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Assay Detail

CHEMBL889784

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

Binding
Displacement of Dexamethasone from human glucocorticoid receptor by fluorescence polarization assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and SAR study of novel dihydroquinoline-containing glucocorticoid receptor agonists.
Takahashi H, Bekkali Y, Capolino AJ, Gilmore T, Goldrick SE, Kaplita PV, Liu L, Nelson RM, Terenzio D, Wang J, Zuvela-Jelaska L, Proudfoot J, Nabozny G, Thomson D.
Bioorg Med Chem Lett (2007) 17 : 5091 -5095
PubMed 17681466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.63 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395506 1 7.47
CHEMBL541908 1 7.40
CHEMBL379024 1 7.08
CHEMBL537887 1 6.96
CHEMBL228610 1 6.94
CHEMBL396997 1 6.94
CHEMBL430004 1 6.73
CHEMBL206278 1 6.72
CHEMBL382785 1 6.71
CHEMBL242675 1 6.71
CHEMBL397018 1 6.68
CHEMBL228932 1 6.58
CHEMBL242872 1 6.56
CHEMBL388017 1 6.54
CHEMBL228611 1 6.45
CHEMBL203885 1 6.44
CHEMBL394343 1 6.40
CHEMBL395051 1 6.40
CHEMBL394345 1 6.39
CHEMBL228878 1 6.25
CHEMBL395535 1 6.15
CHEMBL394344 1 6.01
CHEMBL228767 1 5.97
CHEMBL228661 1 -
CHEMBL228663 1 -
CHEMBL395536 1 -
CHEMBL228715 1 -
CHEMBL228766 1 -
CHEMBL388170 1 -
CHEMBL202897 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395506 IC50 = 34.0 nM 7.47
CHEMBL541908 IC50 = 40.0 nM 7.40
CHEMBL379024 IC50 = 84.0 nM 7.08
CHEMBL537887 IC50 = 110.0 nM 6.96
CHEMBL228610 IC50 = 116.0 nM 6.94
CHEMBL396997 IC50 = 116.0 nM 6.94
CHEMBL430004 IC50 = 185.0 nM 6.73
CHEMBL206278 IC50 = 190.0 nM 6.72
CHEMBL382785 IC50 = 194.0 nM 6.71
CHEMBL242675 IC50 = 195.0 nM 6.71
CHEMBL397018 IC50 = 210.0 nM 6.68
CHEMBL228932 IC50 = 260.0 nM 6.58
CHEMBL242872 IC50 = 275.0 nM 6.56
CHEMBL388017 IC50 = 290.0 nM 6.54
CHEMBL228611 IC50 = 355.0 nM 6.45
CHEMBL203885 IC50 = 360.0 nM 6.44
CHEMBL394343 IC50 = 395.0 nM 6.40
CHEMBL395051 IC50 = 400.0 nM 6.40
CHEMBL394345 IC50 = 404.0 nM 6.39
CHEMBL228878 IC50 = 565.0 nM 6.25
CHEMBL395535 IC50 = 710.0 nM 6.15
CHEMBL394344 IC50 = 980.0 nM 6.01
CHEMBL228767 IC50 = 1060.0 nM 5.97
CHEMBL228661 IC50 > 2000.0 nM -
CHEMBL228663 IC50 > 2000.0 nM -
CHEMBL395536 IC50 > 2000.0 nM -
CHEMBL228715 IC50 > 2000.0 nM -
CHEMBL228766 IC50 > 2000.0 nM -
CHEMBL388170 IC50 > 2000.0 nM -
CHEMBL202897 IC50 > 2000.0 nM -