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Assay Detail

CHEMBL666796

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

Functional
Glucocorticoid-induced aromatase activity in human skin fibroblasts
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.
Coghlan MJ, Kym PR, Elmore SW, Wang AX, Luly JR, Wilcox D, Stashko M, Lin CW, Miner J, Tyree C, Nakane M, Jacobson P, Lane BC.
J Med Chem (2001) 44 : 2879 -2885
PubMed 11520196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.90 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131 PREDNISOLONE 4.0 1 7.39
CHEMBL99123 1 7.25
CHEMBL95644 1 6.98
CHEMBL327757 1 6.88
CHEMBL419158 1 6.86
CHEMBL97206 1 6.85
CHEMBL330638 1 6.84
CHEMBL99046 1 6.79
CHEMBL317578 1 6.67
CHEMBL100219 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131 PREDNISOLONE IC50 = 41.0 nM 7.39
CHEMBL99123 IC50 = 56.0 nM 7.25
CHEMBL95644 IC50 = 105.0 nM 6.98
CHEMBL327757 IC50 = 131.0 nM 6.88
CHEMBL419158 IC50 = 139.0 nM 6.86
CHEMBL97206 IC50 = 140.0 nM 6.85
CHEMBL330638 IC50 = 146.0 nM 6.84
CHEMBL99046 IC50 = 164.0 nM 6.79
CHEMBL317578 IC50 = 216.0 nM 6.67
CHEMBL100219 IC50 = 314.0 nM 6.50