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Assay Detail

CHEMBL1049519

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Functional
Agonist activity at human TRPA1 expressed in HEK293 cells assessed as [45]Ca2+ influx by microbeta plate count
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Oxime derivatives related to AP18: Agonists and antagonists of the TRPA1 receptor.
Defalco J, Steiger D, Gustafson A, Emerling DE, Kelly MG, Duncton MA.
Bioorg Med Chem Lett (2010) 20 : 276 -279
PubMed 19945872 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 4.52 5.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL589866 1 5.03
CHEMBL590847 1 4.94
CHEMBL589870 1 4.84
CHEMBL590846 1 4.80
CHEMBL589871 1 4.56
CHEMBL594133 1 4.34
CHEMBL293492 CINNAMALDEHYDE -1.0 1 4.29
CHEMBL589875 1 4.20
CHEMBL589873 1 4.16
CHEMBL589794 1 4.01
CHEMBL602101 1 -
CHEMBL590119 1 -
CHEMBL590118 1 -
CHEMBL603735 1 -
CHEMBL593903 1 -
CHEMBL590845 1 -
CHEMBL594134 1 -
CHEMBL589872 1 -
CHEMBL589874 1 -
CHEMBL593902 AP18 5 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL589866 EC50 = 9400.0 nM 5.03
CHEMBL590847 EC50 = 11500.0 nM 4.94
CHEMBL589870 EC50 = 14400.0 nM 4.84
CHEMBL590846 EC50 = 15900.0 nM 4.80
CHEMBL589871 EC50 = 27600.0 nM 4.56
CHEMBL594133 EC50 = 46100.0 nM 4.34
CHEMBL293492 CINNAMALDEHYDE EC50 = 51400.0 nM 4.29
CHEMBL589875 EC50 = 63100.0 nM 4.20
CHEMBL589873 EC50 = 69400.0 nM 4.16
CHEMBL589794 EC50 = 96600.0 nM 4.01
CHEMBL602101 EC50 - -
CHEMBL590119 EC50 - -
CHEMBL590118 EC50 - -
CHEMBL603735 EC50 - -
CHEMBL593903 EC50 - -
CHEMBL590845 EC50 - -
CHEMBL594134 EC50 - -
CHEMBL589872 EC50 - -
CHEMBL589874 EC50 - -
CHEMBL593902 AP18 5 EC50 - -