Reaction Details
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Transient receptor potential cation channel subfamily V member 2
Ligand
BDBM50463958
Substrate
n/a
Meas. Tech.
ChEMBL_1779721 (CHEMBL4236713)
IC50
1400±n/a nM
Citation
Schiano Moriello, A; López Chinarro, S; Novo Fernández, O; Eras, J; Amodeo, P; Canela-Garayoa, R; Vitale, RM; Di Marzo, V; De Petrocellis, L 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 61:8255-8281 (2018) [PubMed] Article More Info.:
Target
Name:
Transient receptor potential cation channel subfamily V member 2
Synonyms:
Sac2b | TRPV2_RAT | Transient receptor potential cation channel subfamily V member 2 | Trpv2 | Vanilloid receptor | Vrl1
Type:
PROTEIN
Mol. Mass.:
86707.60
Organism:
Rattus norvegicus
Description:
ChEMBL_768011
Residue:
761
Sequence:
MTSASSPPAFRLETSDGDEEGNAEVNKGKQEPPPMESPFQREDRNSSPQIKVNLNFIKRPPKNTSAPSQQEPDRFDRDRLFSVVSRGVPEELTGLLEYLRWNSKYLTDSAYTEGSTGKTCLMKAVLNLQDGVNACIMPLLQIDKDSGNPKLLVNAQCTDEFYQGHSALHIAIEKRSLQCVKLLVENGADVHLRACGRFFQKHQGTCFYFGELPLSLAACTKQWDVVTYLLENPHQPASLEATDSLGNTVLHALVMIADNSPENSALVIHMYDGLLQMGARLCPTVQLEEISNHQGLTPLKLAAKEGKIEIFRHILQREFSGPYQPLSRKFTEWCYGPVRVSLYDLSSVDSWEKNSVLEIIAFHCKSPNRHRMVVLEPLNKLLQEKWDRLVSRFFFNFACYLVYMFIFTVVAYHQPSLDQPAIPSSKATFGESMLLLGHILILLGGIYLLLGQLWYFWRRRLFIWISFMDSYFEILFLLQALLTVLSQVLRFMETEWYLPLLVLSLVLGWLNLLYYTRGFQHTGIYSVMIQKVILRDLLRFLLVYLVFLFGFAVALVSLSREARSPKAPEDNNSTVTEQPTVGQEEEPAPYRSILDASLELFKFTIGMGELAFQEQLRFRGVVLLLLLAYVLLTYVLLLNMLIALMSETVNHVADNSWSIWKLQKAISVLEMENGYWWCRRKKHREGRLLKVGTRGDGTPDERWCFRVEEVNWAAWEKTLPTLSEDPSGPGITGNKKNPTSKPGKNSASEEDHLPLQVLQSP
Inhibitor
Name:
BDBM50463958
Synonyms:
CHEMBL4246820
Type:
Small organic molecule
Emp. Form.:
C29H47NO3Se
Mol. Mass.:
536.65
SMILES:
[#6]-[#6]-[#6]-[#6]-[#6]\[#6]=[#6]/[#6]\[#6]=[#6]/[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6]-[#6][Se;v2][#6]-[#6]-[#6](=O)-[#7]-[#6]-c1ccc(-[#8])c(-[#8]-[#6])c1
Structure:
