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Assay Detail

CHEMBL616624

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

Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist.
Perez M, Pauwels PJ, Fourrier C, Chopin P, Valentin JP, John GW, Marien M, Halazy S.
Bioorg Med Chem Lett (1998) 8 : 675 -680
PubMed 9871581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.15 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158941 1 9.24
CHEMBL1185 ZOLMITRIPTAN 4.0 1 7.80
CHEMBL128 SUMATRIPTAN 4.0 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158941 EC50 = 0.58 nM 9.24
CHEMBL1185 ZOLMITRIPTAN EC50 = 15.7 nM 7.80
CHEMBL128 SUMATRIPTAN EC50 = 38.3 nM 7.42