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Assay Detail

CHEMBL5224630

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

ADMET
Inhibition of CYP1A2 (unknown origin)
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 1A2 (CHEMBL3356)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer.
Padmakar Darne C, Velaparthi U, Saulnier M, Frennesson D, Liu P, Huang A, Tokarski J, Fura A, Spires T, Newitt J, Spires VM, Obermeier MT, Elzinga PA, Gottardis MM, Jayaraman L, Vite GD, Balog A.
Bioorg Med Chem Lett (2022) 75 : 128951 -128951
PubMed 36031020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 5.98 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3696099 1 7.55
CHEMBL5284599 1 7.47
CHEMBL3902750 1 7.24
CHEMBL5286021 1 6.87
CHEMBL5290740 1 6.85
CHEMBL5280658 1 6.75
CHEMBL5267526 1 6.67
CHEMBL5285321 1 6.60
CHEMBL5265915 1 6.55
CHEMBL3956116 1 6.50
CHEMBL5284207 1 6.49
CHEMBL5286511 1 6.42
CHEMBL5266728 1 6.25
CHEMBL5267699 1 6.21
CHEMBL5287403 1 6.18
CHEMBL5289188 1 6.18
CHEMBL5286288 1 6.14
CHEMBL5290743 1 5.83
CHEMBL5284019 1 5.67
CHEMBL5287872 1 5.63
CHEMBL5278006 1 5.56
CHEMBL5275088 1 5.33
CHEMBL5269068 1 5.33
CHEMBL5278719 1 5.29
CHEMBL5274940 1 5.28
CHEMBL5276101 1 5.28
CHEMBL5284859 1 5.06
CHEMBL5275896 1 4.96
CHEMBL5267919 1 4.95
CHEMBL5277196 1 4.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3696099 IC50 = 28.0 nM 7.55
CHEMBL5284599 IC50 = 34.0 nM 7.47
CHEMBL3902750 IC50 = 58.0 nM 7.24
CHEMBL5286021 IC50 = 134.0 nM 6.87
CHEMBL5290740 IC50 = 140.0 nM 6.85
CHEMBL5280658 IC50 = 180.0 nM 6.75
CHEMBL5267526 IC50 = 216.0 nM 6.67
CHEMBL5285321 IC50 = 250.0 nM 6.60
CHEMBL5265915 IC50 = 281.0 nM 6.55
CHEMBL3956116 IC50 = 318.0 nM 6.50
CHEMBL5284207 IC50 = 321.0 nM 6.49
CHEMBL5286511 IC50 = 384.0 nM 6.42
CHEMBL5266728 IC50 = 560.0 nM 6.25
CHEMBL5267699 IC50 = 617.0 nM 6.21
CHEMBL5289188 IC50 = 658.0 nM 6.18
CHEMBL5287403 IC50 = 662.0 nM 6.18
CHEMBL5286288 IC50 = 717.0 nM 6.14
CHEMBL5290743 IC50 = 1480.0 nM 5.83
CHEMBL5284019 IC50 = 2142.0 nM 5.67
CHEMBL5287872 IC50 = 2330.0 nM 5.63
CHEMBL5278006 IC50 = 2741.0 nM 5.56
CHEMBL5269068 IC50 = 4710.0 nM 5.33
CHEMBL5275088 IC50 = 4736.0 nM 5.33
CHEMBL5278719 IC50 = 5144.0 nM 5.29
CHEMBL5274940 IC50 = 5200.0 nM 5.28
CHEMBL5276101 IC50 = 5283.0 nM 5.28
CHEMBL5284859 IC50 = 8700.0 nM 5.06
CHEMBL5275896 IC50 = 10870.0 nM 4.96
CHEMBL5267919 IC50 = 11230.0 nM 4.95
CHEMBL5277196 IC50 = 15440.0 nM 4.81
CHEMBL5269382 IC50 = 16680.0 nM 4.78
CHEMBL5290106 IC50 = 26880.0 nM 4.57
CHEMBL5290029 IC50 > 40000.0 nM -
CHEMBL5265986 IC50 > 40000.0 nM -
CHEMBL5282733 IC50 > 40000.0 nM -
CHEMBL5282485 IC50 > 40000.0 nM -
CHEMBL5267216 IC50 > 40000.0 nM -
CHEMBL5286147 IC50 > 40000.0 nM -
CHEMBL5276695 IC50 > 40000.0 nM -
CHEMBL5289901 IC50 > 40000.0 nM -