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Assay Detail

CHEMBL616815

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

Binding
Compound was evaluated for its inhibitory activity against 5-hydroxytryptamine 1C receptor of pig choroid plexus using [3H]mesulergine as the radioligand
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

3-(1,2,5,6-Tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one: a potent and selective serotonin (5-HT1B) agonist and rotationally restricted phenolic analogue of 5-methoxy-3-(1,2,5,6-tetrahydropyrid-4-yl)indole.
Macor JE, Burkhart CA, Heym JH, Ives JL, Lebel LA, Newman ME, Nielsen JA, Ryan K, Schulz DW, Torgersen LK.
J Med Chem (1990) 33 : 2087 -2093
PubMed 2374139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.89 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274866 1 6.82
CHEMBL18785 RU-24969 1 6.54
CHEMBL304008 1 5.19
CHEMBL28178 1 5.00
CHEMBL27403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274866 IC50 = 150.0 nM 6.82
CHEMBL18785 RU-24969 IC50 = 290.0 nM 6.54
CHEMBL304008 IC50 = 6400.0 nM 5.19
CHEMBL28178 IC50 = 10000.0 nM 5.00
CHEMBL27403 IC50 > 10000.0 nM -