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Assay Detail

CHEMBL677375

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

Binding
Displacement of [3H]GBR-12935 from rat forebrain Dopamine transporter
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis and monoamine transporter affinity of 2beta-carbomethoxy-3beta-(2''-, 3''- or 4''-substituted) biphenyltropanes.
Tamagnan G, Baldwin RM, Kula NS, Baldessarini RJ, Innis RB.
Bioorg Med Chem Lett (2000) 10 : 1783 -1785
PubMed 10969967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.63 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311347 1 9.02
CHEMBL300511 1 8.29
CHEMBL301174 1 8.02
CHEMBL52334 1 7.91
CHEMBL296394 1 7.88
CHEMBL51896 1 7.82
CHEMBL50997 1 7.72
CHEMBL50674 1 7.62
CHEMBL51454 1 7.23
CHEMBL299635 1 6.45
CHEMBL50886 1 5.99
CHEMBL50675 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311347 Ki = 0.96 nM 9.02
CHEMBL300511 Ki = 5.1 nM 8.29
CHEMBL301174 Ki = 9.54 nM 8.02
CHEMBL52334 Ki = 12.4 nM 7.91
CHEMBL296394 Ki = 13.2 nM 7.88
CHEMBL51896 Ki = 15.2 nM 7.82
CHEMBL50997 Ki = 19.1 nM 7.72
CHEMBL50674 Ki = 24.2 nM 7.62
CHEMBL51454 Ki = 58.7 nM 7.23
CHEMBL299635 Ki = 357.0 nM 6.45
CHEMBL50886 Ki = 1016.0 nM 5.99
CHEMBL50675 Ki > 3000.0 nM -