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Assay Detail

CHEMBL615927

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

Binding
Displacement of [3H]8-OH-DPAT from rat cortex 5-hydroxytryptamine 1A receptor
13
Total Activities
13
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 1A (CHEMBL273)
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 13 7.33 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 8.28
CHEMBL27592 1 7.89
CHEMBL18785 RU-24969 1 7.85
CHEMBL27403 1 7.72
CHEMBL282994 1 7.58
CHEMBL26378 1 7.52
CHEMBL26379 1 7.50
CHEMBL283257 1 7.44
CHEMBL28178 1 7.43
CHEMBL26906 1 7.19
CHEMBL27811 1 6.85
CHEMBL274866 1 6.54
CHEMBL304008 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN IC50 = 5.2 nM 8.28
CHEMBL27592 IC50 = 13.0 nM 7.89
CHEMBL18785 RU-24969 IC50 = 14.0 nM 7.85
CHEMBL27403 IC50 = 19.0 nM 7.72
CHEMBL282994 IC50 = 26.0 nM 7.58
CHEMBL26378 IC50 = 30.0 nM 7.52
CHEMBL26379 IC50 = 32.0 nM 7.50
CHEMBL283257 IC50 = 36.0 nM 7.44
CHEMBL28178 IC50 = 37.0 nM 7.43
CHEMBL26906 IC50 = 65.0 nM 7.19
CHEMBL27811 IC50 = 140.0 nM 6.85
CHEMBL274866 IC50 = 290.0 nM 6.54
CHEMBL304008 IC50 = 3000.0 nM 5.52