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Assay Detail

CHEMBL648856

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

Binding
In vitro inhibitory activity against Angiotensin II receptor, type 1 to displace 125I-Sar,Ile8-AII in rabbit aorta
25
Total Activities
25
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 Intermediate

Target

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

Publication

Potent imidazole angiotensinII antagonists: acyl sulfonamides and acyl sulfamides as tetrazole replacements
Naylor EM, Chakravarty PK, Costello CA, Chang RS, Chen T, Faust KA, Lotti VJ, Kivlighn SD, Zingaro GJ, Siegl PK, Wong PC, Carini DJ, Wexler RR, Patchett AA, Greenlee WJ
Bioorg Med Chem Lett (1994) 4 : 69 -74
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 8.23 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL350121 1 9.70
CHEMBL162148 1 9.30
CHEMBL165349 1 8.77
CHEMBL348758 1 8.72
CHEMBL165354 1 8.70
CHEMBL59957 1 8.62
CHEMBL163486 1 8.59
CHEMBL349389 1 8.54
CHEMBL164059 1 8.37
CHEMBL349856 1 8.24
CHEMBL423801 1 8.22
CHEMBL115021 1 8.22
CHEMBL162859 1 8.21
CHEMBL352675 1 8.15
CHEMBL163485 1 8.13
CHEMBL291582 1 8.10
CHEMBL350493 1 8.06
CHEMBL349869 1 7.92
CHEMBL164617 1 7.89
CHEMBL422200 1 7.82
CHEMBL349652 1 7.70
CHEMBL163628 1 7.68
CHEMBL350851 1 7.50
CHEMBL349020 1 7.41
CHEMBL164552 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL350121 IC50 = 0.2 nM 9.70
CHEMBL162148 IC50 = 0.5 nM 9.30
CHEMBL165349 IC50 = 1.7 nM 8.77
CHEMBL348758 IC50 = 1.9 nM 8.72
CHEMBL165354 IC50 = 2.0 nM 8.70
CHEMBL59957 IC50 = 2.4 nM 8.62
CHEMBL163486 IC50 = 2.6 nM 8.59
CHEMBL349389 IC50 = 2.9 nM 8.54
CHEMBL164059 IC50 = 4.3 nM 8.37
CHEMBL349856 IC50 = 5.8 nM 8.24
CHEMBL423801 IC50 = 6.0 nM 8.22
CHEMBL115021 IC50 = 6.0 nM 8.22
CHEMBL162859 IC50 = 6.2 nM 8.21
CHEMBL352675 IC50 = 7.0 nM 8.15
CHEMBL163485 IC50 = 7.4 nM 8.13
CHEMBL291582 IC50 = 8.0 nM 8.10
CHEMBL350493 IC50 = 8.8 nM 8.06
CHEMBL349869 IC50 = 12.0 nM 7.92
CHEMBL164617 IC50 = 13.0 nM 7.89
CHEMBL422200 IC50 = 15.0 nM 7.82
CHEMBL349652 IC50 = 20.0 nM 7.70
CHEMBL163628 IC50 = 21.0 nM 7.68
CHEMBL350851 IC50 = 32.0 nM 7.50
CHEMBL349020 IC50 = 39.0 nM 7.41
CHEMBL164552 IC50 = 50.0 nM 7.30