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Assay Detail

CHEMBL4617361

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Functional
Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method
1
Total Activities
1
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

Discovery of a lead series of potent benzodiazepine 5-HT<sub>2C</sub> receptor agonists with high selectivity in functional and binding assays.
Ren A, Zhu X, Feichtinger K, Lehman J, Kasem M, Schrader TO, Wong A, Dang H, Le M, Frazer J, Unett DJ, Grottick AJ, Whelan KT, Morgan ME, Sage CR, Semple G.
Bioorg Med Chem Lett (2020) 30 : 126929 -126929
PubMed 31952960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.12 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360328 LORCASERIN 4.0 1 8.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360328 LORCASERIN EC50 = 7.6 nM 8.12