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Assay Detail

CHEMBL2396137

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Functional
Agonist activity at serotonin-activated human recombinant 5HT-2C receptor expressed in HEK293 cells assessed as increase in intracellular calcium level after 5 mins measured for 1 min by fluorescence assay
5
Total Activities
5
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 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel pyrimidoazepine analogs as serotonin 5-HT(2A) and 5-HT(2C) receptor ligands for the treatment of obesity.
Yang HY, Tae J, Seo YW, Kim YJ, Im HY, Choi GD, Cho H, Park WK, Kwon OS, Cho YS, Ko M, Jang H, Lee J, Choi K, Kim CH, Lee J, Pae AN.
Eur J Med Chem (2013) 63 : 558 -569
PubMed 23537943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.34 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL478 CHLOROPHENYLPIPERAZINE 2.0 1 8.09
CHEMBL2393233 1 5.92
CHEMBL2393235 1 5.02
CHEMBL2393236 1 -
CHEMBL2393232 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL478 CHLOROPHENYLPIPERAZINE EC50 = 8.1 nM 8.09
CHEMBL2393233 EC50 = 1200.0 nM 5.92
CHEMBL2393235 EC50 = 9600.0 nM 5.02
CHEMBL2393236 EC50 > 10000.0 nM -
CHEMBL2393232 EC50 > 10000.0 nM -