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Assay Detail

CHEMBL675226

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

Binding
The compound was tested for its affinity at the rat striatal dopamine transporter by the displacement of [3H]WIN-35428
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Further evidence for a dopamine reuptake pharmacophore. The effect of N-methylation on Threo-methylphenidate and its analogs
Froimowitz M, Deutsh HM, Shi Q, Wu K, Glaser R, Adin I, George C, Schweri MM
Bioorg Med Chem Lett (1997) 7 : 1213 -1218
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.04 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19607 1 8.29
CHEMBL1253339 1 7.67
CHEMBL283772 1 7.48
CHEMBL827 DEXMETHYLPHENIDATE 4.0 1 7.08
CHEMBL1253698 1 7.01
CHEMBL19686 1 6.97
CHEMBL20110 1 6.86
CHEMBL19869 1 6.79
CHEMBL20099 1 6.30
CHEMBL19891 1 5.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19607 IC50 = 5.1 nM 8.29
CHEMBL1253339 IC50 = 21.4 nM 7.67
CHEMBL283772 IC50 = 33.0 nM 7.48
CHEMBL827 DEXMETHYLPHENIDATE IC50 = 83.0 nM 7.08
CHEMBL1253698 IC50 = 98.0 nM 7.01
CHEMBL19686 IC50 = 108.0 nM 6.97
CHEMBL20110 IC50 = 139.0 nM 6.86
CHEMBL19869 IC50 = 161.0 nM 6.79
CHEMBL20099 IC50 = 500.0 nM 6.30
CHEMBL19891 IC50 = 1220.0 nM 5.91