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Assay Detail

CHEMBL805335

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

Binding
Binding affinity towards Serotonin transporter was determined in rat forebrain membrane
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Forebrain
Subcellular Membrane
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. 2. Molecular basis of the intrinsic efficacy of arylpiperazine derivatives at the central 5-HT3 receptors.
Cappelli A, Anzini M, Vomero S, Canullo L, Mennuni L, Makovec F, Doucet E, Hamon M, Menziani MC, De Benedetti PG, Bruni G, Romeo MR, Giorgi G, Donati A.
J Med Chem (1999) 42 : 1556 -1575
PubMed 10229626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.78 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41140 6-NITROQUIPAZINE 1 9.92
CHEMBL18772 QUIPAZINE 2.0 1 7.51
CHEMBL39 SEROTONIN 3.0 1 6.13
CHEMBL43304 1 5.96
CHEMBL43512 1 5.80
CHEMBL288069 1 5.34

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
CHEMBL39 SEROTONIN Ki = 740.0 nM 6.13
CHEMBL43304 Ki = 1100.0 nM 5.96
CHEMBL43512 Ki = 1600.0 nM 5.80
CHEMBL288069 Ki = 4600.0 nM 5.34