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Assay Detail

CHEMBL827154

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ADMET
Inhibitory concentration against cytochrome P450 2D6
37
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition.
Kemp CA, Flanagan JU, van Eldik AJ, Maréchal JD, Wolf CR, Roberts GC, Paine MJ, Sutcliffe MJ.
J Med Chem (2004) 47 : 5340 -5346
PubMed 15481972 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 5.24 8.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL15245 YOHIMBINE 3.0 1 8.08
CHEMBL1294 QUINIDINE 4.0 1 8.00
CHEMBL22077 HYCANTHONE 2.0 1 5.82
CHEMBL188237 1 5.80
CHEMBL588619 CINCHONINE -1.0 1 5.75
CHEMBL189724 1 5.68
CHEMBL187216 1 5.66
CHEMBL363332 1 5.62
CHEMBL445 NORTRIPTYLINE 4.0 1 5.58
CHEMBL188641 2 5.46
CHEMBL422093 1 5.14
CHEMBL189830 1 5.14
CHEMBL364208 1 5.10
CHEMBL186039 1 5.07
CHEMBL188797 1 5.06
CHEMBL43 AMSACRINE 4.0 2 4.99
CHEMBL284134 1 4.96
CHEMBL188427 ACODAZOLE 2.0 1 4.74
CHEMBL84440 1 4.52
CHEMBL428676 AMONAFIDE 3.0 1 4.40
CHEMBL114283 DANIQUIDONE 2.0 1 4.32
CHEMBL515 CHLORAMBUCIL 4.0 1 4.19
CHEMBL58 MITOXANTRONE 4.0 1 4.12
CHEMBL188642 1 4.03
CHEMBL186414 1 -
CHEMBL363082 1 -
CHEMBL182440 1 -
CHEMBL188374 1 -
CHEMBL189023 1 -
CHEMBL509895 BRUCEANTIN 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL15245 YOHIMBINE IC50 = 8.4 nM 8.08
CHEMBL1294 QUINIDINE IC50 = 10.0 nM 8.00
CHEMBL22077 HYCANTHONE IC50 = 1500.0 nM 5.82
CHEMBL188237 IC50 = 1600.0 nM 5.80
CHEMBL588619 CINCHONINE IC50 = 1800.0 nM 5.75
CHEMBL189724 IC50 = 2100.0 nM 5.68
CHEMBL187216 IC50 = 2200.0 nM 5.66
CHEMBL363332 IC50 = 2400.0 nM 5.62
CHEMBL445 NORTRIPTYLINE IC50 = 2600.0 nM 5.58
CHEMBL188641 IC50 = 3500.0 nM 5.46
CHEMBL422093 IC50 = 7300.0 nM 5.14
CHEMBL189830 IC50 = 7200.0 nM 5.14
CHEMBL364208 IC50 = 8000.0 nM 5.10
CHEMBL186039 IC50 = 8500.0 nM 5.07
CHEMBL188797 IC50 = 8700.0 nM 5.06
CHEMBL43 AMSACRINE IC50 = 10200.0 nM 4.99
CHEMBL43 AMSACRINE IC50 = 10500.0 nM 4.98
CHEMBL284134 IC50 = 11000.0 nM 4.96
CHEMBL188427 ACODAZOLE IC50 = 18100.0 nM 4.74
CHEMBL84440 IC50 = 30000.0 nM 4.52
CHEMBL428676 AMONAFIDE IC50 = 39600.0 nM 4.40
CHEMBL114283 DANIQUIDONE IC50 = 48000.0 nM 4.32
CHEMBL515 CHLORAMBUCIL IC50 = 65100.0 nM 4.19
CHEMBL188641 IC50 = 71000.0 nM 4.15
CHEMBL58 MITOXANTRONE IC50 = 76300.0 nM 4.12
CHEMBL188642 IC50 = 94300.0 nM 4.03
CHEMBL361064 IC50 = 554000.0 nM -
CHEMBL43326 IC50 = 196000.0 nM -
CHEMBL185952 IC50 = 310000.0 nM -
CHEMBL186292 IC50 = 570000.0 nM -
CHEMBL187575 IC50 = 265000.0 nM -
CHEMBL509895 BRUCEANTIN IC50 = 514000.0 nM -
CHEMBL189023 IC50 = 288000.0 nM -
CHEMBL188374 IC50 = 1017000.0 nM -
CHEMBL182440 IC50 = 699000.0 nM -
CHEMBL363082 IC50 = 2021000.0 nM -
CHEMBL186414 IC50 = 234000.0 nM -