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Assay Detail

CHEMBL616270

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 alpha expressed in HEK 293 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

5-HT1D receptor agonist properties of novel 2-[5-[[(trifluoromethyl)sulfonyl]oxy]indolyl]ethylamines and their use as synthetic intermediates.
Barf TA, de Boer P, Wikström H, Peroutka SJ, Swensson K, Ennis MD, Ghazal NB, McGuire JC, Smith MW.
J Med Chem (1996) 39 : 4717 -4726
PubMed 8941384 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.82 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL357130 1 7.60
CHEMBL142629 1 7.11
CHEMBL143723 1 6.96
CHEMBL143745 1 6.33
CHEMBL141706 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL357130 IC50 = 25.0 nM 7.60
CHEMBL142629 IC50 = 77.0 nM 7.11
CHEMBL143723 IC50 = 110.0 nM 6.96
CHEMBL143745 IC50 = 470.0 nM 6.33
CHEMBL141706 IC50 = 820.0 nM 6.09