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Assay Detail

CHEMBL2340916

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Binding
Agonist activity at 5-HT2C receptor (unknown origin)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.
Fevig JM, Feng J, Rossi KA, Miller KJ, Wu G, Hung CP, Ung T, Malmstrom SE, Zhang G, Keim WJ, Cullen MJ, Rohrbach KW, Qu Q, Gan J, Pelleymounter MA, Robl JA.
Bioorg Med Chem Lett (2013) 23 : 330 -335
PubMed 23177783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.95 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360328 LORCASERIN 4.0 1 8.05
CHEMBL2337102 1 6.78
CHEMBL2337103 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360328 LORCASERIN EC50 = 9.0 nM 8.05
CHEMBL2337102 EC50 = 168.0 nM 6.78
CHEMBL2337103 EC50 = 943.0 nM 6.03