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Assay Detail

CHEMBL806136

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

Binding
Ability to displace [3H]paroxetine bound to Serotonin transporter receptor in rat forebrain
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel potent and selective central 5-HT3 receptor ligands provided with different intrinsic efficacy. 1. Mapping the central 5-HT3 receptor binding site by arylpiperazine derivatives.
Cappelli A, Anzini M, Vomero S, Mennuni L, Makovec F, Doucet E, Hamon M, Bruni G, Romeo MR, Menziani MC, De Benedetti PG, Langer T.
J Med Chem (1998) 41 : 728 -741
PubMed 9513601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.72 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41140 6-NITROQUIPAZINE 1 9.92
CHEMBL18772 QUIPAZINE 2.0 1 7.51
CHEMBL352107 1 7.23
CHEMBL39 SEROTONIN 3.0 1 6.13
CHEMBL43355 1 4.92
CHEMBL287987 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41140 6-NITROQUIPAZINE Ki = 0.12 nM 9.92
CHEMBL18772 QUIPAZINE Ki = 31.0 nM 7.51
CHEMBL352107 Ki = 59.0 nM 7.23
CHEMBL39 SEROTONIN Ki = 740.0 nM 6.13
CHEMBL43355 Ki = 12000.0 nM 4.92
CHEMBL287987 Ki = 24000.0 nM 4.62