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Assay Detail

CHEMBL1947490

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

Binding
Displacement of [3H]mesulergine from human 5HT2C receptor expressed in CHO cells after 60 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and pharmacological evaluation of new series of naphthalenic analogues as melatoninergic (MT1/MT2) and serotoninergic 5-HT2C dual ligands (I).
Ettaoussi M, Sabaouni A, Rami M, Boutin JA, Delagrange P, Renard P, Spedding M, Caignard DH, Berthelot P, Yous S.
Eur J Med Chem (2012) 49 : 310 -323
PubMed 22301214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.35 6.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946234 1 6.84
CHEMBL342432 1 6.41
CHEMBL10878 AGOMELATINE 4.0 1 6.15
CHEMBL1946233 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946234 Ki = 144.0 nM 6.84
CHEMBL342432 Ki = 391.0 nM 6.41
CHEMBL10878 AGOMELATINE Ki = 708.0 nM 6.15
CHEMBL1946233 Ki = 1000.0 nM 6.00