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TargetTransient receptor potential cation channel subfamily M member 8
LigandBDBM50089245
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1496190 (CHEMBL3579074)
IC50 181±n/a nM
Citation Andrews, MDAf Forselles, KBeaumont, KGalan, SRGlossop, PAGrenie, MJessiman, AKenyon, ASLunn, GMaw, GOwen, RMPryde, DCRoberts, DTran, TD Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain. ACS Med Chem Lett6:419-24 (2015) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Transient receptor potential cation channel subfamily M member 8
Name:Transient receptor potential cation channel subfamily M member 8
Synonyms:LTRPC6 | TRPM8 | TRPM8_HUMAN | TRPP8 | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential cation channel subfamily M member 8 | Transient receptor potential cation channel subfamily M member 8 (TRPM8)
Type:Enzyme
Mol. Mass.:127693.26
Organism:Homo sapiens (Human)
Description:Q7Z2W7
Residue:1104
Sequence:
MSFRAARLSMRNRRNDTLDSTRTLYSSASRSTDLSYSESDLVNFIQANFKKRECVFFTKD
SKATENVCKCGYAQSQHMEGTQINQSEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRL
SCDTDAEILYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRSSEENIVAIGIAAWGMVSNRDTLIRNCDAEGYFLAQY
LMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIP
IVCFAQGGGKETLKAINTSIKNKIPCVVVEGSGQIADVIASLVEVEDALTSSAVKEKLVR
FLPRTVSRLPEEETESWIKWLKEILECSHLLTVIKMEEAGDEIVSNAISYALYKAFSTSE
QDKDNWNGQLKLLLEWNQLDLANDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLRKFLTHDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDR
NGRDEMDIELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPVDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHPPELVLYSLVFVLFC
DEVRQWYVNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCSRLNIPFPFIVFAY
FYMVVKKCFKCCCKEKNMESSVCCFKNEDNETLAWEGVMKENYLVKINTKANDTSEEMRH
RFRQLDTKLNDLKGLLKEIANKIK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50089245
n/a
NameBDBM50089245
Synonyms:CHEMBL3577885
TypeSmall organic molecule
Emp. Form.C26H21FN2O3
Mol. Mass.428.4549
SMILESC[C@@H](N(Cc1cccc(c1)C(O)=O)C(=O)c1cnc2ccccc2c1)c1ccc(F)cc1 |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: