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Assay Detail

CHEMBL2065334

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

Binding
Displacement of [3H]WIN-35,428 from human DAT expressed in mouse N2A cells after 15 mins by liquid scintillation counting
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type N2a
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Evolution of a Compact Photoprobe for the Dopamine Transporter Based on (±)-threo-Methylphenidate.
Lapinsky DJ, Yarravarapu N, Nolan TL, Surratt CK, Lever JR, Tomlinson M, Vaughan RA, Deutsch HM.
ACS Med Chem Lett (2012) 3 : 378 -382
PubMed 23066448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.01 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1179011 1 8.74
CHEMBL2062931 1 8.40
CHEMBL1641691 1 8.35
CHEMBL1253709 1 8.20
CHEMBL2062932 1 8.04
CHEMBL827 DEXMETHYLPHENIDATE 4.0 1 7.80
CHEMBL2062933 1 7.46
CHEMBL1254439 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1179011 Ki = 1.8 nM 8.74
CHEMBL2062931 Ki = 4.0 nM 8.40
CHEMBL1641691 Ki = 4.5 nM 8.35
CHEMBL1253709 Ki = 6.3 nM 8.20
CHEMBL2062932 Ki = 9.1 nM 8.04
CHEMBL827 DEXMETHYLPHENIDATE Ki = 16.0 nM 7.80
CHEMBL2062933 Ki = 35.0 nM 7.46
CHEMBL1254439 Ki = 77.0 nM 7.11