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Assay Detail

CHEMBL648855

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Binding
In vitro inhibitory activity against Angiotensin II receptor, type 1 in rabbit aorta membrane preparations.
ChEMBL ↗
54
Total Activities
54
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 Intermediate

Target

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

Publication

Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes.
Chang LL, Ashton WT, Flanagan KL, Chen TB, O'Malley SS, Zingaro GJ, Kivlighn SD, Siegl PK, Lotti VJ, Chang RS.
J Med Chem (1995) 38 : 3741 -3758
PubMed 7562905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 9.47 10.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339672 — — 1 10.14
CHEMBL339722 — — 1 10.00
CHEMBL124771 — — 1 9.92
CHEMBL339256 — — 1 9.89
CHEMBL339605 — — 1 9.89
CHEMBL332576 — — 1 9.89
CHEMBL332909 — — 1 9.85
CHEMBL338101 — — 1 9.85
CHEMBL435811 — — 1 9.85
CHEMBL339004 — — 1 9.80
CHEMBL338027 — — 1 9.80
CHEMBL340632 — — 1 9.77
CHEMBL93907 — — 1 9.77
CHEMBL125008 — — 1 9.72
CHEMBL331450 — — 1 9.72
CHEMBL122917 — — 1 9.70
CHEMBL331507 — — 1 9.70
CHEMBL334300 — — 1 9.68
CHEMBL341369 — — 1 9.68
CHEMBL125280 — — 1 9.66
CHEMBL122273 — — 1 9.66
CHEMBL122380 — — 1 9.64
CHEMBL338342 — — 1 9.62
CHEMBL331455 — — 1 9.62
CHEMBL125231 — — 1 9.60
CHEMBL338433 — — 1 9.59
CHEMBL444065 — — 1 9.59
CHEMBL339040 — — 1 9.57
CHEMBL121872 — — 1 9.55
CHEMBL339113 — — 1 9.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339672 — IC50 = 0.072 nM 10.14
CHEMBL339722 — IC50 = 0.1 nM 10.00
CHEMBL124771 — IC50 = 0.12 nM 9.92
CHEMBL339256 — IC50 = 0.13 nM 9.89
CHEMBL339605 — IC50 = 0.13 nM 9.89
CHEMBL332576 — IC50 = 0.13 nM 9.89
CHEMBL332909 — IC50 = 0.14 nM 9.85
CHEMBL338101 — IC50 = 0.14 nM 9.85
CHEMBL435811 — IC50 = 0.14 nM 9.85
CHEMBL339004 — IC50 = 0.16 nM 9.80
CHEMBL338027 — IC50 = 0.16 nM 9.80
CHEMBL340632 — IC50 = 0.17 nM 9.77
CHEMBL93907 — IC50 = 0.17 nM 9.77
CHEMBL331450 — IC50 = 0.19 nM 9.72
CHEMBL125008 — IC50 = 0.19 nM 9.72
CHEMBL122917 — IC50 = 0.2 nM 9.70
CHEMBL331507 — IC50 = 0.2 nM 9.70
CHEMBL334300 — IC50 = 0.21 nM 9.68
CHEMBL341369 — IC50 = 0.21 nM 9.68
CHEMBL125280 — IC50 = 0.22 nM 9.66
CHEMBL122273 — IC50 = 0.22 nM 9.66
CHEMBL122380 — IC50 = 0.23 nM 9.64
CHEMBL338342 — IC50 = 0.24 nM 9.62
CHEMBL331455 — IC50 = 0.24 nM 9.62
CHEMBL125231 — IC50 = 0.25 nM 9.60
CHEMBL338433 — IC50 = 0.26 nM 9.59
CHEMBL444065 — IC50 = 0.26 nM 9.59
CHEMBL339040 — IC50 = 0.27 nM 9.57
CHEMBL121872 — IC50 = 0.28 nM 9.55
CHEMBL339113 — IC50 = 0.28 nM 9.55
CHEMBL276674 — IC50 = 0.29 nM 9.54
CHEMBL436396 — IC50 = 0.35 nM 9.46
CHEMBL340078 — IC50 = 0.36 nM 9.44
CHEMBL340473 — IC50 = 0.37 nM 9.43
CHEMBL333224 — IC50 = 0.38 nM 9.42
CHEMBL338137 — IC50 = 0.38 nM 9.42
CHEMBL122158 — IC50 = 0.38 nM 9.42
CHEMBL338889 — IC50 = 0.41 nM 9.39
CHEMBL338434 — IC50 = 0.42 nM 9.38
CHEMBL279629 L-159913 IC50 = 0.43 nM 9.37
CHEMBL121907 — IC50 = 0.44 nM 9.36
CHEMBL122401 — IC50 = 0.44 nM 9.36
CHEMBL338888 — IC50 = 0.51 nM 9.29
CHEMBL124903 — IC50 = 0.53 nM 9.28
CHEMBL122157 — IC50 = 0.56 nM 9.25
CHEMBL338687 — IC50 = 0.82 nM 9.09
CHEMBL323506 — IC50 = 0.84 nM 9.08
CHEMBL421478 — IC50 = 0.91 nM 9.04
CHEMBL273542 — IC50 = 1.5 nM 8.82
CHEMBL302102 — IC50 = 1.7 nM 8.77