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Assay Detail

CHEMBL999388

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

ADMET
Inhibition of human recombinant CYP1A2
41
Total Activities
21
Compounds Tested
2
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

Structure-activity relationships for the inhibition of recombinant human cytochromes P450 by curcumin analogues.
Appiah-Opong R, de Esch I, Commandeur JN, Andarini M, Vermeulen NP.
Eur J Med Chem (2008) 43 : 1621 -1631
PubMed 18249473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 4.81 6.05
log(1/IC50) 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274993 2,6-DIBENZYLIDENECYCLOHEXANONE 2 6.05
CHEMBL404678 2 5.58
CHEMBL503570 2 5.47
CHEMBL497783 2 5.47
CHEMBL17201 2 5.43
CHEMBL498591 2 5.40
CHEMBL498193 2 4.98
CHEMBL482410 2 4.96
CHEMBL502160 2 4.68
CHEMBL496321 2 4.58
CHEMBL498371 2 4.55
CHEMBL498590 2 4.55
CHEMBL407034 2 4.52
CHEMBL151734 2 4.44
CHEMBL497137 2 4.43
CHEMBL270361 2 4.41
CHEMBL140 CURCUMIN 3.0 1 4.40
CHEMBL128729 2 4.38
CHEMBL498372 2 4.37
CHEMBL452101 2 4.34
CHEMBL493001 2 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274993 2,6-DIBENZYLIDENECYCLOHEXANONE IC50 = 900.0 nM 6.05
CHEMBL404678 IC50 = 2600.0 nM 5.58
CHEMBL497783 IC50 = 3400.0 nM 5.47
CHEMBL503570 IC50 = 3400.0 nM 5.47
CHEMBL17201 IC50 = 3700.0 nM 5.43
CHEMBL498591 IC50 = 4000.0 nM 5.40
CHEMBL498193 IC50 = 10400.0 nM 4.98
CHEMBL482410 IC50 = 11000.0 nM 4.96
CHEMBL502160 IC50 = 21000.0 nM 4.68
CHEMBL496321 IC50 = 26600.0 nM 4.58
CHEMBL498590 IC50 = 28000.0 nM 4.55
CHEMBL498371 IC50 = 28400.0 nM 4.55
CHEMBL407034 IC50 = 30400.0 nM 4.52
CHEMBL151734 IC50 = 36600.0 nM 4.44
CHEMBL497137 IC50 = 36700.0 nM 4.43
CHEMBL270361 IC50 = 38900.0 nM 4.41
CHEMBL140 CURCUMIN IC50 = 40000.0 nM 4.40
CHEMBL128729 IC50 = 41500.0 nM 4.38
CHEMBL498372 IC50 = 42800.0 nM 4.37
CHEMBL452101 IC50 = 45600.0 nM 4.34
CHEMBL493001 IC50 = 75200.0 nM 4.12
CHEMBL274993 2,6-DIBENZYLIDENECYCLOHEXANONE IC50 = 899497.58 nM -
CHEMBL482410 IC50 = 10990058.39 nM -
CHEMBL502160 IC50 = 20989398.84 nM -
CHEMBL498193 IC50 = 10399201.66 nM -
CHEMBL404678 IC50 = 2600159.56 nM -
CHEMBL503570 IC50 = 3396252.73 nM -
CHEMBL452101 IC50 = 45603691.6 nM -
CHEMBL270361 IC50 = 38904514.5 nM -
CHEMBL151734 IC50 = 36559479.16 nM -
CHEMBL497137 IC50 = 36728230.05 nM -
CHEMBL498371 IC50 = 28379190.28 nM -
CHEMBL498372 IC50 = 42756288.62 nM -
CHEMBL128729 IC50 = 41495404.26 nM -
CHEMBL17201 IC50 = 3698281.8 nM -
CHEMBL496321 IC50 = 26607250.6 nM -
CHEMBL498590 IC50 = 27989813.2 nM -
CHEMBL498591 IC50 = 3999447.5 nM -
CHEMBL497783 IC50 = 3396252.73 nM -
CHEMBL407034 IC50 = 30408850.26 nM -
CHEMBL493001 log(1/IC50) = 1.124 mM -