302102 IC50 = 1.5 nM 8.82
CHEMBL17487 IC50 = 2.0 nM 8.70
CHEMBL311386 IC50 = 2.2 nM 8.66
CHEMBL75401 IC50 = 2.3 nM 8.64
CHEMBL305956 IC50 = 2.3 nM 8.64
CHEMBL74144 IC50 = 2.3 nM 8.64
CHEMBL307290 IC50 = 3.8 nM 8.42
CHEMBL311484 IC50 = 4.0 nM 8.40