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Assay Detail

CHEMBL616400

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

Binding
Binding activity against 5-hydroxytryptamine 1A receptor from pig cortex membrane using [3H]8-OH-DPAT-HT as radioligand.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.
Street LJ, Baker R, Davey WB, Guiblin AR, Jelley RA, Reeve AJ, Routledge H, Sternfeld F, Watt AP, Beer MS.
J Med Chem (1995) 38 : 1799 -1810
PubMed 7752204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.73 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54265 1 7.60
CHEMBL300209 1 7.20
CHEMBL53764 1 7.20
CHEMBL50837 1 6.90
CHEMBL52912 1 6.80
CHEMBL53485 1 6.80
CHEMBL53128 1 6.70
CHEMBL53467 1 6.70
CHEMBL54103 1 6.50
CHEMBL52264 1 6.50
CHEMBL50834 1 6.50
CHEMBL53349 1 6.50
CHEMBL39243 1 6.50
CHEMBL299213 1 6.30
CHEMBL298544 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54265 IC50 = 25.12 nM 7.60
CHEMBL300209 IC50 = 63.1 nM 7.20
CHEMBL53764 IC50 = 63.1 nM 7.20
CHEMBL50837 IC50 = 125.89 nM 6.90
CHEMBL52912 IC50 = 158.49 nM 6.80
CHEMBL53485 IC50 = 158.49 nM 6.80
CHEMBL53128 IC50 = 199.53 nM 6.70
CHEMBL53467 IC50 = 199.53 nM 6.70
CHEMBL54103 IC50 = 316.23 nM 6.50
CHEMBL52264 IC50 = 316.23 nM 6.50
CHEMBL50834 IC50 = 316.23 nM 6.50
CHEMBL53349 IC50 = 316.23 nM 6.50
CHEMBL39243 IC50 = 316.23 nM 6.50
CHEMBL299213 IC50 = 501.19 nM 6.30
CHEMBL298544 IC50 = 630.96 nM 6.20