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Assay Detail

CHEMBL2340914

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Binding
Agonist activity at 5-HT2B 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 2B (CHEMBL1833)
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
Ki 3 8.19 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360328 LORCASERIN 4.0 1 8.89
CHEMBL2337102 1 7.85
CHEMBL2337103 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360328 LORCASERIN Ki = 1.3 nM 8.89
CHEMBL2337102 Ki = 14.0 nM 7.85
CHEMBL2337103 Ki = 15.0 nM 7.82