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Assay Detail

CHEMBL4276609

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

Functional
Antagonist activity at serotonin human 5-HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay
2
Total Activities
2
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 and Biological Evaluation of Fused Tricyclic Heterocycle Piperazine (Piperidine) Derivatives As Potential Multireceptor Atypical Antipsychotics.
Cao X, Zhang Y, Chen Y, Qiu Y, Yu M, Xu X, Liu X, Liu BF, Zhang L, Zhang G.
J Med Chem (2018) 61 : 10017 -10039
PubMed 30383372 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.23 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.70
CHEMBL4293999 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE IC50 = 20.0 nM 7.70
CHEMBL4293999 IC50 = 177.6 nM 6.75