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Assay Detail

CHEMBL674109

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

Binding
Inhibition of [3H]WIN-35428 binding to the dopamine transporter
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
Carroll FI, Lewin AH, Boja JW, Kuhar MJ.
J Med Chem (1992) 35 : 969 -981
PubMed 1552510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.97 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610897 1 9.00
CHEMBL2310852 1 8.70
CHEMBL2373744 1 8.10
CHEMBL1237136 1 8.00
CHEMBL2373745 1 7.89
CHEMBL607198 1 7.60
CHEMBL175251 1 7.15
CHEMBL120901 3 7.00
CHEMBL425854 1 6.71
CHEMBL178269 1 6.64
CHEMBL262308 1 6.61
CHEMBL176723 1 6.59
CHEMBL434361 1 6.22
CHEMBL177269 1 6.17
CHEMBL1790051 1 5.54
CHEMBL369375 1 5.47
CHEMBL1947052 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610897 IC50 = 1.0 nM 9.00
CHEMBL2310852 IC50 = 2.0 nM 8.70
CHEMBL2373744 IC50 = 8.0 nM 8.10
CHEMBL1237136 IC50 = 10.0 nM 8.00
CHEMBL2373745 IC50 = 13.0 nM 7.89
CHEMBL607198 IC50 = 25.0 nM 7.60
CHEMBL175251 IC50 = 71.0 nM 7.15
CHEMBL120901 IC50 = 100.0 nM 7.00
CHEMBL120901 IC50 = 102.0 nM 6.99
CHEMBL425854 IC50 = 196.0 nM 6.71
CHEMBL120901 IC50 = 208.0 nM 6.68
CHEMBL178269 IC50 = 227.0 nM 6.64
CHEMBL262308 IC50 = 248.0 nM 6.61
CHEMBL176723 IC50 = 257.0 nM 6.59
CHEMBL434361 IC50 = 601.0 nM 6.22
CHEMBL177269 IC50 = 668.0 nM 6.17
CHEMBL1790051 IC50 = 2900.0 nM 5.54
CHEMBL369375 IC50 = 3370.0 nM 5.47
CHEMBL1947052 IC50 = 5180.0 nM 5.29