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Assay Detail

CHEMBL1019340

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

Binding
Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assay
22
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.
Yang BV, Vaccaro W, Doweyko AM, Doweyko LM, Huynh T, Tortolani D, Nadler SG, McKay L, Somerville J, Holloway DA, Habte S, Weinstein DS, Barrish JC.
Bioorg Med Chem Lett (2009) 19 : 2139 -2143
PubMed 19321341 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.93 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473801 1 9.05
CHEMBL474189 2 9.00
CHEMBL384467 DEXAMETHASONE 4.0 1 8.96
CHEMBL514630 2 8.89
CHEMBL514646 1 8.89
CHEMBL131 PREDNISOLONE 4.0 1 8.82
CHEMBL475159 1 8.54
CHEMBL472801 1 8.41
CHEMBL474770 3 8.39
CHEMBL515738 1 8.27
CHEMBL472800 1 8.06
CHEMBL514455 1 7.65
CHEMBL474576 1 7.58
CHEMBL473802 1 7.42
CHEMBL474965 1 7.08
CHEMBL474381 1 7.03
CHEMBL514185 1 6.80
CHEMBL474771 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473801 Ki = 0.9 nM 9.05
CHEMBL474189 Ki = 1.0 nM 9.00
CHEMBL384467 DEXAMETHASONE Ki = 1.1 nM 8.96
CHEMBL514630 Ki = 1.3 nM 8.89
CHEMBL514646 Ki = 1.3 nM 8.89
CHEMBL131 PREDNISOLONE Ki = 1.5 nM 8.82
CHEMBL475159 Ki = 2.9 nM 8.54
CHEMBL472801 Ki = 3.9 nM 8.41
CHEMBL474770 Ki = 4.1 nM 8.39
CHEMBL515738 Ki = 5.4 nM 8.27
CHEMBL472800 Ki = 8.7 nM 8.06
CHEMBL474770 Ki = 12.7 nM 7.90
CHEMBL514455 Ki = 22.6 nM 7.65
CHEMBL474576 Ki = 26.2 nM 7.58
CHEMBL473802 Ki = 37.8 nM 7.42
CHEMBL514630 Ki = 49.7 nM 7.30
CHEMBL474189 Ki = 67.8 nM 7.17
CHEMBL474965 Ki = 82.5 nM 7.08
CHEMBL474381 Ki = 92.6 nM 7.03
CHEMBL514185 Ki = 157.7 nM 6.80
CHEMBL474770 Ki = 187.0 nM 6.73
CHEMBL474771 Ki = 303.0 nM 6.52