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Assay Detail

CHEMBL805328

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

Binding
Binding affinity at serotonin transporter from rat caudate-putamen tissue by [3H]WIN-35428 displacement.
18
Total Activities
18
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 serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of dopamine transporter selective 3-[2-(diarylmethoxyethylidene)]-8-alkylaryl-8-azabicyclo[3.2.1]octanes.
Bradley AL, Izenwasser S, Wade D, Cararas S, Trudell ML.
Bioorg Med Chem Lett (2003) 13 : 629 -632
PubMed 12639545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.90 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3084919 1 6.76
CHEMBL443291 1 6.75
CHEMBL156286 1 6.43
CHEMBL348907 1 6.25
CHEMBL348583 1 6.19
CHEMBL3084920 1 6.12
CHEMBL160246 1 6.09
CHEMBL157259 1 6.08
CHEMBL157045 1 5.94
CHEMBL160857 1 5.87
CHEMBL157260 1 5.84
CHEMBL346995 1 5.71
CHEMBL157183 1 5.65
CHEMBL126235 1 5.61
CHEMBL160391 1 5.46
CHEMBL76603 1 5.32
CHEMBL349548 1 5.27
CHEMBL3084922 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3084919 Ki = 175.0 nM 6.76
CHEMBL443291 Ki = 177.0 nM 6.75
CHEMBL156286 Ki = 374.0 nM 6.43
CHEMBL348907 Ki = 562.0 nM 6.25
CHEMBL348583 Ki = 651.0 nM 6.19
CHEMBL3084920 Ki = 750.0 nM 6.12
CHEMBL160246 Ki = 809.0 nM 6.09
CHEMBL157259 Ki = 822.0 nM 6.08
CHEMBL157045 Ki = 1160.0 nM 5.94
CHEMBL160857 Ki = 1340.0 nM 5.87
CHEMBL157260 Ki = 1430.0 nM 5.84
CHEMBL346995 Ki = 1940.0 nM 5.71
CHEMBL157183 Ki = 2220.0 nM 5.65
CHEMBL126235 Ki = 2470.0 nM 5.61
CHEMBL160391 Ki = 3430.0 nM 5.46
CHEMBL76603 Ki = 4780.0 nM 5.32
CHEMBL349548 Ki = 5420.0 nM 5.27
CHEMBL3084922 Ki = 14100.0 nM 4.85