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Assay Detail

CHEMBL1647746

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

Binding
Displacement of [3H]WIN-35428 from human DAT stably expressed in mouse N2A cells by scintillation countnig
9
Total Activities
9
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

Azido-iodo-N-benzyl derivatives of threo-methylphenidate (Ritalin, Concerta): Rational design, synthesis, pharmacological evaluation, and dopamine transporter photoaffinity labeling.
Lapinsky DJ, Velagaleti R, Yarravarapu N, Liu Y, Huang Y, Surratt CK, Lever JR, Foster JD, Acharya R, Vaughan RA, Deutsch HM.
Bioorg Med Chem (2011) 19 : 504 -512
PubMed 21129986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.66 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1641691 1 8.35
CHEMBL1253735 1 7.85
CHEMBL827 DEXMETHYLPHENIDATE 4.0 1 7.60
CHEMBL1641692 1 6.44
CHEMBL1641694 1 6.29
CHEMBL1641695 1 6.18
CHEMBL1641697 1 5.95
CHEMBL1641696 1 5.69
CHEMBL1641693 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1641691 Ki = 4.5 nM 8.35
CHEMBL1253735 Ki = 14.0 nM 7.85
CHEMBL827 DEXMETHYLPHENIDATE Ki = 25.0 nM 7.60
CHEMBL1641692 Ki = 363.0 nM 6.44
CHEMBL1641694 Ki = 517.0 nM 6.29
CHEMBL1641695 Ki = 658.0 nM 6.18
CHEMBL1641697 Ki = 1112.0 nM 5.95
CHEMBL1641696 Ki = 2056.0 nM 5.69
CHEMBL1641693 Ki = 2754.0 nM 5.56