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Target
Transient receptor potential cation channel subfamily A member 1
Ligand
BDBM452655
Substrate
n/a
Meas. Tech.
FLIPR Assay (90 minutes)
IC50
1.40±n/a nM
Citation
 Terrett, JA; Chen, H; Constantineau-Forget, L; Larouche-Gauthier, R; Lépissier, L; Beaumier, F; Déry, M; Grand-Maître, C; Sturino, C; Volgraf, M; Villemure, E Oxadiazole transient receptor potential channel inhibitors US Patent  US10710994 Publication Date 7/14/2020 
Target
Name:
Transient receptor potential cation channel subfamily A member 1
Synonyms:
ANKTM1 | Ankyrin-like with transmembrane domains protein 1 | TRPA1 | TRPA1_HUMAN | Transformation-sensitive protein p120 | Transient receptor potential cation channel subfamily A member 1 (TRPA1)
Type:
Protein
Mol. Mass.:
127514.20
Organism:
Homo sapiens (Human)
Description:
O75762
Residue:
1119
Sequence:
MKRSLRKMWRPGEKKEPQGVVYEDVPDDTEDFKESLKVVFEGSAYGLQNFNKQKKLKRCDDMDTFFLHYAAAEGQIELMEKITRDSSLEVLHEMDDYGNTPLHCAVEKNQIESVKFLLSRGANPNLRNFNMMAPLHIAVQGMNNEVMKVLLEHRTIDVNLEGENGNTAVIIACTTNNSEALQILLKKGAKPCKSNKWGCFPIHQAAFSGSKECMEIILRFGEEHGYSRQLHINFMNNGKATPLHLAVQNGDLEMIKMCLDNGAQIDPVEKGRCTAIHFAATQGATEIVKLMISSYSGSVDIVNTTDGCHETMLHRASLFDHHELADYLISVGADINKIDSEGRSPLILATASASWNIVNLLLSKGAQVDIKDNFGRNFLHLTVQQPYGLKNLRPEFMQMQQIKELVMDEDNDGCTPLHYACRQGGPGSVNNLLGFNVSIHSKSKDKKSPLHFAASYGRINTCQRLLQDISDTRLLNEGDLHGMTPLHLAAKNGHDKVVQLLLKKGALFLSDHNGWTALHHASMGGYTQTMKVILDTNLKCTDRLDEDGNTALHFAAREGHAKAVALLLSHNADIVLNKQQASFLHLALHNKRKEVVLTIIRSKRWDECLKIFSHNSPGNKCPITEMIEYLPECMKVLLDFCMLHSTEDKSCRDYYIEYNFKYLQCPLEFTKKTPTQDVIYEPLTALNAMVQNNRIELLNHPVCKEYLLMKWLAYGFRAHMMNLGSYCLGLIPMTILVVNIKPGMAFNSTGIINETSDHSEILDTTNSYLIKTCMILVFLSSIFGYCKEAGQIFQQKRNYFMDISNVLEWIIYTTGIIFVLPLFVEIPAHLQWQCGAIAVYFYWMNFLLYLQRFENCGIFIVMLEVILKTLLRSTVVFIFLLLAFGLSFYILLNLQDPFSSPLLSIIQTFSMMLGDINYRESFLEPYLRNELAHPVLSFAQLVSFTIFVPIVLMNLLIGLAVGDIAEVQKHASLKRIAMQVELHTSLEKKLPLWFLRKVDQKSTIVYPNKPRSGGMLFHIFCFLFCTGEIRQEIPNADKSLEMEILKQKYRLKDLTFLLEKQHELIKLIIQKMEIISETEDDDSHCSFQDRFKKEQMEQRNSRWNTVLRAVKAKTHHLEP
  
Inhibitor
Name:
BDBM452655
Synonyms:
2-amino-3-((3-((3R,5R)- 5-(4-fluorophenyl)tetra- hydrofuran-3-yl)-1,2,4- oxadiazol-5-yl)methyl)- 5-methylpyrido[2,3-d] pyrimidin-4(3H)-one | US10710994, Example 133
Type:
Small organic molecule
Emp. Form.:
C21H19FN6O3
Mol. Mass.:
422.4124
SMILES:
Cc1ccnc2nc(N)n(Cc3nc(no3)[C@@H]3CO[C@H](C3)c3ccc(F)cc3)c(=O)c12 |r|
Structure:
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