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Assay Detail

CHEMBL1040066

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

Functional
Antagonist activity at mouse 5HT6 receptor C3.36A mutant expressed in COS7 cells assessed as inhibition of serotonin-induced cAMP accumulation by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL1075268)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation.
de la Fuente T, Martín-Fontecha M, Sallander J, Benhamú B, Campillo M, Medina RA, Pellissier LP, Claeysen S, Dumuis A, Pardo L, López-Rodríguez ML.
J Med Chem (2010) 53 : 1357 -1369
PubMed 20078106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.37 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL584690 1 7.47
CHEMBL60264 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL584690 Ki = 34.0 nM 7.47
CHEMBL60264 Ki = 54.0 nM 7.27