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Assay Detail

CHEMBL921967

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Functional
Agonist activity at human cloned 5HT2B receptor expressed in HEK293-EBNA cells assessed as myo-[3H]inositol hydrolysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293-EBNA
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2B (CHEMBL1833)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of a series of substituted 2-(1H-furo[2,3-g]indazol-1-yl)ethylamine derivatives as 5-HT2C receptor agonists.
Shimada I, Maeno K, Kazuta K, Kubota H, Kimizuka T, Kimura Y, Hatanaka K, Naitou Y, Wanibuchi F, Sakamoto S, Tsukamoto S.
Bioorg Med Chem (2008) 16 : 1966 -1982
PubMed 18035544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.10 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76781 1 8.62
CHEMBL407909 1 8.49
CHEMBL39 SEROTONIN 3.0 1 8.24
CHEMBL272942 MECOPROP 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76781 EC50 = 2.4 nM 8.62
CHEMBL407909 EC50 = 3.2 nM 8.49
CHEMBL39 SEROTONIN EC50 = 5.8 nM 8.24
CHEMBL272942 MECOPROP EC50 = 93.0 nM 7.03