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Assay Detail

CHEMBL647885

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Binding
In vitro inhibitory activity against angiotensin II type 1 receptor in rat adrenal membrane preparations.
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Angiotensin II receptor (AT-1) type-1 (CHEMBL2094250) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 50 9.63 10.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338101 — — 1 10.15
CHEMBL331450 — — 1 10.14
CHEMBL338342 — — 1 10.05
CHEMBL436396 — — 1 10.00
CHEMBL340473 — — 1 9.96
CHEMBL93907 — — 1 9.96
CHEMBL122401 — — 1 9.92
CHEMBL339004 — — 1 9.92
CHEMBL339672 — — 1 9.92
CHEMBL334300 — — 1 9.89
CHEMBL338433 — — 1 9.85
CHEMBL339040 — — 1 9.85
CHEMBL124771 — — 1 9.82
CHEMBL332909 — — 1 9.82
CHEMBL339256 — — 1 9.82
CHEMBL341369 — — 1 9.82
CHEMBL340078 — — 1 9.80
CHEMBL125008 — — 1 9.80
CHEMBL122158 — — 1 9.77
CHEMBL421478 — — 1 9.77
CHEMBL331455 — — 1 9.74
CHEMBL435811 — — 1 9.74
CHEMBL122273 — — 1 9.74
CHEMBL340632 — — 1 9.74
CHEMBL444065 — — 1 9.70
CHEMBL125231 — — 1 9.68
CHEMBL121872 — — 1 9.68
CHEMBL339605 — — 1 9.66
CHEMBL122380 — — 1 9.66
CHEMBL338434 — — 1 9.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338101 — IC50 = 0.071 nM 10.15
CHEMBL331450 — IC50 = 0.072 nM 10.14
CHEMBL338342 — IC50 = 0.089 nM 10.05
CHEMBL436396 — IC50 = 0.1 nM 10.00
CHEMBL340473 — IC50 = 0.11 nM 9.96
CHEMBL93907 — IC50 = 0.11 nM 9.96
CHEMBL122401 — IC50 = 0.12 nM 9.92
CHEMBL339004 — IC50 = 0.12 nM 9.92
CHEMBL339672 — IC50 = 0.12 nM 9.92
CHEMBL334300 — IC50 = 0.13 nM 9.89
CHEMBL338433 — IC50 = 0.14 nM 9.85
CHEMBL339040 — IC50 = 0.14 nM 9.85
CHEMBL332909 — IC50 = 0.15 nM 9.82
CHEMBL124771 — IC50 = 0.15 nM 9.82
CHEMBL339256 — IC50 = 0.15 nM 9.82
CHEMBL341369 — IC50 = 0.15 nM 9.82
CHEMBL340078 — IC50 = 0.16 nM 9.80
CHEMBL125008 — IC50 = 0.16 nM 9.80
CHEMBL122158 — IC50 = 0.17 nM 9.77
CHEMBL421478 — IC50 = 0.17 nM 9.77
CHEMBL331455 — IC50 = 0.18 nM 9.74
CHEMBL435811 — IC50 = 0.18 nM 9.74
CHEMBL122273 — IC50 = 0.18 nM 9.74
CHEMBL340632 — IC50 = 0.18 nM 9.74
CHEMBL444065 — IC50 = 0.2 nM 9.70
CHEMBL125231 — IC50 = 0.21 nM 9.68
CHEMBL121872 — IC50 = 0.21 nM 9.68
CHEMBL339605 — IC50 = 0.22 nM 9.66
CHEMBL122380 — IC50 = 0.22 nM 9.66
CHEMBL338434 — IC50 = 0.22 nM 9.66
CHEMBL125280 — IC50 = 0.22 nM 9.66
CHEMBL338027 — IC50 = 0.23 nM 9.64
CHEMBL339113 — IC50 = 0.24 nM 9.62
CHEMBL122917 — IC50 = 0.24 nM 9.62
CHEMBL121907 — IC50 = 0.25 nM 9.60
CHEMBL338137 — IC50 = 0.25 nM 9.60
CHEMBL339722 — IC50 = 0.27 nM 9.57
CHEMBL331507 — IC50 = 0.29 nM 9.54
CHEMBL276674 — IC50 = 0.3 nM 9.52
CHEMBL338889 — IC50 = 0.38 nM 9.42
CHEMBL338888 — IC50 = 0.43 nM 9.37
CHEMBL273542 — IC50 = 0.48 nM 9.32
CHEMBL333224 — IC50 = 0.49 nM 9.31
CHEMBL332576 — IC50 = 0.55 nM 9.26
CHEMBL338687 — IC50 = 0.69 nM 9.16
CHEMBL124903 — IC50 = 0.88 nM 9.06
CHEMBL122157 — IC50 = 0.88 nM 9.06
CHEMBL125760 — IC50 = 1.0 nM 9.00
CHEMBL331632 — IC50 = 1.2 nM 8.92
CHEMBL339806 — IC50 = 3.5 nM 8.46