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Assay Detail

CHEMBL617838

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

Binding
Inhibition of radiolabeled [3H]mesulergine ligand binding to 5-hydroxytryptamine 2C receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL324)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel and highly potent 5-HT3 receptor agonists based on a pyrroloquinoxaline structure.
Campiani G, Cappelli A, Nacci V, Anzini M, Vomero S, Hamon M, Cagnotto A, Fracasso C, Uboldi C, Caccia S, Consolo S, Mennini T.
J Med Chem (1997) 40 : 3670 -3678
PubMed 9357534 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.31 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 7.38
CHEMBL341474 1 6.38
CHEMBL18772 QUIPAZINE 2.0 1 6.33
CHEMBL327197 1 6.11
CHEMBL331304 1 6.11
CHEMBL120216 1 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN IC50 = 42.0 nM 7.38
CHEMBL341474 IC50 = 413.0 nM 6.38
CHEMBL18772 QUIPAZINE IC50 = 470.0 nM 6.33
CHEMBL327197 IC50 = 780.0 nM 6.11
CHEMBL331304 IC50 = 784.0 nM 6.11
CHEMBL120216 IC50 = 2803.0 nM 5.55