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Assay Detail

CHEMBL677367

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

Binding
Binding affinity towards dopamine transporter using [3H]WIN-35428 as radioligand in rat caudate-putamen tissue
8
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Caudate-putamen
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and dopamine transporter affinity of the four stereoisomers of (+/-)-2-(methoxycarbonyl)-7-methyl-3-phenyl-7-azabicyclo[2.2.1]heptane.
Zhang C, Izenwasser S, Katz JL, Terry PD, Trudell ML.
J Med Chem (1998) 41 : 2430 -2435
PubMed 9632375 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.76 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370805 COCAINE 4.0 2 7.50
CHEMBL1790051 2 7.48
CHEMBL414881 1 5.25
CHEMBL78985 1 4.72
CHEMBL81329 1 4.22
CHEMBL545473 1 4.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370805 COCAINE Ki = 32.0 nM 7.50
CHEMBL1790051 Ki = 33.0 nM 7.48
CHEMBL1790051 Ki = 310.0 nM 6.51
CHEMBL370805 COCAINE Ki = 390.0 nM 6.41
CHEMBL414881 Ki = 5620.0 nM 5.25
CHEMBL78985 Ki = 18900.0 nM 4.72
CHEMBL81329 Ki = 60400.0 nM 4.22
CHEMBL545473 Ki = 96500.0 nM 4.01