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Assay Detail

CHEMBL831374

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

Binding
Inhibition of [3H]dexamethasone binding to rat glucocorticoid receptor
6
Total Activities
6
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

Antidiabetic activity of passive nonsteroidal glucocorticoid receptor modulators.
Link JT, Sorensen B, Patel J, Grynfarb M, Goos-Nilsson A, Wang J, Fung S, Wilcox D, Zinker B, Nguyen P, Hickman B, Schmidt JM, Swanson S, Tian Z, Reisch TJ, Rotert G, Du J, Lane B, von Geldern TW, Jacobson PB.
J Med Chem (2005) 48 : 5295 -5304
PubMed 16078847 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.93 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191423 1 9.70
CHEMBL185265 1 9.00
CHEMBL1276308 MIFEPRISTONE 4.0 1 8.85
CHEMBL190109 1 8.72
CHEMBL190225 1 8.68
CHEMBL363151 1 8.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191423 IC50 = 0.2 nM 9.70
CHEMBL185265 IC50 = 1.0 nM 9.00
CHEMBL1276308 MIFEPRISTONE IC50 = 1.4 nM 8.85
CHEMBL190109 IC50 = 1.9 nM 8.72
CHEMBL190225 IC50 = 2.1 nM 8.68
CHEMBL363151 IC50 = 2.4 nM 8.62