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Assay Detail

CHEMBL1002258

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

Binding
Inhibition of human glucocorticoid receptor
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of betamethasone 17alpha-carbamates as dissociated glucocorticoid receptor modulators in the rat.
Ali A, Balkovec JM, Greenlee M, Hammond ML, Rouen G, Taylor G, Einstein M, Ge L, Harris G, Kelly TM, Mazur P, Pandit S, Santoro J, Sitlani A, Wang C, Williamson J, Forrest MJ, Carballo-Jane E, Luell S, Lowitz K, Visco D.
Bioorg Med Chem (2008) 16 : 7535 -7542
PubMed 18691892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.17 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL526106 1 9.30
CHEMBL500897 1 8.89
CHEMBL499630 1 8.68
CHEMBL497472 1 8.62
CHEMBL499629 1 8.55
CHEMBL503848 1 8.46
CHEMBL500938 1 8.44
CHEMBL525442 1 8.42
CHEMBL500678 1 8.29
CHEMBL509182 1 8.28
CHEMBL501745 1 8.24
CHEMBL503041 1 8.24
CHEMBL501474 1 7.91
CHEMBL498651 1 7.76
CHEMBL525923 1 7.67
CHEMBL525273 1 7.54
CHEMBL506241 1 7.26
CHEMBL526566 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL526106 IC50 = 0.5 nM 9.30
CHEMBL500897 IC50 = 1.3 nM 8.89
CHEMBL499630 IC50 = 2.1 nM 8.68
CHEMBL497472 IC50 = 2.4 nM 8.62
CHEMBL499629 IC50 = 2.8 nM 8.55
CHEMBL503848 IC50 = 3.5 nM 8.46
CHEMBL500938 IC50 = 3.6 nM 8.44
CHEMBL525442 IC50 = 3.8 nM 8.42
CHEMBL500678 IC50 = 5.1 nM 8.29
CHEMBL509182 IC50 = 5.2 nM 8.28
CHEMBL501745 IC50 = 5.7 nM 8.24
CHEMBL503041 IC50 = 5.8 nM 8.24
CHEMBL501474 IC50 = 12.3 nM 7.91
CHEMBL498651 IC50 = 17.4 nM 7.76
CHEMBL525923 IC50 = 21.5 nM 7.67
CHEMBL525273 IC50 = 28.6 nM 7.54
CHEMBL506241 IC50 = 55.1 nM 7.26
CHEMBL526566 IC50 = 352.0 nM 6.45