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Assay Detail

CHEMBL677550

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

Binding
Displacement of [3H]WIN-35428 from the dopamine transporter in rat caudate putamen
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Caudate-putamen
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Highly selective chiral N-substituted 3alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues for the dopamine transporter: synthesis and comparative molecular field analysis.
Robarge MJ, Agoston GE, Izenwasser S, Kopajtic T, George C, Katz JL, Newman AH.
J Med Chem (2000) 43 : 1085 -1093
PubMed 10737741 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.24 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2308105 1 8.07
CHEMBL11776 1 7.95
CHEMBL317757 DIFLUOROBENZTROPINE 1 7.93
CHEMBL3085021 1 7.86
CHEMBL3084934 1 7.70
CHEMBL11493 1 7.61
CHEMBL275802 1 7.53
CHEMBL3084929 1 7.53
CHEMBL417249 1 7.52
CHEMBL12377 1 7.50
CHEMBL440272 1 7.49
CHEMBL12227 1 7.38
CHEMBL3085022 1 7.35
CHEMBL429015 1 7.25
CHEMBL12619 1 7.24
CHEMBL11497 1 7.22
CHEMBL12375 1 7.08
CHEMBL275979 1 7.06
CHEMBL11768 1 7.02
CHEMBL1907641 1 6.64
CHEMBL1907826 1 6.52
CHEMBL12004 1 6.43
CHEMBL267562 1 6.41
CHEMBL1907825 1 6.40
CHEMBL1907642 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2308105 Ki = 8.51 nM 8.07
CHEMBL11776 Ki = 11.2 nM 7.95
CHEMBL317757 DIFLUOROBENZTROPINE Ki = 11.8 nM 7.93
CHEMBL3085021 Ki = 13.9 nM 7.86
CHEMBL3084934 Ki = 20.2 nM 7.70
CHEMBL11493 Ki = 24.6 nM 7.61
CHEMBL275802 Ki = 29.5 nM 7.53
CHEMBL3084929 Ki = 29.7 nM 7.53
CHEMBL417249 Ki = 29.9 nM 7.52
CHEMBL12377 Ki = 31.9 nM 7.50
CHEMBL440272 Ki = 32.4 nM 7.49
CHEMBL12227 Ki = 41.9 nM 7.38
CHEMBL3085022 Ki = 44.6 nM 7.35
CHEMBL429015 Ki = 56.4 nM 7.25
CHEMBL12619 Ki = 57.0 nM 7.24
CHEMBL11497 Ki = 60.7 nM 7.22
CHEMBL12375 Ki = 82.2 nM 7.08
CHEMBL275979 Ki = 86.4 nM 7.06
CHEMBL11768 Ki = 95.6 nM 7.02
CHEMBL1907641 Ki = 228.0 nM 6.64
CHEMBL1907826 Ki = 301.0 nM 6.52
CHEMBL12004 Ki = 367.0 nM 6.43
CHEMBL267562 Ki = 392.0 nM 6.41
CHEMBL1907825 Ki = 400.0 nM 6.40
CHEMBL1907642 Ki = 477.0 nM 6.32