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Assay Detail

CHEMBL1805665

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

Binding
Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.
Yang BV, Weinstein DS, Doweyko LM, Gong H, Vaccaro W, Huynh T, Xiao HY, Doweyko AM, McKay L, Holloway DA, Somerville JE, Habte S, Cunningham M, McMahon M, Townsend R, Shuster D, Dodd JH, Nadler SG, Barrish JC.
J Med Chem (2010) 53 : 8241 -8251
PubMed 21073190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.89 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL384467 DEXAMETHASONE 4.0 1 8.38
CHEMBL1800984 1 7.22
CHEMBL1800982 1 7.17
CHEMBL131 PREDNISOLONE 4.0 1 7.08
CHEMBL1800985 1 7.07
CHEMBL1801006 1 6.94
CHEMBL1801008 1 6.92
CHEMBL1800981 1 6.92
CHEMBL1801009 1 6.67
CHEMBL1801012 1 6.43
CHEMBL1801004 1 6.42
CHEMBL1800983 1 6.25
CHEMBL1801013 1 6.06
CHEMBL1801011 1 -
CHEMBL1801010 1 -
CHEMBL1801007 1 -
CHEMBL1801005 1 -
CHEMBL1801003 1 -
CHEMBL1800980 1 -
CHEMBL1800979 1 -
CHEMBL1800986 1 -
CHEMBL1800987 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL384467 DEXAMETHASONE EC50 = 4.2 nM 8.38
CHEMBL1800984 EC50 = 60.1 nM 7.22
CHEMBL1800982 EC50 = 67.2 nM 7.17
CHEMBL131 PREDNISOLONE EC50 = 82.7 nM 7.08
CHEMBL1800985 EC50 = 85.7 nM 7.07
CHEMBL1801006 EC50 = 114.7 nM 6.94
CHEMBL1801008 EC50 = 119.0 nM 6.92
CHEMBL1800981 EC50 = 121.0 nM 6.92
CHEMBL1801009 EC50 = 216.4 nM 6.67
CHEMBL1801012 EC50 = 372.1 nM 6.43
CHEMBL1801004 EC50 = 380.2 nM 6.42
CHEMBL1800983 EC50 = 555.8 nM 6.25
CHEMBL1801013 EC50 = 863.4 nM 6.06
CHEMBL1801011 EC50 > 10000.0 nM -
CHEMBL1801010 EC50 > 10000.0 nM -
CHEMBL1801007 EC50 > 10000.0 nM -
CHEMBL1801005 EC50 > 10000.0 nM -
CHEMBL1801003 EC50 > 10000.0 nM -
CHEMBL1800980 EC50 > 10000.0 nM -
CHEMBL1800979 EC50 > 10000.0 nM -
CHEMBL1800986 EC50 > 10000.0 nM -
CHEMBL1800987 EC50 > 10000.0 nM -