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Assay Detail

CHEMBL3052668

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Binding
Antagonist activity at Oryctolagus cuniculus (rabbit) aortic AT1 receptor
ChEMBL ↗
100
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Insight into the structural requirement of aryltriazolinone derivatives as angiotensin II AT1 receptor: 2D and 3D-QSAR k-Nearest Neighbor Molecular Field Analysis approach
Sharma MC, Kohli DV
Med Chem Res (2012) 21 : 2837 -2853
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 100 9.53 10.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339672 — — 2 10.14
CHEMBL339722 — — 2 10.00
CHEMBL124771 — — 2 9.92
CHEMBL339256 — — 2 9.89
CHEMBL332576 — — 2 9.89
CHEMBL339605 — — 2 9.89
CHEMBL332909 — — 2 9.85
CHEMBL338101 — — 2 9.85
CHEMBL435811 — — 2 9.85
CHEMBL338027 — — 2 9.80
CHEMBL339004 — — 2 9.80
CHEMBL340632 — — 2 9.77
CHEMBL93907 — — 2 9.77
CHEMBL2236976 — — 2 9.72
CHEMBL125008 — — 2 9.72
CHEMBL122917 — — 2 9.70
CHEMBL331507 — — 2 9.70
CHEMBL334300 — — 2 9.68
CHEMBL341369 — — 2 9.68
CHEMBL125280 — — 2 9.66
CHEMBL122273 — — 2 9.66
CHEMBL122380 — — 2 9.64
CHEMBL331455 — — 2 9.62
CHEMBL338342 — — 2 9.62
CHEMBL125231 — — 2 9.60
CHEMBL338433 — — 2 9.59
CHEMBL444065 — — 2 9.59
CHEMBL339040 — — 2 9.57
CHEMBL339113 — — 2 9.55
CHEMBL121872 — — 2 9.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339672 — IC50 = 0.07211 nM 10.14
CHEMBL339672 — IC50 = 0.072 nM 10.14
CHEMBL339722 — IC50 = 0.1 nM 10.00
CHEMBL339722 — IC50 = 0.1 nM 10.00
CHEMBL124771 — IC50 = 0.1202 nM 9.92
CHEMBL124771 — IC50 = 0.12 nM 9.92
CHEMBL339256 — IC50 = 0.13 nM 9.89
CHEMBL332576 — IC50 = 0.13 nM 9.89
CHEMBL339605 — IC50 = 0.13 nM 9.89
CHEMBL332576 — IC50 = 0.13 nM 9.89
CHEMBL339256 — IC50 = 0.13 nM 9.89
CHEMBL339605 — IC50 = 0.13 nM 9.89
CHEMBL435811 — IC50 = 0.14 nM 9.85
CHEMBL338101 — IC50 = 0.1403 nM 9.85
CHEMBL435811 — IC50 = 0.1403 nM 9.85
CHEMBL332909 — IC50 = 0.14 nM 9.85
CHEMBL338101 — IC50 = 0.14 nM 9.85
CHEMBL332909 — IC50 = 0.1403 nM 9.85
CHEMBL339004 — IC50 = 0.16 nM 9.80
CHEMBL338027 — IC50 = 0.16 nM 9.80
CHEMBL339004 — IC50 = 0.1603 nM 9.79
CHEMBL338027 — IC50 = 0.1603 nM 9.79
CHEMBL93907 — IC50 = 0.1702 nM 9.77
CHEMBL340632 — IC50 = 0.17 nM 9.77
CHEMBL93907 — IC50 = 0.17 nM 9.77
CHEMBL340632 — IC50 = 0.1782 nM 9.75
CHEMBL2236976 — IC50 = 0.19 nM 9.72
CHEMBL125008 — IC50 = 0.1901 nM 9.72
CHEMBL125008 — IC50 = 0.19 nM 9.72
CHEMBL2236976 — IC50 = 0.1901 nM 9.72
CHEMBL331507 — IC50 = 0.2004 nM 9.70
CHEMBL331507 — IC50 = 0.2 nM 9.70
CHEMBL122917 — IC50 = 0.2004 nM 9.70
CHEMBL122917 — IC50 = 0.2 nM 9.70
CHEMBL341369 — IC50 = 0.21 nM 9.68
CHEMBL334300 — IC50 = 0.21 nM 9.68
CHEMBL341369 — IC50 = 0.2104 nM 9.68
CHEMBL334300 — IC50 = 0.2104 nM 9.68
CHEMBL125280 — IC50 = 0.22 nM 9.66
CHEMBL122273 — IC50 = 0.22 nM 9.66
CHEMBL125280 — IC50 = 0.2203 nM 9.66
CHEMBL122273 — IC50 = 0.2203 nM 9.66
CHEMBL122380 — IC50 = 0.23 nM 9.64
CHEMBL122380 — IC50 = 0.2301 nM 9.64
CHEMBL338342 — IC50 = 0.24 nM 9.62
CHEMBL338342 — IC50 = 0.2404 nM 9.62
CHEMBL331455 — IC50 = 0.24 nM 9.62
CHEMBL331455 — IC50 = 0.2404 nM 9.62
CHEMBL125231 — IC50 = 0.25 nM 9.60
CHEMBL125231 — IC50 = 0.25 nM 9.60