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Assay Detail

CHEMBL616749

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

Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
11
Total Activities
11
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 1B (CHEMBL3459)
Type SINGLE PROTEIN
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 11 8.25 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26379 1 9.10
CHEMBL26378 1 8.92
CHEMBL26906 1 8.72
CHEMBL18785 RU-24969 1 8.70
CHEMBL27592 1 8.49
CHEMBL282994 1 8.48
CHEMBL283257 1 8.46
CHEMBL304008 1 7.82
CHEMBL28178 1 7.68
CHEMBL274866 1 7.57
CHEMBL27403 1 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26379 IC50 = 0.8 nM 9.10
CHEMBL26378 IC50 = 1.2 nM 8.92
CHEMBL26906 IC50 = 1.9 nM 8.72
CHEMBL18785 RU-24969 IC50 = 2.0 nM 8.70
CHEMBL27592 IC50 = 3.2 nM 8.49
CHEMBL282994 IC50 = 3.3 nM 8.48
CHEMBL283257 IC50 = 3.5 nM 8.46
CHEMBL304008 IC50 = 15.0 nM 7.82
CHEMBL28178 IC50 = 21.0 nM 7.68
CHEMBL274866 IC50 = 27.0 nM 7.57
CHEMBL27403 IC50 = 150.0 nM 6.82