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Assay Detail

CHEMBL677547

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

Binding
Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen
9
Total Activities
9
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

Novel 3 alpha-(diphenylmethoxy)tropane analogs: potent dopamine uptake inhibitors without cocaine-like behavioral profiles.
Newman AH, Allen AC, Izenwasser S, Katz JL.
J Med Chem (1994) 37 : 2258 -2261
PubMed 8057273 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.03 7.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 7.94
CHEMBL543113 1 7.93
CHEMBL541825 1 7.70
CHEMBL3085569 1 7.52
CHEMBL557818 1 7.11
CHEMBL1201203 BENZTROPINE 4.0 1 6.93
CHEMBL370805 COCAINE 4.0 1 6.41
CHEMBL310310 1 6.07
CHEMBL545227 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE Ki = 11.6 nM 7.94
CHEMBL543113 Ki = 11.8 nM 7.93
CHEMBL541825 Ki = 20.0 nM 7.70
CHEMBL3085569 Ki = 30.0 nM 7.52
CHEMBL557818 Ki = 78.4 nM 7.11
CHEMBL1201203 BENZTROPINE Ki = 118.0 nM 6.93
CHEMBL370805 COCAINE Ki = 388.0 nM 6.41
CHEMBL310310 Ki = 854.0 nM 6.07
CHEMBL545227 Ki = 2000.0 nM 5.70