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Assay Detail

CHEMBL828940

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

Binding
Inhibition of GR-mediated tyrosine amino transferase activity in human HepG2 cells
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
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
EC50 7 6.44 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131 PREDNISOLONE 4.0 1 7.62
CHEMBL310570 1 7.44
CHEMBL372684 1 6.45
CHEMBL313062 1 6.28
CHEMBL82546 1 6.00
CHEMBL193404 1 5.97
CHEMBL364015 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131 PREDNISOLONE EC50 = 24.0 nM 7.62
CHEMBL310570 EC50 = 36.0 nM 7.44
CHEMBL372684 EC50 = 356.0 nM 6.45
CHEMBL313062 EC50 = 521.0 nM 6.28
CHEMBL82546 EC50 = 1004.0 nM 6.00
CHEMBL193404 EC50 = 1068.0 nM 5.97
CHEMBL364015 EC50 = 4443.0 nM 5.35