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Target
Transient receptor potential M8 protein
Ligand
BDBM248292
Substrate
n/a
Meas. Tech.
Functional Assay
Temperature
310.15±n/a K
IC50
2±n/a nM
Comments
extracted
Citation
 Branum, ST; Colburn, RW; Dax, SL; Flores, CM; Jetter, MC; Liu, Y; Ludovici, D; Macielag, MJ; Matthews, JM; McNally, JJ; Andraka, LM; Russell, RK; Qin, N; Teleha, C; Wells, KM; Youells, SC; Youngman, MA Sulfonamides as TRPM8 modulators US Patent  US9434711 Publication Date 9/6/2016 
Target
Name:
Transient receptor potential M8 protein
Synonyms:
Cold-menthol receptor (TRPM8) | TRPM8 Receptor | Transient receptor potential M8 protein | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential melastatin subfamily, type 8 (TRPM8)
Type:
Enzyme
Mol. Mass.:
127589.43
Organism:
Canis lupus familiaris (Dog)
Description:
Q1A7N1
Residue:
1104
Sequence:
MSFEGARLSMRNRRNGTLDSTRTLYSSTSRSTDVSYSESDLVNFIQANFKKRECVFFTKDSKATENVCKCGYAQSQHIEGTQINSNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRLSCDTDAETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLLRNCDAEGYFSAQYIMDDFKRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIPIVCFAQGGGRETLKAINTSIKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSVVKEKLVRFLPRTVSRLPEEETESWIKWLKEILESSHLLTVIKMEEAGDEIVSNAISYALYKAFSTNEQDKDNWNGQLKLLLEWNQLDLANEEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLRKFLTNDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDRSSRDDIDVELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPIDKHKKILWYYVAFFTSPFVVFAWNVVFYIAFLLLFAYVLLMDFHSVPHSPELVLYALVFVLFCDEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHPSNKTSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEHRWRWIFRSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAYFYMVVKKCFGCCCREKHAEPSACCFRNEDNETLAWEGVMKENYLVKINTKANDTSQEMRHRFRQLDTKINDLKGLLKEIANKIK
  
Inhibitor
Name:
BDBM248292
Synonyms:
US9434711, 140
Type:
Small organic molecule
Emp. Form.:
C21H15BrFNO2S2
Mol. Mass.:
476.382
SMILES:
Fc1ccc(CN(c2sc3ccccc3c2Br)S(=O)(=O)c2ccccc2)cc1
Structure:
Search PDB for entries with ligand similarity: