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Assay Detail

CHEMBL2428850

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

Binding
Antagonist activity at AT1 receptor in rabbit aorta membranes
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Comparative QSAR and pharmacophore analysis for a series of 2,4-dihydro-3H-1,2,4-triazol-3-ones derivatives as angiotensin II AT1 receptor antagonists
Sharma MC, Sharma S, Sharma P, Kumar A, Bhadoriya KS
Med Chem Res (2013) : 1 -17
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 9.41 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138690 — — 1 10.37
CHEMBL265797 — — 1 10.28
CHEMBL341828 — — 1 10.14
CHEMBL343309 — — 1 10.10
CHEMBL316300 — — 1 9.96
CHEMBL341934 — — 1 9.96
CHEMBL343142 — — 1 9.96
CHEMBL140708 — — 1 9.92
CHEMBL338101 — — 1 9.85
CHEMBL139452 — — 1 9.85
CHEMBL96075 — — 1 9.80
CHEMBL136465 — — 1 9.80
CHEMBL93907 — — 1 9.77
CHEMBL337118 — — 1 9.74
CHEMBL435792 — — 1 9.68
CHEMBL334300 — — 1 9.68
CHEMBL275552 — — 1 9.68
CHEMBL341783 — — 1 9.60
CHEMBL344597 — — 1 9.60
CHEMBL139041 — — 1 9.59
CHEMBL276674 — — 1 9.54
CHEMBL343634 — — 1 9.52
CHEMBL342492 — — 1 9.43
CHEMBL139325 — — 1 9.39
CHEMBL141592 — — 1 9.39
CHEMBL342605 — — 1 9.38
CHEMBL279629 L-159913 — 1 9.37
CHEMBL292150 — — 1 9.35
CHEMBL342843 — — 1 9.25
CHEMBL344387 — — 1 9.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138690 — IC50 = 0.043 nM 10.37
CHEMBL265797 — IC50 = 0.052 nM 10.28
CHEMBL341828 — IC50 = 0.072 nM 10.14
CHEMBL343309 — IC50 = 0.08 nM 10.10
CHEMBL316300 — IC50 = 0.11 nM 9.96
CHEMBL341934 — IC50 = 0.11 nM 9.96
CHEMBL343142 — IC50 = 0.11 nM 9.96
CHEMBL140708 — IC50 = 0.12 nM 9.92
CHEMBL338101 — IC50 = 0.14 nM 9.85
CHEMBL139452 — IC50 = 0.14 nM 9.85
CHEMBL96075 — IC50 = 0.16 nM 9.80
CHEMBL136465 — IC50 = 0.16 nM 9.80
CHEMBL93907 — IC50 = 0.17 nM 9.77
CHEMBL337118 — IC50 = 0.18 nM 9.74
CHEMBL275552 — IC50 = 0.21 nM 9.68
CHEMBL435792 — IC50 = 0.21 nM 9.68
CHEMBL334300 — IC50 = 0.21 nM 9.68
CHEMBL341783 — IC50 = 0.25 nM 9.60
CHEMBL344597 — IC50 = 0.25 nM 9.60
CHEMBL139041 — IC50 = 0.26 nM 9.59
CHEMBL276674 — IC50 = 0.29 nM 9.54
CHEMBL343634 — IC50 = 0.3 nM 9.52
CHEMBL342492 — IC50 = 0.37 nM 9.43
CHEMBL139325 — IC50 = 0.41 nM 9.39
CHEMBL141592 — IC50 = 0.41 nM 9.39
CHEMBL342605 — IC50 = 0.42 nM 9.38
CHEMBL279629 L-159913 IC50 = 0.43 nM 9.37
CHEMBL292150 — IC50 = 0.45 nM 9.35
CHEMBL342843 — IC50 = 0.56 nM 9.25
CHEMBL344387 — IC50 = 0.56 nM 9.25
CHEMBL344811 — IC50 = 0.63 nM 9.20
CHEMBL2425239 — IC50 = 0.78 nM 9.11
CHEMBL344467 — IC50 = 0.85 nM 9.07
CHEMBL140619 — IC50 = 0.9 nM 9.05
CHEMBL139582 — IC50 = 1.0 nM 9.00
CHEMBL337588 — IC50 = 1.4 nM 8.85
CHEMBL341715 — IC50 = 1.6 nM 8.80
CHEMBL138654 — IC50 = 1.8 nM 8.74
CHEMBL344466 — IC50 = 2.4 nM 8.62
CHEMBL343719 — IC50 = 5.8 nM 8.24
CHEMBL2425138 — IC50 = 24.0 nM 7.62
CHEMBL293501 — IC50 = 31.0 nM 7.51