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Assay Detail

CHEMBL650312

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Binding
In vitro inhibitory activity against angiotensin II receptor type 1, in human adrenal membrane preparations.
ChEMBL ↗
48
Total Activities
48
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 (CHEMBL227) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 48 8.87 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL435811 — — 1 9.85
CHEMBL334300 — — 1 9.55
CHEMBL332909 — — 1 9.49
CHEMBL339672 — — 1 9.49
CHEMBL436396 — — 1 9.47
CHEMBL125280 — — 1 9.44
CHEMBL444065 — — 1 9.40
CHEMBL341369 — — 1 9.37
CHEMBL339256 — — 1 9.37
CHEMBL339605 — — 1 9.36
CHEMBL331455 — — 1 9.35
CHEMBL124771 — — 1 9.30
CHEMBL339004 — — 1 9.26
CHEMBL339722 — — 1 9.25
CHEMBL339040 — — 1 9.19
CHEMBL122273 — — 1 9.14
CHEMBL339113 — — 1 9.13
CHEMBL340632 — — 1 9.12
CHEMBL121872 — — 1 9.08
CHEMBL121907 — — 1 9.06
CHEMBL338434 — — 1 9.05
CHEMBL338433 — — 1 9.03
CHEMBL340078 — — 1 9.02
CHEMBL331450 — — 1 9.00
CHEMBL331507 — — 1 9.00
CHEMBL122917 — — 1 9.00
CHEMBL125008 — — 1 8.96
CHEMBL338137 — — 1 8.85
CHEMBL340473 — — 1 8.82
CHEMBL122158 — — 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL435811 — IC50 = 0.14 nM 9.85
CHEMBL334300 — IC50 = 0.28 nM 9.55
CHEMBL339672 — IC50 = 0.32 nM 9.49
CHEMBL332909 — IC50 = 0.32 nM 9.49
CHEMBL436396 — IC50 = 0.34 nM 9.47
CHEMBL125280 — IC50 = 0.36 nM 9.44
CHEMBL444065 — IC50 = 0.4 nM 9.40
CHEMBL341369 — IC50 = 0.43 nM 9.37
CHEMBL339256 — IC50 = 0.43 nM 9.37
CHEMBL339605 — IC50 = 0.44 nM 9.36
CHEMBL331455 — IC50 = 0.45 nM 9.35
CHEMBL124771 — IC50 = 0.5 nM 9.30
CHEMBL339004 — IC50 = 0.55 nM 9.26
CHEMBL339722 — IC50 = 0.56 nM 9.25
CHEMBL339040 — IC50 = 0.64 nM 9.19
CHEMBL122273 — IC50 = 0.72 nM 9.14
CHEMBL339113 — IC50 = 0.74 nM 9.13
CHEMBL340632 — IC50 = 0.76 nM 9.12
CHEMBL121872 — IC50 = 0.84 nM 9.08
CHEMBL121907 — IC50 = 0.88 nM 9.06
CHEMBL338434 — IC50 = 0.9 nM 9.05
CHEMBL338433 — IC50 = 0.94 nM 9.03
CHEMBL340078 — IC50 = 0.96 nM 9.02
CHEMBL122917 — IC50 = 1.0 nM 9.00
CHEMBL331507 — IC50 = 1.0 nM 9.00
CHEMBL331450 — IC50 = 1.0 nM 9.00
CHEMBL125008 — IC50 = 1.1 nM 8.96
CHEMBL338137 — IC50 = 1.4 nM 8.85
CHEMBL340473 — IC50 = 1.5 nM 8.82
CHEMBL122158 — IC50 = 1.6 nM 8.80
CHEMBL122401 — IC50 = 1.6 nM 8.80
CHEMBL276674 — IC50 = 1.8 nM 8.74
CHEMBL122380 — IC50 = 1.9 nM 8.72
CHEMBL338342 — IC50 = 2.0 nM 8.70
CHEMBL421478 — IC50 = 2.2 nM 8.66
CHEMBL338889 — IC50 = 2.2 nM 8.66
CHEMBL338888 — IC50 = 3.3 nM 8.48
CHEMBL122157 — IC50 = 3.4 nM 8.47
CHEMBL338027 — IC50 = 3.5 nM 8.46
CHEMBL338687 — IC50 = 4.3 nM 8.37
CHEMBL333224 — IC50 = 4.6 nM 8.34
CHEMBL125760 — IC50 = 6.1 nM 8.21
CHEMBL124903 — IC50 = 8.8 nM 8.06
CHEMBL339806 — IC50 = 17.0 nM 7.77
CHEMBL273542 — IC50 = 24.0 nM 7.62
CHEMBL331632 — IC50 = 28.0 nM 7.55
CHEMBL191 LOSARTAN IC50 = 88.0 nM 7.06
CHEMBL332576 — IC50 < 0.3 nM -