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Assay Detail

CHEMBL887361

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

Functional
Antagonist activity at human androgen receptor expressed in CV1 cells
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CV-1
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Androgen receptor (CHEMBL1871)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones.
van Oeveren A, Pio BA, Tegley CM, Higuchi RI, Wu M, Jones TK, Marschke KB, Negro-Vilar A, Zhi L.
Bioorg Med Chem Lett (2007) 17 : 1523 -1526
PubMed 17257838 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 7.13 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3706899 1 7.85
CHEMBL3706874 1 7.85
CHEMBL3706908 1 7.77
CHEMBL3706907 1 7.75
CHEMBL3706898 1 7.72
CHEMBL3706888 1 7.68
CHEMBL3706910 1 7.66
CHEMBL3706897 1 7.64
CHEMBL385509 1 7.58
CHEMBL350877 1 7.57
CHEMBL3706911 1 7.57
CHEMBL3706876 1 7.55
CHEMBL3706877 1 7.52
CHEMBL3706875 1 7.50
CHEMBL3706878 1 7.46
CHEMBL3706894 1 7.38
CHEMBL3706909 1 7.38
CHEMBL3706885 1 7.37
CHEMBL3706904 1 7.30
CHEMBL3706880 1 7.25
CHEMBL3706889 1 7.24
CHEMBL3706905 1 7.20
CHEMBL3706879 1 7.17
CHEMBL3706881 1 7.13
CHEMBL3706896 1 7.12
CHEMBL3706882 1 7.01
CHEMBL3706906 1 6.96
CHEMBL3706884 1 6.91
CHEMBL3706886 1 6.83
CHEMBL409 BICALUTAMIDE 4.0 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3706899 IC50 = 14.0 nM 7.85
CHEMBL3706874 IC50 = 14.0 nM 7.85
CHEMBL3706908 IC50 = 17.0 nM 7.77
CHEMBL3706907 IC50 = 18.0 nM 7.75
CHEMBL3706898 IC50 = 19.0 nM 7.72
CHEMBL3706888 IC50 = 21.0 nM 7.68
CHEMBL3706910 IC50 = 22.0 nM 7.66
CHEMBL3706897 IC50 = 23.0 nM 7.64
CHEMBL385509 IC50 = 26.0 nM 7.58
CHEMBL350877 IC50 = 27.0 nM 7.57
CHEMBL3706911 IC50 = 27.0 nM 7.57
CHEMBL3706876 IC50 = 28.0 nM 7.55
CHEMBL3706877 IC50 = 30.0 nM 7.52
CHEMBL3706875 IC50 = 32.0 nM 7.50
CHEMBL3706878 IC50 = 35.0 nM 7.46
CHEMBL3706894 IC50 = 42.0 nM 7.38
CHEMBL3706909 IC50 = 42.0 nM 7.38
CHEMBL3706885 IC50 = 43.0 nM 7.37
CHEMBL3706904 IC50 = 50.0 nM 7.30
CHEMBL3706880 IC50 = 56.0 nM 7.25
CHEMBL3706889 IC50 = 58.0 nM 7.24
CHEMBL3706905 IC50 = 63.0 nM 7.20
CHEMBL3706879 IC50 = 67.0 nM 7.17
CHEMBL3706881 IC50 = 74.0 nM 7.13
CHEMBL3706896 IC50 = 76.0 nM 7.12
CHEMBL3706882 IC50 = 98.0 nM 7.01
CHEMBL3706906 IC50 = 111.0 nM 6.96
CHEMBL3706884 IC50 = 122.0 nM 6.91
CHEMBL3706886 IC50 = 149.0 nM 6.83
CHEMBL409 BICALUTAMIDE IC50 = 162.0 nM 6.79
CHEMBL3706883 IC50 = 209.0 nM 6.68
CHEMBL3706903 IC50 = 216.0 nM 6.67
CHEMBL3706891 IC50 = 294.0 nM 6.53
CHEMBL3706901 IC50 = 301.0 nM 6.52
CHEMBL3706902 IC50 = 504.0 nM 6.30
CHEMBL3706887 IC50 = 507.0 nM 6.29
CHEMBL3706895 IC50 = 549.0 nM 6.26
CHEMBL3706893 IC50 = 591.0 nM 6.23
CHEMBL3706900 IC50 = 674.0 nM 6.17
CHEMBL3706892 IC50 = 1160.0 nM 5.94