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Assay Detail

CHEMBL1647134

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

ADMET
Inhibition of CYP2C19
14
Total Activities
14
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 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.
Shao L, Wang F, Malcolm SC, Ma J, Hewitt MC, Campbell UC, Bush LR, Spicer NA, Engel SR, Saraswat LD, Hardy LW, Koch P, Schreiber R, Spear KL, Varney MA.
Bioorg Med Chem (2011) 19 : 663 -676
PubMed 21093273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.50 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL809 SERTRALINE 4.0 1 6.51
CHEMBL1642913 1 5.79
CHEMBL1642907 1 5.66
CHEMBL1642912 1 5.42
CHEMBL1642895 1 5.28
CHEMBL1642908 1 5.22
CHEMBL1642906 1 5.11
CHEMBL1642897 1 4.99
CHEMBL1642914 1 -
CHEMBL1642915 1 -
CHEMBL1642916 1 -
CHEMBL1642917 1 -
CHEMBL1642894 1 -
CHEMBL1642896 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL809 SERTRALINE IC50 = 310.0 nM 6.51
CHEMBL1642913 IC50 = 1640.0 nM 5.79
CHEMBL1642907 IC50 = 2170.0 nM 5.66
CHEMBL1642912 IC50 = 3760.0 nM 5.42
CHEMBL1642895 IC50 = 5260.0 nM 5.28
CHEMBL1642908 IC50 = 6020.0 nM 5.22
CHEMBL1642906 IC50 = 7690.0 nM 5.11
CHEMBL1642897 IC50 = 10150.0 nM 4.99
CHEMBL1642914 IC50 - -
CHEMBL1642915 IC50 - -
CHEMBL1642916 IC50 - -
CHEMBL1642917 IC50 - -
CHEMBL1642894 IC50 > 25000.0 nM -
CHEMBL1642896 IC50 > 25000.0 nM -