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Assay Detail

CHEMBL1120512

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

ADMET
Inhibition of CYP2D6
16
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Fray MJ, Fish PV, Allan GA, Bish G, Clarke N, Eccles R, Harrison AC, Le Net JL, Phillips SC, Regan N, Sobry C, Stobie A, Wakenhut F, Westbrook D, Westbrook SL, Whitlock GA.
Bioorg Med Chem Lett (2010) 20 : 3788 -3792
PubMed 20471260 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.16 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1084033 1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) 2 5.85
CHEMBL1083708 1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) 3 5.52
CHEMBL1083426 1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) 2 5.51
CHEMBL375131 1 5.44
CHEMBL1085567 1 4.92
CHEMBL1085959 1 4.75
CHEMBL214335 2 4.70
CHEMBL403441 1 4.52
CHEMBL1080787 1 -
CHEMBL1084971 1 -
CHEMBL1086273 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1084033 1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) IC50 = 1400.0 nM 5.85
CHEMBL1083708 1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) IC50 = 3000.0 nM 5.52
CHEMBL1083426 1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) IC50 = 3100.0 nM 5.51
CHEMBL1083426 1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) IC50 = 3500.0 nM 5.46
CHEMBL375131 IC50 = 3600.0 nM 5.44
CHEMBL1084033 1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) IC50 = 3600.0 nM 5.44
CHEMBL1083708 1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) IC50 = 4900.0 nM 5.31
CHEMBL1085567 IC50 = 12100.0 nM 4.92
CHEMBL1085959 IC50 = 17700.0 nM 4.75
CHEMBL214335 IC50 = 20000.0 nM 4.70
CHEMBL403441 IC50 = 30000.0 nM 4.52
CHEMBL1083708 1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) IC50 = 30000.0 nM 4.52
CHEMBL1080787 IC50 > 30000.0 nM -
CHEMBL1084971 IC50 > 30000.0 nM -
CHEMBL1086273 IC50 > 30000.0 nM -
CHEMBL214335 IC50 > 30000.0 nM -