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Assay Detail

CHEMBL650165

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Binding
Binding affinity for rat brain Angiotensin II receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Angiotensin II receptor (CHEMBL2094112)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype.
Blankley CJ, Hodges JC, Klutchko SR, Himmelsbach RJ, Chucholowski A, Connolly CJ, Neergaard SJ, Van Nieuwenhze MS, Sebastian A, Quin J.
J Med Chem (1991) 34 : 3248 -3260
PubMed 1956044 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.71 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404594 1 10.00
CHEMBL408403 ANGIOTENSIN II 4.0 1 8.40
CHEMBL312754 1 8.29
CHEMBL320336 1 6.89
CHEMBL109921 1 6.77
CHEMBL321820 1 6.68
CHEMBL432794 1 6.40
CHEMBL112970 1 6.10
CHEMBL112874 1 5.80
CHEMBL111330 1 5.42
CHEMBL324414 1 5.09
CHEMBL109616 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404594 IC50 = 0.1 nM 10.00
CHEMBL408403 ANGIOTENSIN II IC50 = 4.0 nM 8.40
CHEMBL312754 IC50 = 5.1 nM 8.29
CHEMBL320336 IC50 = 130.0 nM 6.89
CHEMBL109921 IC50 = 170.0 nM 6.77
CHEMBL321820 IC50 = 210.0 nM 6.68
CHEMBL432794 IC50 = 400.0 nM 6.40
CHEMBL112970 IC50 = 800.0 nM 6.10
CHEMBL112874 IC50 = 1600.0 nM 5.80
CHEMBL111330 IC50 = 3800.0 nM 5.42
CHEMBL324414 IC50 = 8200.0 nM 5.09
CHEMBL109616 IC50 = 19000.0 nM 4.72