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Assay Detail

CHEMBL685138

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

Binding
Competitive displacement of [3H]dexamethasone from glucocorticoid receptor of rat liver cytosol
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL3368)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of antiinflammatory activities of a series of corticosteroid 17 alpha-esters containing a functional group.
Ueno H, Maruyama A, Miyake M, Nakao E, Nakao K, Umezu K, Nitta I.
J Med Chem (1991) 34 : 2468 -2473
PubMed 1875343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.16 8.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE 4.0 1 8.50
CHEMBL315931 1 8.29
CHEMBL1200384 BETAMETHASONE DIPROPIONATE 4.0 1 8.28
CHEMBL81387 1 8.01
CHEMBL83845 1 7.97
CHEMBL311802 1 7.92
CHEMBL311457 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159650 CLOBETASOL PROPIONATE IC50 = 3.17 nM 8.50
CHEMBL315931 IC50 = 5.18 nM 8.29
CHEMBL1200384 BETAMETHASONE DIPROPIONATE IC50 = 5.25 nM 8.28
CHEMBL81387 IC50 = 9.68 nM 8.01
CHEMBL83845 IC50 = 10.8 nM 7.97
CHEMBL311802 IC50 = 12.1 nM 7.92
CHEMBL311457 IC50 > 150.0 nM -