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Assay Detail

CHEMBL2343885

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ADMET
Inhibition of human recombinant CYP2D6 by luminescence assay
16
Total Activities
16
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 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel class of 3-(phenoxy-phenyl-methyl)-pyrrolidines as potent and balanced norepinephrine and serotonin reuptake inhibitors: synthesis and structure-activity relationships.
Van Orden LJ, Van Dyke PM, Saito DR, Church TJ, Chang R, Smith JA, Martin WJ, Jaw-Tsai S, Stangeland EL.
Bioorg Med Chem Lett (2013) 23 : 1456 -1461
PubMed 23347683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.76 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2337594 1 6.60
CHEMBL2338036 1 6.50
CHEMBL2338035 1 6.30
CHEMBL2337607 1 6.20
CHEMBL2337602 1 6.10
CHEMBL2338043 1 6.00
CHEMBL2338042 1 5.90
CHEMBL2338049 1 5.70
CHEMBL2338041 1 5.70
CHEMBL1175 DULOXETINE 4.0 1 5.70
CHEMBL180101 ESREBOXETINE 3.0 1 5.50
CHEMBL2338053 1 5.40
CHEMBL2338048 1 5.40
CHEMBL2337608 1 5.40
CHEMBL2338038 1 5.30
CHEMBL259209 MILNACIPRAN 4.0 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2337594 IC50 = 251.19 nM 6.60
CHEMBL2338036 IC50 = 316.23 nM 6.50
CHEMBL2338035 IC50 = 501.19 nM 6.30
CHEMBL2337607 IC50 = 630.96 nM 6.20
CHEMBL2337602 IC50 = 794.33 nM 6.10
CHEMBL2338043 IC50 = 1000.0 nM 6.00
CHEMBL2338042 IC50 = 1258.93 nM 5.90
CHEMBL2338049 IC50 = 1995.26 nM 5.70
CHEMBL2338041 IC50 = 1995.26 nM 5.70
CHEMBL1175 DULOXETINE IC50 = 1995.26 nM 5.70
CHEMBL180101 ESREBOXETINE IC50 = 3162.28 nM 5.50
CHEMBL2338053 IC50 = 3981.07 nM 5.40
CHEMBL2338048 IC50 = 3981.07 nM 5.40
CHEMBL2337608 IC50 = 3981.07 nM 5.40
CHEMBL2338038 IC50 = 5011.87 nM 5.30
CHEMBL259209 MILNACIPRAN IC50 = 31622.78 nM 4.50