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Assay Detail

CHEMBL685254

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

Binding
Inhibition of human glucocorticoid receptor at 10e-12 to 10e-5 M
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glucocorticoid receptor (CHEMBL2034)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
Zhi L, Tegley CM, Pio B, Edwards JP, Motamedi M, Jones TK, Marschke KB, Mais DE, Risek B, Schrader WT.
J Med Chem (2003) 46 : 4104 -4112
PubMed 12954062 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.70 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 8.00
CHEMBL415524 1 7.11
CHEMBL335996 1 7.05
CHEMBL134277 1 7.00
CHEMBL336169 1 6.96
CHEMBL132363 1 6.73
CHEMBL130141 1 6.61
CHEMBL413309 1 6.60
CHEMBL337856 1 6.53
CHEMBL336353 1 6.50
CHEMBL336736 1 6.19
CHEMBL422444 1 6.07
CHEMBL134602 1 5.69
CHEMBL103 PROGESTERONE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 = 10.0 nM 8.00
CHEMBL415524 IC50 = 77.0 nM 7.11
CHEMBL335996 IC50 = 90.0 nM 7.05
CHEMBL134277 IC50 = 100.0 nM 7.00
CHEMBL336169 IC50 = 109.0 nM 6.96
CHEMBL132363 IC50 = 188.0 nM 6.73
CHEMBL130141 IC50 = 245.0 nM 6.61
CHEMBL413309 IC50 = 250.0 nM 6.60
CHEMBL337856 IC50 = 297.0 nM 6.53
CHEMBL336353 IC50 = 320.0 nM 6.50
CHEMBL336736 IC50 = 650.0 nM 6.19
CHEMBL422444 IC50 = 860.0 nM 6.07
CHEMBL134602 IC50 = 2050.0 nM 5.69
CHEMBL103 PROGESTERONE IC50 > 1000.0 nM -