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Assay Detail

CHEMBL616129

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

Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
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
Ki 3 7.02 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158941 1 7.75
CHEMBL1185 ZOLMITRIPTAN 4.0 1 6.91
CHEMBL128 SUMATRIPTAN 4.0 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158941 Ki = 17.7 nM 7.75
CHEMBL1185 ZOLMITRIPTAN Ki = 124.0 nM 6.91
CHEMBL128 SUMATRIPTAN Ki = 407.1 nM 6.39