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Assay Detail

CHEMBL897790

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Binding
Binding affinity to glucocorticoid receptor
22
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous 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 7.94 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL234988 2 8.37
CHEMBL393011 2 8.33
CHEMBL236947 2 8.29
CHEMBL235208 2 8.26
CHEMBL1276308 MIFEPRISTONE 4.0 1 8.16
CHEMBL394168 1 8.13
CHEMBL384467 DEXAMETHASONE 4.0 1 8.12
CHEMBL392319 2 8.12
CHEMBL235205 2 8.02
CHEMBL237973 2 8.01
CHEMBL391874 4 7.52
CHEMBL236320 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL234988 IC50 = 4.266 nM 8.37
CHEMBL393011 IC50 = 4.677 nM 8.33
CHEMBL393011 IC50 = 4.677 nM 8.33
CHEMBL234988 IC50 = 4.786 nM 8.32
CHEMBL236947 IC50 = 5.129 nM 8.29
CHEMBL235208 IC50 = 5.495 nM 8.26
CHEMBL236947 IC50 = 5.754 nM 8.24
CHEMBL235208 IC50 = 6.761 nM 8.17
CHEMBL1276308 MIFEPRISTONE IC50 = 6.918 nM 8.16
CHEMBL394168 IC50 = 7.413 nM 8.13
CHEMBL384467 DEXAMETHASONE IC50 = 7.586 nM 8.12
CHEMBL392319 IC50 = 7.586 nM 8.12
CHEMBL392319 IC50 = 9.333 nM 8.03
CHEMBL235205 IC50 = 9.55 nM 8.02
CHEMBL237973 IC50 = 9.772 nM 8.01
CHEMBL237973 IC50 = 19.95 nM 7.70
CHEMBL235205 IC50 = 20.89 nM 7.68
CHEMBL391874 IC50 = 30.2 nM 7.52
CHEMBL391874 IC50 = 34.67 nM 7.46
CHEMBL236320 IC50 = 40.74 nM 7.39
CHEMBL391874 IC50 = 51.29 nM 7.29
CHEMBL391874 IC50 = 158.49 nM 6.80