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Assay Detail

CHEMBL2416142

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

Functional
Antagonist activity at recombinant human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux incubated for 30 mins prior to serotonin challenge measured after 4 mins by FLIPR assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of substituted diphenyl sulfones and their structure-activity relationship with the antagonism of 5-НТ6 receptors.
Ivachtchenko A, Golovina E, Kadieva M, Mitkin O, Tkachenko S, Okun I.
Bioorg Med Chem (2013) 21 : 4614 -4627
PubMed 23787290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355905 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355905 IC50 = 4.0 nM 8.40