Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL670597

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

Binding
Affinity against cocaine binding site of dopamine transporter in rat striatum using [3H]2b as radioligand.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, ligand binding, QSAR, and CoMFA study of 3 beta-(p-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters.
Carroll FI, Gao YG, Rahman MA, Abraham P, Parham K, Lewin AH, Boja JW, Kuhar MJ.
J Med Chem (1991) 34 : 2719 -2725
PubMed 1895292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.84 8.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610897 1 8.93
CHEMBL300226 1 8.90
CHEMBL2373962 1 8.77
CHEMBL2310929 1 8.74
CHEMBL2310852 1 8.67
CHEMBL2373744 1 8.09
CHEMBL1237136 1 8.00
CHEMBL2373745 1 7.88
CHEMBL2079586 1 7.80
CHEMBL1790051 1 7.64
CHEMBL607198 1 7.61
CHEMBL2310855 1 7.19
CHEMBL2310854 1 7.17
CHEMBL120901 1 6.99
CHEMBL2310851 1 6.59
CHEMBL2310853 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610897 IC50 = 1.17 nM 8.93
CHEMBL300226 IC50 = 1.26 nM 8.90
CHEMBL2373962 IC50 = 1.71 nM 8.77
CHEMBL2310929 IC50 = 1.81 nM 8.74
CHEMBL2310852 IC50 = 2.12 nM 8.67
CHEMBL2373744 IC50 = 8.14 nM 8.09
CHEMBL1237136 IC50 = 10.1 nM 8.00
CHEMBL2373745 IC50 = 13.1 nM 7.88
CHEMBL2079586 IC50 = 15.7 nM 7.80
CHEMBL1790051 IC50 = 23.0 nM 7.64
CHEMBL607198 IC50 = 24.8 nM 7.61
CHEMBL2310855 IC50 = 64.2 nM 7.19
CHEMBL2310854 IC50 = 68.0 nM 7.17
CHEMBL120901 IC50 = 102.0 nM 6.99
CHEMBL2310851 IC50 = 257.0 nM 6.59
CHEMBL2310853 IC50 = 316.0 nM 6.50