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Assay Detail

CHEMBL677369

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

Binding
Binding affinity towards dopamine transporter using [3H]-mazindol as radioligand in rat striatal membranes.
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

Chemistry and biology of the 2 beta-alkyl-3 beta-phenyl analogues of cocaine: subnanomolar affinity ligands that suggest a new pharmacophore model at the C-2 position.
Kozikowski AP, Eddine Saiah MK, Johnson KM, Bergmann JS.
J Med Chem (1995) 38 : 3086 -3093
PubMed 7636872 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.98 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL320427 1 9.85
CHEMBL107808 1 9.66
CHEMBL106627 1 9.51
CHEMBL28394 1 9.38
CHEMBL281288 1 9.23
CHEMBL610897 1 9.08
CHEMBL321888 1 9.03
CHEMBL432401 1 8.92
CHEMBL104567 1 8.84
CHEMBL420291 1 8.73
CHEMBL27336 1 8.66
CHEMBL322365 1 6.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL320427 Ki = 0.14 nM 9.85
CHEMBL107808 Ki = 0.22 nM 9.66
CHEMBL106627 Ki = 0.31 nM 9.51
CHEMBL28394 Ki = 0.42 nM 9.38
CHEMBL281288 Ki = 0.59 nM 9.23
CHEMBL610897 Ki = 0.83 nM 9.08
CHEMBL321888 Ki = 0.94 nM 9.03
CHEMBL432401 Ki = 1.21 nM 8.92
CHEMBL104567 Ki = 1.46 nM 8.84
CHEMBL420291 Ki = 1.87 nM 8.73
CHEMBL27336 Ki = 2.17 nM 8.66
CHEMBL322365 Ki = 155.7 nM 6.81