Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET03NUC)
Name	Vanilloid receptor 2 (TrpV2)
Synonyms	Click to Show/Hide the Synonyms of This DBT Transient receptor potential cation channel subfamily V member 2; OTRPC2; Osm-9-like TRP channel 2; Stretch-activated channel 2B; TrpV2; VRL-1; Vanilloid receptor-like protein 1
Family	Transmembrane channel/porin (TC/P) >> Transient receptor potential Ca channel (TRP-CC)
Organism	Homo sapiens (Human)
Gene Name	TRPV2		Gene ID	51393
UniProt ID	TRPV2_HUMAN	(click to find more protein-related data of this DBT)
TTD ID	T82267	(click to find more therapeutic target data of this DBT)
	Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence	MTSPSSSPVFRLETLDGGQEDGSEADRGKLDFGSGLPPMESQFQGEDRKFAPQIRVNLNY RKGTGASQPDPNRFDRDRLFNAVSRGVPEDLAGLPEYLSKTSKYLTDSEYTEGSTGKTCL MKAVLNLKDGVNACILPLLQIDRDSGNPQPLVNAQCTDDYYRGHSALHIAIEKRSLQCVK LLVENGANVHARACGRFFQKGQGTCFYFGELPLSLAACTKQWDVVSYLLENPHQPASLQA TDSQGNTVLHALVMISDNSAENIALVTSMYDGLLQAGARLCPTVQLEDIRNLQDLTPLKL AAKEGKIEIFRHILQREFSGLSHLSRKFTEWCYGPVRVSLYDLASVDSCEENSVLEIIAF HCKSPHRHRMVVLEPLNKLLQAKWDLLIPKFFLNFLCNLIYMFIFTAVAYHQPTLKKQAA PHLKAEVGNSMLLTGHILILLGGIYLLVGQLWYFWRRHVFIWISFIDSYFEILFLFQALL TVVSQVLCFLAIEWYLPLLVSALVLGWLNLLYYTRGFQHTGIYSVMIQKVILRDLLRFLL IYLVFLFGFAVALVSLSQEAWRPEAPTGPNATESVQPMEGQEDEGNGAQYRGILEASLEL FKFTIGMGELAFQEQLHFRGMVLLLLLAYVLLTYILLLNMLIALMSETVNSVATDSWSIW KLQKAISVLEMENGYWWCRKKQRAGVMLTVGTKPDGSPDERWCFRVEEVNWASWEQTLPT LCEDPSGAGVPRTLENPVLASPPKEDEDGASEENYVPVQLLQSN
Function	Calcium-permeable, non-selective cation channel with an outward rectification. Seems to be regulated, at least in part, by growth factors, like IGF1, PDGF and morphogenetic neuropeptide/head activator. May transduce physical stimuli in mast cells. Activated by temperatures higher than 52 degrees Celsius; is not activated by vanilloids and acidic pH.

Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
DIG Name: Oleic acid		Click to Show/Hide
Detailed Information	DIG Info click to show the detail info of this DIG
Functional Class	Click to Show/Hide the Functional Class of This DIG Emulsifying agent; Penetration agent; Solubilizing agent
Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
Biological Activity	IC50 > 10000 nM (tested by experiment)		[1]
Tested Species	Rattus norvegicus (Rat)
UniProt ID	TRPV2_RAT
DIG Name: Palmitic acid		Click to Show/Hide
Detailed Information	DIG Info click to show the detail info of this DIG
Functional Class	Click to Show/Hide the Functional Class of This DIG Emulsifying agent; Penetration agent; lubricant
Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
Biological Activity	IC50 > 10000 nM (tested by experiment)		[1]
Tested Species	Rattus norvegicus (Rat)
UniProt ID	TRPV2_RAT
DIG Name: Sodium stearate		Click to Show/Hide
Detailed Information	DIG Info click to show the detail info of this DIG
Functional Class	Click to Show/Hide the Functional Class of This DIG Emulsifying agent; Gelling agent; Glidant; Modified-release agent; Stiffening agent; lubricant
Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
Biological Activity	IC50 > 10000 nM (estimated based on the structural similarity with CHEMBL1173381 )		[1]
Structural Similarity	Tanimoto coefficient = 1
Tested Species	Rattus norvegicus (Rat)
UniProt ID	TRPV2_RAT

References
1	Elongation of the Hydrophobic Chain as a Molecular Switch: Discovery of Capsaicin Derivatives and Endogenous Lipids as Potent Transient Receptor Potential Vanilloid Channel 2 Antagonists. J Med Chem. 2018 Sep 27; 61(18):8255-8281.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhang and Dr. Mou.