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Assay Detail

CHEMBL678930

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

Binding
Binding affinity for dopamine transporter was determined in vitro in rat brain using [3H]WIN-35428 s radioligand
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Structure-activity relationships at monoamine transporters and muscarinic receptors for N-substituted-3alpha-(3'-chloro-, 4'-chloro-, and 4',4''-dichloro-substituted-diphenyl)methoxytropanes.
Newman AH, Robarge MJ, Howard IM, Wittkopp SL, George C, Kopajtic T, Izenwasser S, Katz JL.
J Med Chem (2001) 44 : 633 -640
PubMed 11170654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.13 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084884 1 7.70
CHEMBL3084870 1 7.67
CHEMBL559215 1 7.58
CHEMBL310310 1 7.52
CHEMBL543231 1 7.47
CHEMBL539821 1 7.43
CHEMBL3084608 1 7.27
CHEMBL545574 1 7.26
CHEMBL539829 1 7.21
CHEMBL545342 1 7.08
CHEMBL3084607 1 7.07
CHEMBL3084621 1 7.00
CHEMBL3084609 1 6.83
CHEMBL542275 1 6.82
CHEMBL3084623 1 6.80
CHEMBL542521 1 6.72
CHEMBL544177 1 6.44
CHEMBL541612 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084884 Ki = 20.0 nM 7.70
CHEMBL3084870 Ki = 21.6 nM 7.67
CHEMBL559215 Ki = 26.2 nM 7.58
CHEMBL310310 Ki = 30.0 nM 7.52
CHEMBL543231 Ki = 33.6 nM 7.47
CHEMBL539821 Ki = 36.8 nM 7.43
CHEMBL3084608 Ki = 53.3 nM 7.27
CHEMBL545574 Ki = 54.6 nM 7.26
CHEMBL539829 Ki = 61.7 nM 7.21
CHEMBL545342 Ki = 84.2 nM 7.08
CHEMBL3084607 Ki = 85.0 nM 7.07
CHEMBL3084621 Ki = 101.0 nM 7.00
CHEMBL3084609 Ki = 148.0 nM 6.83
CHEMBL542275 Ki = 153.0 nM 6.82
CHEMBL3084623 Ki = 158.0 nM 6.80
CHEMBL542521 Ki = 191.0 nM 6.72
CHEMBL544177 Ki = 365.0 nM 6.44
CHEMBL541612 Ki = 399.0 nM 6.40