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Assay Detail

CHEMBL677556

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

Binding
Displacement of [3H]WIN-35428 binding to the dopamine transporter (DAT) in Rat Caudate Putamen
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

3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.
Kline RH, Izenwasser S, Katz JL, Joseph DB, Bowen WD, Newman AH.
J Med Chem (1997) 40 : 851 -857
PubMed 9083473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.95 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084870 1 7.67
CHEMBL310310 1 7.52
CHEMBL120901 1 7.50
CHEMBL3084909 1 7.32
CHEMBL3084869 1 7.30
CHEMBL3084907 1 7.16
CHEMBL1201203 BENZTROPINE 4.0 1 6.93
CHEMBL3084901 1 6.73
CHEMBL3084910 1 6.64
CHEMBL3084878 1 6.51
CHEMBL370805 COCAINE 4.0 1 6.41
CHEMBL3084891 AMINOBENZTROPINE 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084870 Ki = 21.6 nM 7.67
CHEMBL310310 Ki = 30.0 nM 7.52
CHEMBL120901 Ki = 32.0 nM 7.50
CHEMBL3084909 Ki = 47.4 nM 7.32
CHEMBL3084869 Ki = 50.0 nM 7.30
CHEMBL3084907 Ki = 68.5 nM 7.16
CHEMBL1201203 BENZTROPINE Ki = 118.0 nM 6.93
CHEMBL3084901 Ki = 187.0 nM 6.73
CHEMBL3084910 Ki = 228.0 nM 6.64
CHEMBL3084878 Ki = 309.0 nM 6.51
CHEMBL370805 COCAINE Ki = 388.0 nM 6.41
CHEMBL3084891 AMINOBENZTROPINE Ki = 1840.0 nM 5.74