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Assay Detail

CHEMBL616903

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

Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.
MacLeod AM, Street LJ, Reeve AJ, Jelley RA, Sternfeld F, Beer MS, Stanton JA, Watt AP, Rathbone D, Matassa VG.
J Med Chem (1997) 40 : 3501 -3503
PubMed 9357515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.69 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65367 1 9.70
CHEMBL292779 1 9.22
CHEMBL116031 1 9.22
CHEMBL116153 1 9.15
CHEMBL115750 1 9.10
CHEMBL119668 1 9.00
CHEMBL119785 1 8.89
CHEMBL117633 1 8.85
CHEMBL333089 1 8.74
CHEMBL116092 1 8.47
CHEMBL128 SUMATRIPTAN 4.0 1 8.30
CHEMBL117249 1 7.46
CHEMBL324931 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65367 IC50 = 0.2 nM 9.70
CHEMBL292779 IC50 = 0.6 nM 9.22
CHEMBL116031 IC50 = 0.6 nM 9.22
CHEMBL116153 IC50 = 0.7 nM 9.15
CHEMBL115750 IC50 = 0.8 nM 9.10
CHEMBL119668 IC50 = 1.0 nM 9.00
CHEMBL119785 IC50 = 1.3 nM 8.89
CHEMBL117633 IC50 = 1.4 nM 8.85
CHEMBL333089 IC50 = 1.8 nM 8.74
CHEMBL116092 IC50 = 3.4 nM 8.47
CHEMBL128 SUMATRIPTAN IC50 = 5.0 nM 8.30
CHEMBL117249 IC50 = 35.0 nM 7.46
CHEMBL324931 IC50 = 140.0 nM 6.85