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Assay Detail

CHEMBL784335

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

Functional
Compound was evaluated for its ability to inhibit uptake of [3H]-dopamine into rat caudate putamen tissue
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Caudate-putamen
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Synthesis, structure, dopamine transporter affinity, and dopamine uptake inhibition of 6-alkyl-3-benzyl-2-[(methoxycarbonyl)methyl]tropane derivatives.
Lomenzo SA, Izenwasser S, Katz JL, Terry PD, Zhu N, Klein CL, Trudell ML.
J Med Chem (1997) 40 : 4406 -4414
PubMed 9435910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.61 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339395 1 7.03
CHEMBL3085521 2 6.97
CHEMBL136499 1 6.79
CHEMBL545080 2 6.68
CHEMBL1790051 1 6.43
CHEMBL370805 COCAINE 4.0 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339395 IC50 = 94.0 nM 7.03
CHEMBL3085521 IC50 = 107.0 nM 6.97
CHEMBL136499 IC50 = 161.0 nM 6.79
CHEMBL545080 IC50 = 208.0 nM 6.68
CHEMBL1790051 IC50 = 373.0 nM 6.43
CHEMBL370805 COCAINE IC50 = 405.0 nM 6.39
CHEMBL545080 IC50 = 457.0 nM 6.34
CHEMBL3085521 IC50 = 532.0 nM 6.27