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Assay Detail

CHEMBL1647932

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Binding
Inhibition of human recombinant norepinephrine transporter
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor.
Shao L, Ma J, Wang F, Malcolm SC, Hewitt MC, Campbell UC, Spicer NA, Hardy LW, Schreiber R, Spear KL, Varney MA.
Bioorg Med Chem Lett (2011) 21 : 520 -523
PubMed 21095126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.99 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1642897 1 7.14
CHEMBL1643512 1 6.86
CHEMBL1643513 1 6.22
CHEMBL1643509 1 6.03
CHEMBL1643511 1 6.03
CHEMBL1643517 1 6.00
CHEMBL1643514 1 5.93
CHEMBL1643518 1 5.90
CHEMBL1643516 1 5.73
CHEMBL1641622 1 5.73
CHEMBL1643515 1 5.59
CHEMBL1643519 1 5.51
CHEMBL1643510 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1642897 IC50 = 73.0 nM 7.14
CHEMBL1643512 IC50 = 138.0 nM 6.86
CHEMBL1643513 IC50 = 601.0 nM 6.22
CHEMBL1643509 IC50 = 926.0 nM 6.03
CHEMBL1643511 IC50 = 934.0 nM 6.03
CHEMBL1643517 IC50 = 1005.0 nM 6.00
CHEMBL1643514 IC50 = 1184.0 nM 5.93
CHEMBL1643518 IC50 = 1246.0 nM 5.90
CHEMBL1643516 IC50 = 1857.0 nM 5.73
CHEMBL1641622 IC50 = 1849.0 nM 5.73
CHEMBL1643515 IC50 = 2597.0 nM 5.59
CHEMBL1643519 IC50 = 3091.0 nM 5.51
CHEMBL1643510 IC50 = 7141.0 nM 5.15