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Assay Detail

CHEMBL805338

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

Binding
Binding affinity towards serotonin transporter 5-HTT was determined using [3H]paroxetine radioligand.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes.
Carroll FI, Pawlush N, Kuhar MJ, Pollard GT, Howard JL.
J Med Chem (2004) 47 : 296 -302
PubMed 14711303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.40 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103523 1 8.09
CHEMBL317905 1 7.42
CHEMBL370805 COCAINE 4.0 1 7.35
CHEMBL316528 1 7.28
CHEMBL1790051 1 6.74
CHEMBL321780 1 6.68
CHEMBL103227 1 6.55
CHEMBL298580 1 6.52
CHEMBL103228 1 6.46
CHEMBL322856 1 6.44
CHEMBL316585 1 6.33
CHEMBL322385 1 6.28
CHEMBL320627 1 6.27
CHEMBL317904 1 6.24
CHEMBL329517 1 6.18
CHEMBL321806 1 5.94
CHEMBL14144 1 5.75
CHEMBL100652 1 5.47
CHEMBL322400 1 5.41
CHEMBL317909 1 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103523 Ki = 8.2 nM 8.09
CHEMBL317905 Ki = 38.0 nM 7.42
CHEMBL370805 COCAINE Ki = 45.0 nM 7.35
CHEMBL316528 Ki = 52.0 nM 7.28
CHEMBL1790051 Ki = 182.0 nM 6.74
CHEMBL321780 Ki = 211.0 nM 6.68
CHEMBL103227 Ki = 281.0 nM 6.55
CHEMBL298580 Ki = 305.0 nM 6.52
CHEMBL103228 Ki = 348.0 nM 6.46
CHEMBL322856 Ki = 366.0 nM 6.44
CHEMBL316585 Ki = 465.0 nM 6.33
CHEMBL322385 Ki = 522.0 nM 6.28
CHEMBL320627 Ki = 535.0 nM 6.27
CHEMBL317904 Ki = 582.0 nM 6.24
CHEMBL329517 Ki = 660.0 nM 6.18
CHEMBL321806 Ki = 1160.0 nM 5.94
CHEMBL14144 Ki = 1780.0 nM 5.75
CHEMBL100652 Ki = 3350.0 nM 5.47
CHEMBL322400 Ki = 3900.0 nM 5.41
CHEMBL317909 Ki = 26000.0 nM 4.58