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Assay Detail

CHEMBL648578

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

Binding
In vitro inhibitory activity against Angiotensin II receptor type 2 in human adrenal membrane preparations.
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL4607)
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 47 8.49 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122273 1 9.19
CHEMBL338687 1 8.96
CHEMBL436396 1 8.85
CHEMBL122380 1 8.82
CHEMBL125760 1 8.82
CHEMBL122157 1 8.77
CHEMBL331450 1 8.77
CHEMBL435811 1 8.74
CHEMBL338888 1 8.70
CHEMBL125280 1 8.70
CHEMBL122401 1 8.70
CHEMBL333224 1 8.68
CHEMBL338433 1 8.66
CHEMBL341369 1 8.66
CHEMBL124771 1 8.64
CHEMBL339722 1 8.60
CHEMBL121872 1 8.60
CHEMBL121907 1 8.59
CHEMBL331507 1 8.59
CHEMBL331455 1 8.57
CHEMBL339113 1 8.54
CHEMBL340632 1 8.51
CHEMBL339672 1 8.51
CHEMBL339040 1 8.47
CHEMBL338027 1 8.47
CHEMBL339256 1 8.46
CHEMBL338889 1 8.44
CHEMBL338342 1 8.44
CHEMBL339605 1 8.43
CHEMBL339806 1 8.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122273 IC50 = 0.64 nM 9.19
CHEMBL338687 IC50 = 1.1 nM 8.96
CHEMBL436396 IC50 = 1.4 nM 8.85
CHEMBL122380 IC50 = 1.5 nM 8.82
CHEMBL125760 IC50 = 1.5 nM 8.82
CHEMBL122157 IC50 = 1.7 nM 8.77
CHEMBL331450 IC50 = 1.7 nM 8.77
CHEMBL435811 IC50 = 1.8 nM 8.74
CHEMBL338888 IC50 = 2.0 nM 8.70
CHEMBL125280 IC50 = 2.0 nM 8.70
CHEMBL122401 IC50 = 2.0 nM 8.70
CHEMBL333224 IC50 = 2.1 nM 8.68
CHEMBL341369 IC50 = 2.2 nM 8.66
CHEMBL338433 IC50 = 2.2 nM 8.66
CHEMBL124771 IC50 = 2.3 nM 8.64
CHEMBL339722 IC50 = 2.5 nM 8.60
CHEMBL121872 IC50 = 2.5 nM 8.60
CHEMBL121907 IC50 = 2.6 nM 8.59
CHEMBL331507 IC50 = 2.6 nM 8.59
CHEMBL331455 IC50 = 2.7 nM 8.57
CHEMBL339113 IC50 = 2.9 nM 8.54
CHEMBL340632 IC50 = 3.1 nM 8.51
CHEMBL339672 IC50 = 3.1 nM 8.51
CHEMBL339040 IC50 = 3.4 nM 8.47
CHEMBL338027 IC50 = 3.4 nM 8.47
CHEMBL339256 IC50 = 3.5 nM 8.46
CHEMBL338889 IC50 = 3.6 nM 8.44
CHEMBL338342 IC50 = 3.6 nM 8.44
CHEMBL339605 IC50 = 3.7 nM 8.43
CHEMBL339806 IC50 = 3.7 nM 8.43
CHEMBL339004 IC50 = 3.7 nM 8.43
CHEMBL338434 IC50 = 3.8 nM 8.42
CHEMBL444065 IC50 = 4.1 nM 8.39
CHEMBL273542 IC50 = 4.1 nM 8.39
CHEMBL122917 IC50 = 4.3 nM 8.37
CHEMBL332909 IC50 = 4.3 nM 8.37
CHEMBL332576 IC50 = 4.6 nM 8.34
CHEMBL340078 IC50 = 5.1 nM 8.29
CHEMBL122158 IC50 = 5.3 nM 8.28
CHEMBL334300 IC50 = 5.8 nM 8.24
CHEMBL125008 IC50 = 6.1 nM 8.21
CHEMBL338137 IC50 = 6.3 nM 8.20
CHEMBL421478 IC50 = 7.5 nM 8.12
CHEMBL124903 IC50 = 8.2 nM 8.09
CHEMBL331632 IC50 = 10.0 nM 8.00
CHEMBL276674 IC50 = 18.0 nM 7.75
CHEMBL340473 IC50 = 20.0 nM 7.70