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Assay Detail

CHEMBL897791

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Functional
Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay
22
Total Activities
12
Compounds Tested
1
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
IC50 22 8.17 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235208 2 9.34
CHEMBL384467 DEXAMETHASONE 4.0 1 9.00
CHEMBL394168 1 8.78
CHEMBL237973 2 8.52
CHEMBL234988 2 8.43
CHEMBL393011 2 8.35
CHEMBL236947 2 8.23
CHEMBL235205 2 8.07
CHEMBL392319 2 7.31
CHEMBL391874 4 -
CHEMBL236320 1 -
CHEMBL1276308 MIFEPRISTONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235208 IC50 = 0.4571 nM 9.34
CHEMBL384467 DEXAMETHASONE IC50 = 1.0 nM 9.00
CHEMBL394168 IC50 = 1.66 nM 8.78
CHEMBL237973 IC50 = 3.02 nM 8.52
CHEMBL237973 IC50 = 3.631 nM 8.44
CHEMBL234988 IC50 = 3.715 nM 8.43
CHEMBL393011 IC50 = 4.467 nM 8.35
CHEMBL236947 IC50 = 5.888 nM 8.23
CHEMBL393011 IC50 = 6.457 nM 8.19
CHEMBL235205 IC50 = 8.511 nM 8.07
CHEMBL234988 IC50 = 13.18 nM 7.88
CHEMBL236947 IC50 = 16.98 nM 7.77
CHEMBL235208 IC50 = 17.78 nM 7.75
CHEMBL235205 IC50 = 30.2 nM 7.52
CHEMBL392319 IC50 = 48.98 nM 7.31
CHEMBL392319 IC50 = 83.18 nM 7.08
CHEMBL391874 IC50 < 1000.0 nM -
CHEMBL391874 IC50 < 1000.0 nM -
CHEMBL391874 IC50 < 1000.0 nM -
CHEMBL391874 IC50 < 1000.0 nM -
CHEMBL236320 IC50 < 1000.0 nM -
CHEMBL1276308 MIFEPRISTONE IC50 < 1000.0 nM -