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Assay Detail

CHEMBL832816

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

ADMET
Inhibitory concentration against human cytochrome P450 2A6
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 2A6 (CHEMBL5282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme.
Rahnasto M, Raunio H, Poso A, Wittekindt C, Juvonen RO.
J Med Chem (2005) 48 : 440 -449
PubMed 15658857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 4.98 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192643 1 6.26
CHEMBL191864 1 6.17
CHEMBL195036 1 5.77
CHEMBL195895 1 5.62
CHEMBL195820 1 5.60
CHEMBL191357 1 5.60
CHEMBL405 AMPHETAMINE 4.0 1 5.46
CHEMBL15972 BENZALDEHYDE -1.0 1 5.41
CHEMBL610 PHENETHYLAMINE 1 5.36
CHEMBL190927 1 5.31
CHEMBL161598 ANISALDEHYDE 1 5.29
CHEMBL103299 1 5.28
CHEMBL372646 1 5.27
CHEMBL447481 1 5.17
CHEMBL370524 1 5.08
CHEMBL194983 1 5.00
CHEMBL370944 1 4.92
CHEMBL364891 1 4.82
CHEMBL190982 1,4-DICHLOROBENZENE 1 4.77
CHEMBL195338 1 4.75
CHEMBL191664 1 4.68
CHEMBL191667 1 4.60
CHEMBL16293 NAPHTHALENE 1.0 1 4.60
CHEMBL382541 1 4.58
CHEMBL435106 1 4.51
CHEMBL373024 1 4.51
CHEMBL383808 1 4.47
CHEMBL191745 1 4.44
CHEMBL193373 1 4.28
CHEMBL195407 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192643 IC50 = 550.0 nM 6.26
CHEMBL191864 IC50 = 670.0 nM 6.17
CHEMBL195036 IC50 = 1700.0 nM 5.77
CHEMBL195895 IC50 = 2400.0 nM 5.62
CHEMBL195820 IC50 = 2500.0 nM 5.60
CHEMBL191357 IC50 = 2500.0 nM 5.60
CHEMBL405 AMPHETAMINE IC50 = 3500.0 nM 5.46
CHEMBL15972 BENZALDEHYDE IC50 = 3920.0 nM 5.41
CHEMBL610 PHENETHYLAMINE IC50 = 4410.0 nM 5.36
CHEMBL190927 IC50 = 4880.0 nM 5.31
CHEMBL161598 ANISALDEHYDE IC50 = 5150.0 nM 5.29
CHEMBL103299 IC50 = 5300.0 nM 5.28
CHEMBL372646 IC50 = 5400.0 nM 5.27
CHEMBL447481 IC50 = 6700.0 nM 5.17
CHEMBL370524 IC50 = 8300.0 nM 5.08
CHEMBL194983 IC50 = 10000.0 nM 5.00
CHEMBL370944 IC50 = 12000.0 nM 4.92
CHEMBL364891 IC50 = 15000.0 nM 4.82
CHEMBL190982 1,4-DICHLOROBENZENE IC50 = 17000.0 nM 4.77
CHEMBL195338 IC50 = 18000.0 nM 4.75
CHEMBL191664 IC50 = 21000.0 nM 4.68
CHEMBL191667 IC50 = 25000.0 nM 4.60
CHEMBL16293 NAPHTHALENE IC50 = 25000.0 nM 4.60
CHEMBL382541 IC50 = 26000.0 nM 4.58
CHEMBL435106 IC50 = 31000.0 nM 4.51
CHEMBL373024 IC50 = 31000.0 nM 4.51
CHEMBL383808 IC50 = 34000.0 nM 4.47
CHEMBL191745 IC50 = 36000.0 nM 4.44
CHEMBL193373 IC50 = 52000.0 nM 4.28
CHEMBL195407 IC50 = 59000.0 nM 4.23
CHEMBL364698 IC50 = 60000.0 nM 4.22
CHEMBL195857 IC50 = 62000.0 nM 4.21
CHEMBL46730 PHENANTHRENE IC50 = 97000.0 nM 4.01
CHEMBL195661 IC50 = 200000.0 nM -
CHEMBL194502 IC50 = 280000.0 nM -
CHEMBL194876 IC50 = 400000.0 nM -
CHEMBL9732 R-NICOTINE IC50 = 580000.0 nM -
CHEMBL192418 IC50 = 830000.0 nM -
CHEMBL194711 IC50 > 100000.0 nM -
CHEMBL363803 IC50 = 130000.0 nM -
CHEMBL122617 1-NAPHTHOL IC50 = 130000.0 nM -
CHEMBL194931 QUINALDINE IC50 = 190000.0 nM -
CHEMBL364705 IC50 > 60000.0 nM -
CHEMBL276334 IC50 = 150000.0 nM -
CHEMBL192267 IC50 = 2000000.0 nM -
CHEMBL578211 COTININE IC50 = 35000000.0 nM -
CHEMBL195537 IC50 > 600000.0 nM -
CHEMBL14126 BETANAPHTHOL IC50 = 140000.0 nM -