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Assay Detail

CHEMBL3095672

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

Binding
Antagonist activity at human 5-HT2B receptor expressed in HEK293 cells coexpressing EBNA assessed as inhibition of 5-HT-induced IP metabolism incubated for 20 mins prior to substrate addition measured after 20 mins by liquid scintillation counting analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of new carbonyl guanidine derivatives as novel dual 5-HT2B and 5-HT7 receptor antagonists.
Moritomo A, Yamada H, Watanabe T, Itahana H, Akuzawa S, Okada M, Ohta M.
Bioorg Med Chem (2013) 21 : 7841 -7852
PubMed 24189186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.58 7.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092759 1 7.71
CHEMBL3092753 1 7.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092759 IC50 = 19.6 nM 7.71
CHEMBL3092753 IC50 = 36.4 nM 7.44