Assay Detail

CHEMBL5680880

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Binding

Antagonist activity at GFP-tagged human TRPA1 transfected in HEK293F cells assessed as reduction in AITC-induced inward current at -60 mV holding potential by electrophysiological recordings

ChEMBL ↗

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Target

Transient receptor potential cation channel subfamily A member 1 (CHEMBL6007) ↗

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Transient receptor potential cation channel subfamily A member 1 (CHEMBL6007) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Transient receptor potential cation channel subfamily A member 1

CHEMBL6007

Anchored from Assay target.

Protein identity Transient receptor potential cation channel subfamily A member 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Transient receptor potential cation channel subfamily A member 1 (CHEMBL6007) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation.

Chen J, Joshi SK, DiDomenico S, Perner RJ, Mikusa JP, Gauvin DM, Segreti JA, Han P, Zhang XF, Niforatos W, Bianchi BR, Baker SJ, Zhong C, Simler GH, McDonald HA, Schmidt RG, McGaraughty SP, Chu KL, Faltynek CR, Kort ME, Reilly RM, Kym PR.
Pain (2011) 152 : 1165 -1172
PubMed 21402443 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.29	7.29
Activity	1	-	-

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	HP:0012531
EFO_ID	EFO_ID	-	—	EFO:1001905
EFO_ID	EFO_ID	-	—	MP:0001845
EFO_TERM	EFO_TERM	-	—	pain
EFO_TERM	EFO_TERM	-	—	oxidative stress
EFO_TERM	EFO_TERM	-	—	inflammation

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3697701	A-079	—	2	7.29

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3697701	A-079	IC50	=	51.0	nM	7.29
CHEMBL3697701	A-079	Activity		-	—	-