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Assay Detail

CHEMBL616901

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

Binding
Ability to displace [3H]-5-HT from recombinant human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells determined in vitro
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines: selective h5-HT1D agonists for the treatment of migraine.
Bourrain S, Neduvelil JG, Beer MS, Stanton JA, Showell GA, MacLeod AM.
Bioorg Med Chem Lett (1999) 9 : 3369 -3374
PubMed 10612601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.74 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112507 1 10.00
CHEMBL326125 1 9.35
CHEMBL116161 1 9.19
CHEMBL331819 1 9.19
CHEMBL111899 1 8.92
CHEMBL114877 1 8.92
CHEMBL114303 1 8.89
CHEMBL115989 1 8.87
CHEMBL115352 1 8.74
CHEMBL112558 1 8.49
CHEMBL324751 1 8.40
CHEMBL331143 1 8.35
CHEMBL113831 1 8.14
CHEMBL326723 1 7.96
CHEMBL115496 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112507 IC50 = 0.1 nM 10.00
CHEMBL326125 IC50 = 0.45 nM 9.35
CHEMBL116161 IC50 = 0.65 nM 9.19
CHEMBL331819 IC50 = 0.65 nM 9.19
CHEMBL111899 IC50 = 1.2 nM 8.92
CHEMBL114877 IC50 = 1.2 nM 8.92
CHEMBL114303 IC50 = 1.3 nM 8.89
CHEMBL115989 IC50 = 1.35 nM 8.87
CHEMBL115352 IC50 = 1.8 nM 8.74
CHEMBL112558 IC50 = 3.2 nM 8.49
CHEMBL324751 IC50 = 4.0 nM 8.40
CHEMBL331143 IC50 = 4.5 nM 8.35
CHEMBL113831 IC50 = 7.3 nM 8.14
CHEMBL326723 IC50 = 11.0 nM 7.96
CHEMBL115496 IC50 = 21.0 nM 7.68