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Assay Detail

CHEMBL5708946

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

Binding
Antagonist activity at full length rhesus monkey TRPA1 transfected in HEK293F cells assessed as blockade of MO-induced TRPA1 channel activation by measuring Ca2+ influx in presence of 120 uM MO by FLIPR calcium assay
6
Total Activities
6
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Cell Type HEK293F
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Species comparison and pharmacological characterization of human, monkey, rat, and mouse TRPA1 channels.
Bianchi BR, Zhang XF, Reilly RM, Kym PR, Yao BB, Chen J.
J Pharmacol Exp Ther (2012) 341 : 360 -368
PubMed 22319196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.30 6.22

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - HP:0012531
EFO_ID EFO_ID - HP:0002099
EFO_TERM EFO_TERM - pain
EFO_TERM EFO_TERM - asthma

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3697701 A-079 1 6.22
CHEMBL1086589 1 5.57
CHEMBL1086310 1 5.14
CHEMBL593902 AP18 5 1 4.25
CHEMBL256087 MENTHOL 4.0 1 -
CHEMBL113 CAFFEINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3697701 A-079 IC50 = 600.0 nM 6.22
CHEMBL1086589 IC50 = 2700.0 nM 5.57
CHEMBL1086310 IC50 = 7300.0 nM 5.14
CHEMBL593902 AP18 5 IC50 = 56400.0 nM 4.25
CHEMBL256087 MENTHOL IC50 > 1000000.0 nM -
CHEMBL113 CAFFEINE IC50 > 1000000.0 nM -