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Assay Detail

CHEMBL872475

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

Binding
Binding affinity was determined against cocaine receptor by measuring the ability of compound to displace bound [3H]-3 from rat caudate-putamen tissue
3
Total Activities
2
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, cocaine receptor affinity, and dopamine uptake inhibition of several new 2 beta-substituted 3 beta-phenyltropanes.
Kelkar SV, Izenwasser S, Katz JL, Klein CL, Zhu N, Trudell ML.
J Med Chem (1994) 37 : 3875 -3877
PubMed 7966147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.80 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370805 COCAINE 4.0 2 7.50
CHEMBL1790051 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370805 COCAINE Ki = 32.0 nM 7.50
CHEMBL1790051 Ki = 314.0 nM 6.50
CHEMBL370805 COCAINE Ki = 388.0 nM 6.41