Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL831159

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

Binding
Inhibition of human glucocorticoid receptor alpha by displacement of [3H]dexamethasone
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy.
Thompson CF, Quraishi N, Ali A, Tata JR, Hammond ML, Balkovec JM, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Miller DK, Yamin TT, Thompson CM, O'Neill EA, Zaller D, Forrest MJ, Carballo-Jane E, Luell S.
Bioorg Med Chem Lett (2005) 15 : 2163 -2167
PubMed 15808489 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.22 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310570 1 9.10
CHEMBL372684 1 8.82
CHEMBL313062 1 8.72
CHEMBL371376 1 8.54
CHEMBL82546 1 8.34
CHEMBL363179 1 8.29
CHEMBL79807 1 8.28
CHEMBL196347 1 8.15
CHEMBL193404 1 8.12
CHEMBL364015 1 8.04
CHEMBL194077 1 7.99
CHEMBL362914 1 7.87
CHEMBL131 PREDNISOLONE 4.0 1 7.86
CHEMBL365818 1 7.63
CHEMBL195972 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310570 IC50 = 0.8 nM 9.10
CHEMBL372684 IC50 = 1.5 nM 8.82
CHEMBL313062 IC50 = 1.9 nM 8.72
CHEMBL371376 IC50 = 2.9 nM 8.54
CHEMBL82546 IC50 = 4.6 nM 8.34
CHEMBL363179 IC50 = 5.1 nM 8.29
CHEMBL79807 IC50 = 5.3 nM 8.28
CHEMBL196347 IC50 = 7.1 nM 8.15
CHEMBL193404 IC50 = 7.6 nM 8.12
CHEMBL364015 IC50 = 9.1 nM 8.04
CHEMBL194077 IC50 = 10.2 nM 7.99
CHEMBL362914 IC50 = 13.6 nM 7.87
CHEMBL131 PREDNISOLONE IC50 = 13.8 nM 7.86
CHEMBL365818 IC50 = 23.2 nM 7.63
CHEMBL195972 IC50 = 29.1 nM 7.54