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Assay Detail

CHEMBL828024

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Binding
Inhibition against U2OS cells expressing rat Glucocorticoid receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type U2OS
Confidence 9 — Direct single protein target
Curated By Expert

Target

Glucocorticoid receptor (CHEMBL3368)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
Shah N, Scanlan TS.
Bioorg Med Chem Lett (2004) 14 : 5199 -5203
PubMed 15380227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.35 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL186683 1 9.15
CHEMBL433586 1 8.85
CHEMBL363760 1 8.74
CHEMBL366093 1 8.64
CHEMBL186948 1 8.62
CHEMBL186954 1 8.60
CHEMBL183475 1 8.31
CHEMBL184578 1 8.28
CHEMBL362392 1 8.26
CHEMBL186930 1 8.18
CHEMBL362556 1 8.15
CHEMBL181601 1 8.10
CHEMBL186805 1 8.07
CHEMBL184109 1 8.04
CHEMBL360248 1 7.85
CHEMBL182827 1 7.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL186683 IC50 = 0.7 nM 9.15
CHEMBL433586 IC50 = 1.4 nM 8.85
CHEMBL363760 IC50 = 1.8 nM 8.74
CHEMBL366093 IC50 = 2.3 nM 8.64
CHEMBL186948 IC50 = 2.4 nM 8.62
CHEMBL186954 IC50 = 2.5 nM 8.60
CHEMBL183475 IC50 = 4.9 nM 8.31
CHEMBL184578 IC50 = 5.2 nM 8.28
CHEMBL362392 IC50 = 5.5 nM 8.26
CHEMBL186930 IC50 = 6.6 nM 8.18
CHEMBL362556 IC50 = 7.0 nM 8.15
CHEMBL181601 IC50 = 7.9 nM 8.10
CHEMBL186805 IC50 = 8.6 nM 8.07
CHEMBL184109 IC50 = 9.2 nM 8.04
CHEMBL360248 IC50 = 14.0 nM 7.85
CHEMBL182827 IC50 = 15.5 nM 7.81