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Assay Detail

CHEMBL647746

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

Binding
Inhibition of human androgen receptor at 10e-12 to 10e-5 M
11
Total Activities
11
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

Androgen receptor (CHEMBL1871)
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 11 6.64 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE 4.0 1 8.21
CHEMBL103 PROGESTERONE 4.0 1 7.43
CHEMBL132363 1 6.69
CHEMBL134277 1 6.67
CHEMBL336169 1 6.59
CHEMBL134602 1 6.19
CHEMBL336736 1 6.09
CHEMBL413309 1 6.05
CHEMBL336353 1 5.82
CHEMBL335996 1 -
CHEMBL130141 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL717 MEDROXYPROGESTERONE ACETATE IC50 = 6.1 nM 8.21
CHEMBL103 PROGESTERONE IC50 = 37.0 nM 7.43
CHEMBL132363 IC50 = 203.0 nM 6.69
CHEMBL134277 IC50 = 215.0 nM 6.67
CHEMBL336169 IC50 = 258.0 nM 6.59
CHEMBL134602 IC50 = 640.0 nM 6.19
CHEMBL336736 IC50 = 820.0 nM 6.09
CHEMBL413309 IC50 = 900.0 nM 6.05
CHEMBL336353 IC50 = 1500.0 nM 5.82
CHEMBL335996 IC50 = - nM -
CHEMBL130141 IC50 = - nM -