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Assay Detail

CHEMBL805326

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

Binding
Displacement of [3H]paroxetine from serotonin transporter (SERT)
14
Total Activities
14
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 serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.
Lomenzo SA, Izenwasser S, Gerdes RM, Katz JL, Kopajtic T, Trudell ML.
Bioorg Med Chem Lett (1999) 9 : 3273 -3276
PubMed 10612583 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.38 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL419744 1 8.14
CHEMBL326243 1 7.72
CHEMBL113479 1 7.68
CHEMBL109386 1 6.90
CHEMBL113480 1 6.56
CHEMBL112817 1 6.51
CHEMBL607 MEPERIDINE 4.0 1 6.38
CHEMBL110967 1 6.37
CHEMBL113336 1 6.09
CHEMBL324465 1 5.99
CHEMBL323600 1 5.79
CHEMBL324886 1 5.29
CHEMBL324885 1 5.00
CHEMBL111498 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL419744 Ki = 7.2 nM 8.14
CHEMBL326243 Ki = 19.0 nM 7.72
CHEMBL113479 Ki = 21.0 nM 7.68
CHEMBL109386 Ki = 125.0 nM 6.90
CHEMBL113480 Ki = 277.0 nM 6.56
CHEMBL112817 Ki = 308.0 nM 6.51
CHEMBL607 MEPERIDINE Ki = 412.0 nM 6.38
CHEMBL110967 Ki = 430.0 nM 6.37
CHEMBL113336 Ki = 805.0 nM 6.09
CHEMBL324465 Ki = 1020.0 nM 5.99
CHEMBL323600 Ki = 1610.0 nM 5.79
CHEMBL324886 Ki = 5110.0 nM 5.29
CHEMBL324885 Ki = 10100.0 nM 5.00
CHEMBL111498 Ki = 13700.0 nM 4.86