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Assay Detail

CHEMBL617882

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Functional
Agonistic activity for 5-HT2c (5-HT2C) by measuring [3H]inositol monophosphate fromation in CHO cells in which the human 5-HT2C receptor subtype was stably expressed
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Synthesis and 5-hydroxytryptamine (5-HT) activity of 2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5-(6H)ones and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a]quinoxalines.
Welmaker GS, Nelson JA, Sabalski JE, Sabb AL, Potoski JR, Graziano D, Kagan M, Coupet J, Dunlop J, Mazandarani H, Rosenzweig-Lipson S, Sukoff S, Zhang Y.
Bioorg Med Chem Lett (2000) 10 : 1991 -1994
PubMed 10987434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.30 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58009 1 8.12
CHEMBL303516 1 8.10
CHEMBL301466 1 7.92
CHEMBL60280 1 7.72
CHEMBL305123 1 7.72
CHEMBL61695 1 7.35
CHEMBL291794 1 7.31
CHEMBL59631 1 7.07
CHEMBL304013 1 6.87
CHEMBL60830 1 6.54
CHEMBL59619 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58009 EC50 = 7.6 nM 8.12
CHEMBL303516 EC50 = 8.0 nM 8.10
CHEMBL301466 EC50 = 12.0 nM 7.92
CHEMBL60280 EC50 = 19.0 nM 7.72
CHEMBL305123 EC50 = 19.0 nM 7.72
CHEMBL61695 EC50 = 45.0 nM 7.35
CHEMBL291794 EC50 = 49.0 nM 7.31
CHEMBL59631 EC50 = 86.0 nM 7.07
CHEMBL304013 EC50 = 136.0 nM 6.87
CHEMBL60830 EC50 = 290.0 nM 6.54
CHEMBL59619 EC50 = 2600.0 nM 5.58