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Assay Detail

CHEMBL897792

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Functional
Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay
22
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A549
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Clackers M, Coe DM, Demaine DA, Hardy GW, Humphreys D, Inglis GG, Johnston MJ, Jones HT, House D, Loiseau R, Minick DJ, Skone PA, Uings I, McLay IM, Macdonald SJ.
Bioorg Med Chem Lett (2007) 17 : 4737 -4745
PubMed 17616395 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 7.78 8.92
Log EC50 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235208 2 8.92
CHEMBL384467 DEXAMETHASONE 4.0 1 8.27
CHEMBL394168 1 8.25
CHEMBL237973 2 8.11
CHEMBL393011 2 7.91
CHEMBL234988 2 7.82
CHEMBL236947 2 7.74
CHEMBL235205 2 7.02
CHEMBL236320 1 -
CHEMBL391874 4 -
CHEMBL392319 2 -
CHEMBL1276308 MIFEPRISTONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235208 EC50 = 1.202 nM 8.92
CHEMBL384467 DEXAMETHASONE EC50 = 5.37 nM 8.27
CHEMBL394168 EC50 = 5.623 nM 8.25
CHEMBL237973 EC50 = 7.762 nM 8.11
CHEMBL237973 EC50 = 10.72 nM 7.97
CHEMBL393011 EC50 = 12.3 nM 7.91
CHEMBL393011 EC50 = 14.45 nM 7.84
CHEMBL234988 EC50 = 15.14 nM 7.82
CHEMBL235208 EC50 = 15.85 nM 7.80
CHEMBL234988 EC50 = 17.38 nM 7.76
CHEMBL236947 EC50 = 18.2 nM 7.74
CHEMBL235205 EC50 = 95.5 nM 7.02
CHEMBL235205 EC50 = 151.36 nM 6.82
CHEMBL236947 EC50 = 181.97 nM 6.74
CHEMBL392319 EC50 < 1000.0 nM -
CHEMBL392319 EC50 < 1000.0 nM -
CHEMBL1276308 MIFEPRISTONE EC50 < 1000.0 nM -
CHEMBL391874 Log EC50 - -
CHEMBL391874 Log EC50 - -
CHEMBL391874 Log EC50 - -
CHEMBL391874 EC50 < 1000.0 nM -
CHEMBL236320 Log EC50 - -