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Assay Detail

CHEMBL1805661

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

Binding
Displacement of GS-red from GRapha by fluorescence polarization assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dimethyl-diphenyl-propanamide derivatives as nonsteroidal dissociated glucocorticoid receptor agonists.
Yang BV, Weinstein DS, Doweyko LM, Gong H, Vaccaro W, Huynh T, Xiao HY, Doweyko AM, McKay L, Holloway DA, Somerville JE, Habte S, Cunningham M, McMahon M, Townsend R, Shuster D, Dodd JH, Nadler SG, Barrish JC.
J Med Chem (2010) 53 : 8241 -8251
PubMed 21073190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 8.68 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800984 1 9.52
CHEMBL1800982 1 9.40
CHEMBL1801006 1 9.40
CHEMBL1801009 1 9.22
CHEMBL1800981 1 9.15
CHEMBL1801008 1 9.15
CHEMBL1800985 1 9.10
CHEMBL1801005 1 9.05
CHEMBL384467 DEXAMETHASONE 4.0 1 8.96
CHEMBL1801012 1 8.92
CHEMBL1801004 1 8.92
CHEMBL131 PREDNISOLONE 4.0 1 8.82
CHEMBL1800983 1 8.66
CHEMBL1801013 1 8.60
CHEMBL1800979 1 8.54
CHEMBL1801007 1 8.34
CHEMBL1800980 1 8.24
CHEMBL1800987 1 8.22
CHEMBL1801003 1 8.14
CHEMBL1801011 1 7.73
CHEMBL1801010 1 7.68
CHEMBL1800986 1 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800984 Ki = 0.3 nM 9.52
CHEMBL1800982 Ki = 0.4 nM 9.40
CHEMBL1801006 Ki = 0.4 nM 9.40
CHEMBL1801009 Ki = 0.6 nM 9.22
CHEMBL1800981 Ki = 0.7 nM 9.15
CHEMBL1801008 Ki = 0.7 nM 9.15
CHEMBL1800985 Ki = 0.8 nM 9.10
CHEMBL1801005 Ki = 0.9 nM 9.05
CHEMBL384467 DEXAMETHASONE Ki = 1.1 nM 8.96
CHEMBL1801012 Ki = 1.2 nM 8.92
CHEMBL1801004 Ki = 1.2 nM 8.92
CHEMBL131 PREDNISOLONE Ki = 1.5 nM 8.82
CHEMBL1800983 Ki = 2.2 nM 8.66
CHEMBL1801013 Ki = 2.5 nM 8.60
CHEMBL1800979 Ki = 2.9 nM 8.54
CHEMBL1801007 Ki = 4.6 nM 8.34
CHEMBL1800980 Ki = 5.7 nM 8.24
CHEMBL1800987 Ki = 6.0 nM 8.22
CHEMBL1801003 Ki = 7.3 nM 8.14
CHEMBL1801011 Ki = 18.7 nM 7.73
CHEMBL1801010 Ki = 20.7 nM 7.68
CHEMBL1800986 Ki = 58.7 nM 7.23