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Assay Detail

CHEMBL900203

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

Functional
Antagonist activity at human 5HT6 receptor expressed in HeLa cells assessed as cAMP production
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE.
J Med Chem (2007) 50 : 5535 -5538
PubMed 17948978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Imax 2 - -
IC50 2 7.89 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL238770 2 8.02
CHEMBL236988 2 7.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL238770 IC50 = 9.6 nM 8.02
CHEMBL236988 IC50 = 17.5 nM 7.76
CHEMBL236988 Imax = 80.5 % -
CHEMBL238770 Imax = 83.0 % -