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Assay Detail

CHEMBL1293145

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

Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1B (CHEMBL1898)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Bromidge SM, Arban R, Bertani B, Borriello M, Capelli AM, Di-Fabio R, Faedo S, Gianotti M, Gordon LJ, Granci E, Pasquarello A, Spada SK, Worby A, Zonzini L, Zucchelli V.
Bioorg Med Chem Lett (2010) 20 : 7092 -7096
PubMed 20951584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.62 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1289048 1 7.20
CHEMBL1290596 1 6.70
CHEMBL1289164 1 6.50
CHEMBL1290597 1 6.40
CHEMBL1289047 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1289048 EC50 = 63.1 nM 7.20
CHEMBL1290596 EC50 = 199.53 nM 6.70
CHEMBL1289164 EC50 = 316.23 nM 6.50
CHEMBL1290597 EC50 = 398.11 nM 6.40
CHEMBL1289047 EC50 = 501.19 nM 6.30