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Assay Detail

CHEMBL643587

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Binding
In vitro inhibitory activity against Angiotensin II receptor, type 2 in rat midbrain membrane preparations.
ChEMBL ↗
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Midbrain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Type-2 angiotensin II receptor (CHEMBL257) ↗
Type SINGLE PROTEIN
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 54 9.29 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338687 — — 1 10.00
CHEMBL338027 — — 1 9.92
CHEMBL436396 — — 1 9.85
CHEMBL339256 — — 1 9.82
CHEMBL341369 — — 1 9.80
CHEMBL340632 — — 1 9.74
CHEMBL331450 — — 1 9.72
CHEMBL122158 — — 1 9.70
CHEMBL339722 — — 1 9.70
CHEMBL122917 — — 1 9.68
CHEMBL122380 — — 1 9.68
CHEMBL339672 — — 1 9.68
CHEMBL338434 — — 1 9.66
CHEMBL338342 — — 1 9.66
CHEMBL338433 — — 1 9.64
CHEMBL339605 — — 1 9.64
CHEMBL323506 — — 1 9.62
CHEMBL122273 — — 1 9.60
CHEMBL339004 — — 1 9.60
CHEMBL339040 — — 1 9.57
CHEMBL338888 — — 1 9.55
CHEMBL331455 — — 1 9.54
CHEMBL339113 — — 1 9.54
CHEMBL331632 — — 1 9.54
CHEMBL121907 — — 1 9.54
CHEMBL339806 — — 1 9.54
CHEMBL125280 — — 1 9.52
CHEMBL124903 — — 1 9.52
CHEMBL125760 — — 1 9.49
CHEMBL122401 — — 1 9.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338687 — IC50 = 0.1 nM 10.00
CHEMBL338027 — IC50 = 0.12 nM 9.92
CHEMBL436396 — IC50 = 0.14 nM 9.85
CHEMBL339256 — IC50 = 0.15 nM 9.82
CHEMBL341369 — IC50 = 0.16 nM 9.80
CHEMBL340632 — IC50 = 0.18 nM 9.74
CHEMBL331450 — IC50 = 0.19 nM 9.72
CHEMBL122158 — IC50 = 0.2 nM 9.70
CHEMBL339722 — IC50 = 0.2 nM 9.70
CHEMBL339672 — IC50 = 0.21 nM 9.68
CHEMBL122380 — IC50 = 0.21 nM 9.68
CHEMBL122917 — IC50 = 0.21 nM 9.68
CHEMBL338434 — IC50 = 0.22 nM 9.66
CHEMBL338342 — IC50 = 0.22 nM 9.66
CHEMBL339605 — IC50 = 0.23 nM 9.64
CHEMBL338433 — IC50 = 0.23 nM 9.64
CHEMBL323506 — IC50 = 0.24 nM 9.62
CHEMBL122273 — IC50 = 0.25 nM 9.60
CHEMBL339004 — IC50 = 0.25 nM 9.60
CHEMBL339040 — IC50 = 0.27 nM 9.57
CHEMBL338888 — IC50 = 0.28 nM 9.55
CHEMBL339806 — IC50 = 0.29 nM 9.54
CHEMBL121907 — IC50 = 0.29 nM 9.54
CHEMBL339113 — IC50 = 0.29 nM 9.54
CHEMBL331455 — IC50 = 0.29 nM 9.54
CHEMBL331632 — IC50 = 0.29 nM 9.54
CHEMBL125280 — IC50 = 0.3 nM 9.52
CHEMBL124903 — IC50 = 0.3 nM 9.52
CHEMBL125760 — IC50 = 0.32 nM 9.49
CHEMBL122401 — IC50 = 0.36 nM 9.44
CHEMBL340078 — IC50 = 0.37 nM 9.43
CHEMBL124771 — IC50 = 0.39 nM 9.41
CHEMBL435811 — IC50 = 0.39 nM 9.41
CHEMBL331507 — IC50 = 0.44 nM 9.36
CHEMBL122157 — IC50 = 0.48 nM 9.32
CHEMBL444065 — IC50 = 0.48 nM 9.32
CHEMBL125008 — IC50 = 0.54 nM 9.27
CHEMBL332909 — IC50 = 0.56 nM 9.25
CHEMBL332576 — IC50 = 0.58 nM 9.24
CHEMBL338137 — IC50 = 0.57 nM 9.24
CHEMBL302102 — IC50 = 0.7 nM 9.15
CHEMBL421478 — IC50 = 0.8 nM 9.10
CHEMBL338889 — IC50 = 0.81 nM 9.09
CHEMBL340473 — IC50 = 0.89 nM 9.05
CHEMBL273542 — IC50 = 0.93 nM 9.03
CHEMBL276674 — IC50 = 1.0 nM 9.00
CHEMBL121872 — IC50 = 1.1 nM 8.96
CHEMBL333224 — IC50 = 1.3 nM 8.89
CHEMBL125231 — IC50 = 1.4 nM 8.85
CHEMBL334300 — IC50 = 1.6 nM 8.80