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Assay Detail

CHEMBL616499

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 2 receptor of rat anterior cortex using [3H]ketanserin as the radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 6 5.51 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274866 1 6.24
CHEMBL39 SEROTONIN 3.0 1 5.34
CHEMBL18785 RU-24969 1 5.27
CHEMBL27403 1 5.17
CHEMBL304008 1 -
CHEMBL28178 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274866 IC50 = 570.0 nM 6.24
CHEMBL39 SEROTONIN IC50 = 4600.0 nM 5.34
CHEMBL18785 RU-24969 IC50 = 5400.0 nM 5.27
CHEMBL27403 IC50 = 6800.0 nM 5.17
CHEMBL304008 IC50 > 10000.0 nM -
CHEMBL28178 IC50 > 10000.0 nM -