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

CHEMBL829188

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

Binding
Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type C2C12
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL3144)
Type SINGLE PROTEIN
Organism Mus musculus

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
EC50 8 7.56 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372684 1 8.52
CHEMBL131 PREDNISOLONE 4.0 1 8.47
CHEMBL310570 1 8.08
CHEMBL82546 1 7.77
CHEMBL364015 1 7.64
CHEMBL193404 1 7.47
CHEMBL362914 1 6.58
CHEMBL195972 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372684 EC50 = 3.0 nM 8.52
CHEMBL131 PREDNISOLONE EC50 = 3.4 nM 8.47
CHEMBL310570 EC50 = 8.3 nM 8.08
CHEMBL82546 EC50 = 17.0 nM 7.77
CHEMBL364015 EC50 = 23.0 nM 7.64
CHEMBL193404 EC50 = 34.0 nM 7.47
CHEMBL362914 EC50 = 260.0 nM 6.58
CHEMBL195972 EC50 = 1209.0 nM 5.92