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Assay Detail

CHEMBL617280

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity using [3H]mesulergine as radioligand with receptor membranes isolated from a CHO-k cell line expressing the human 5-hydroxytryptamine 2C receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-k
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
Ki 15 6.62 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58009 1 7.75
CHEMBL303516 1 7.50
CHEMBL301466 1 7.24
CHEMBL61695 1 7.21
CHEMBL304013 1 7.08
CHEMBL291794 1 7.06
CHEMBL305123 1 7.04
CHEMBL60280 1 6.80
CHEMBL59631 1 6.62
CHEMBL60830 1 6.54
CHEMBL61771 1 6.43
CHEMBL59620 1 5.77
CHEMBL59807 1 5.75
CHEMBL59619 1 5.44
CHEMBL410512 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58009 Ki = 18.0 nM 7.75
CHEMBL303516 Ki = 32.0 nM 7.50
CHEMBL301466 Ki = 58.0 nM 7.24
CHEMBL61695 Ki = 61.0 nM 7.21
CHEMBL304013 Ki = 84.0 nM 7.08
CHEMBL291794 Ki = 88.0 nM 7.06
CHEMBL305123 Ki = 92.0 nM 7.04
CHEMBL60280 Ki = 160.0 nM 6.80
CHEMBL59631 Ki = 238.0 nM 6.62
CHEMBL60830 Ki = 285.0 nM 6.54
CHEMBL61771 Ki = 368.0 nM 6.43
CHEMBL59620 Ki = 1700.0 nM 5.77
CHEMBL59807 Ki = 1800.0 nM 5.75
CHEMBL59619 Ki = 3600.0 nM 5.44
CHEMBL410512 Ki = 9200.0 nM 5.04