Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL672390

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

Binding
Compound was evaluated for inhibition of specifically bound [3H]- cocaine (2.7 nM) against Dopamine transporter in cynomolgus monkeys
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cercopithecidae
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor.
Milius RA, Saha JK, Madras BK, Neumeyer JL.
J Med Chem (1991) 34 : 1728 -1731
PubMed 2033595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.48 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2079586 1 7.76
CHEMBL48225 1 7.65
CHEMBL21112 1 7.44
CHEMBL416818 1 7.37
CHEMBL370805 COCAINE 4.0 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2079586 IC50 = 17.5 nM 7.76
CHEMBL48225 IC50 = 22.6 nM 7.65
CHEMBL21112 IC50 = 36.4 nM 7.44
CHEMBL416818 IC50 = 43.0 nM 7.37
CHEMBL370805 COCAINE IC50 = 67.8 nM 7.17