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Assay Detail

CHEMBL620654

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

Binding
Inhibition of [3H]-Q-ICS 205-930 binding to rat cortex homogenate 5-hydroxytryptamine 3 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Serotonin 3 (5-HT3) receptor (CHEMBL2094116)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

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 12 5.52 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52912 1 5.90
CHEMBL53485 1 5.90
CHEMBL53349 1 5.80
CHEMBL299213 1 5.60
CHEMBL298544 1 5.60
CHEMBL39243 1 5.60
CHEMBL53764 1 5.50
CHEMBL53467 1 5.50
CHEMBL53128 1 5.30
CHEMBL54265 1 5.00
CHEMBL52264 1 5.00
CHEMBL50834 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52912 IC50 = 1258.93 nM 5.90
CHEMBL53485 IC50 = 1258.93 nM 5.90
CHEMBL53349 IC50 = 1584.89 nM 5.80
CHEMBL299213 IC50 = 2511.89 nM 5.60
CHEMBL298544 IC50 = 2511.89 nM 5.60
CHEMBL39243 IC50 = 2511.89 nM 5.60
CHEMBL53764 IC50 = 3162.28 nM 5.50
CHEMBL53467 IC50 = 3162.28 nM 5.50
CHEMBL53128 IC50 = 5011.87 nM 5.30
CHEMBL54265 IC50 = 10000.0 nM 5.00
CHEMBL52264 IC50 = 10000.0 nM 5.00
CHEMBL50834 IC50 > 10000.0 nM -