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Assay Detail

CHEMBL784328

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

Functional
Compound was evaluated for its ability to block the [3H]-Dopamine uptake in rat caudate-putamen
9
Total Activities
9
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

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
IC50 9 6.65 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 8.30
CHEMBL543113 1 7.15
CHEMBL541825 1 7.12
CHEMBL3085569 1 6.94
CHEMBL1201203 BENZTROPINE 4.0 1 6.39
CHEMBL557818 1 6.33
CHEMBL545227 1 5.54
CHEMBL310310 1 5.45
CHEMBL370805 COCAINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE IC50 = 5.0 nM 8.30
CHEMBL543113 IC50 = 71.0 nM 7.15
CHEMBL541825 IC50 = 75.0 nM 7.12
CHEMBL3085569 IC50 = 115.0 nM 6.94
CHEMBL1201203 BENZTROPINE IC50 = 403.0 nM 6.39
CHEMBL557818 IC50 = 468.0 nM 6.33
CHEMBL545227 IC50 = 2876.0 nM 5.54
CHEMBL310310 IC50 = 3519.0 nM 5.45
CHEMBL370805 COCAINE IC50 = 123254.0 nM -