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Assay Detail

CHEMBL616669

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

Functional
Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor
8
Total Activities
8
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 Expert

Target

5-hydroxytryptamine receptor 1D (CHEMBL1983)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-(Piperazinylpropyl)indoles: selective, orally bioavailable h5-HT1D receptor agonists as potential antimigraine agents.
Chambers MS, Street LJ, Goodacre S, Hobbs SC, Hunt P, Jelley RA, Matassa VG, Reeve AJ, Sternfeld F, Beer MS, Stanton JA, Rathbone D, Watt AP, MacLeod AM.
J Med Chem (1999) 42 : 691 -705
PubMed 10052976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 8 8.20 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296161 1 9.40
CHEMBL420965 1 9.10
CHEMBL116092 1 8.64
CHEMBL163462 1 8.42
CHEMBL163376 1 7.96
CHEMBL128 SUMATRIPTAN 4.0 1 7.85
CHEMBL117249 1 7.27
CHEMBL324931 1 6.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296161 EC50 = 0.4 nM 9.40
CHEMBL420965 EC50 = 0.8 nM 9.10
CHEMBL116092 EC50 = 2.3 nM 8.64
CHEMBL163462 EC50 = 3.8 nM 8.42
CHEMBL163376 EC50 = 11.0 nM 7.96
CHEMBL128 SUMATRIPTAN EC50 = 14.0 nM 7.85
CHEMBL117249 EC50 = 54.0 nM 7.27
CHEMBL324931 EC50 = 105.0 nM 6.98