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Assay Detail

CHEMBL2389181

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

Binding
Displacement of [3H]WIN35428 from human DAT transfected in HEK293 cells after 3 hrs by Wallac counting analysis
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
Dreyfus N, Myers JK, Badescu VO, de Frutos O, de la Puente ML, Ding C, Filla SA, Fynboe K, Gernert DL, Heinz BA, Hemrick-Luecke SK, Johnson KW, Johnson MP, López P, Love PL, Martin LJ, Masquelin T, McCoy MJ, Mendiola J, Morrow D, Muhlhauser M, Pascual G, Perun TJ, Pfeifer LA, Phebus LA, Richards SJ, Rincón JA, Seest EP, Shah J, Shaojuan J, Simmons RM, Stephenson GA, Tromiczak EG, Thompson LK, Walter MW, Weber WW, Zarrinmayeh H, Thomas CE, Joshi E, Iyengar S, Johansson AM.
ACS Med Chem Lett (2013) 4 : 560 -564
PubMed 24900709 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.36 6.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386163 2 6.45
CHEMBL1175 DULOXETINE 4.0 1 6.32
CHEMBL259209 MILNACIPRAN 4.0 1 -
CHEMBL1118 DESVENLAFAXINE 4.0 1 -
CHEMBL637 VENLAFAXINE 4.0 1 -
CHEMBL2386166 1 -
CHEMBL2386165 1 -
CHEMBL2386164 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386163 Ki = 354.0 nM 6.45
CHEMBL1175 DULOXETINE Ki = 484.0 nM 6.32
CHEMBL2386163 Ki = 475.0 nM 6.32
CHEMBL259209 MILNACIPRAN Ki > 854.0 nM -
CHEMBL1118 DESVENLAFAXINE Ki > 854.0 nM -
CHEMBL637 VENLAFAXINE Ki > 890.0 nM -
CHEMBL2386166 Ki > 890.0 nM -
CHEMBL2386165 Ki > 890.0 nM -
CHEMBL2386164 Ki > 890.0 nM -