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Assay Detail

CHEMBL644580

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Binding
Binding affinity against angiotensin II receptor type 1 (AT1) from rat liver.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-1 angiotensin II receptor B (CHEMBL263)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Nonpeptide angiotensin II receptor antagonists. 1. Synthesis and in vitro structure-activity relationships of 4-[[[(1H-pyrrol-1-ylacetyl)amino]phenyl]methyl]imidazole derivatives as angiotensin II receptor antagonists.
Sircar I, Winters RT, Quin J, Lu GH, Major TC, Panek RL.
J Med Chem (1993) 36 : 1735 -1745
PubMed 8510101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 6.47 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191 LOSARTAN 4.0 1 8.30
CHEMBL301705 1 7.70
CHEMBL48824 1 7.66
CHEMBL299130 1 7.62
CHEMBL297653 1 7.57
CHEMBL48363 1 7.22
CHEMBL48195 1 7.10
CHEMBL49170 1 7.04
CHEMBL45659 1 6.85
CHEMBL262958 1 6.85
CHEMBL48168 1 6.85
CHEMBL49526 1 6.75
CHEMBL45814 1 6.75
CHEMBL49306 1 6.68
CHEMBL295311 1 6.68
CHEMBL297202 1 6.68
CHEMBL295737 1 6.62
CHEMBL274447 1 6.52
CHEMBL48640 1 6.48
CHEMBL300487 1 6.47
CHEMBL48486 1 6.43
CHEMBL299557 1 6.30
CHEMBL49748 1 6.23
CHEMBL49954 1 6.17
CHEMBL288753 1 6.10
CHEMBL48756 1 6.03
CHEMBL301328 1 5.96
CHEMBL297465 1 5.95
CHEMBL48798 1 5.89
CHEMBL297265 1 5.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191 LOSARTAN IC50 = 5.0 nM 8.30
CHEMBL301705 IC50 = 20.0 nM 7.70
CHEMBL48824 IC50 = 22.0 nM 7.66
CHEMBL299130 IC50 = 24.0 nM 7.62
CHEMBL297653 IC50 = 27.0 nM 7.57
CHEMBL48363 IC50 = 60.0 nM 7.22
CHEMBL48195 IC50 = 80.0 nM 7.10
CHEMBL49170 IC50 = 92.0 nM 7.04
CHEMBL48168 IC50 = 140.0 nM 6.85
CHEMBL262958 IC50 = 140.0 nM 6.85
CHEMBL45659 IC50 = 140.0 nM 6.85
CHEMBL49526 IC50 = 180.0 nM 6.75
CHEMBL45814 IC50 = 180.0 nM 6.75
CHEMBL297202 IC50 = 210.0 nM 6.68
CHEMBL295311 IC50 = 210.0 nM 6.68
CHEMBL49306 IC50 = 210.0 nM 6.68
CHEMBL295737 IC50 = 240.0 nM 6.62
CHEMBL274447 IC50 = 300.0 nM 6.52
CHEMBL48640 IC50 = 330.0 nM 6.48
CHEMBL300487 IC50 = 340.0 nM 6.47
CHEMBL48486 IC50 = 370.0 nM 6.43
CHEMBL299557 IC50 = 500.0 nM 6.30
CHEMBL49748 IC50 = 590.0 nM 6.23
CHEMBL49954 IC50 = 670.0 nM 6.17
CHEMBL288753 IC50 = 800.0 nM 6.10
CHEMBL48756 IC50 = 930.0 nM 6.03
CHEMBL301328 IC50 = 1100.0 nM 5.96
CHEMBL297465 IC50 = 1120.0 nM 5.95
CHEMBL48798 IC50 = 1290.0 nM 5.89
CHEMBL297265 IC50 = 1470.0 nM 5.83
CHEMBL299324 IC50 = 1920.0 nM 5.72
CHEMBL49257 IC50 = 2500.0 nM 5.60
CHEMBL299105 IC50 = 2600.0 nM 5.58
CHEMBL417009 IC50 = 2600.0 nM 5.58
CHEMBL298364 IC50 = 3250.0 nM 5.49
CHEMBL48526 IC50 = 8370.0 nM 5.08
CHEMBL48955 IC50 = 10900.0 nM 4.96