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TargetTransient receptor potential cation channel subfamily M member 8
LigandBDBM50535865
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1932424 (CHEMBL4478076)
IC50 500±n/a nM
Citation De Petrocellis, LArroyo, FJOrlando, PSchiano Moriello, AVitale, RMAmodeo, PSánchez, ARoncero, CBianchini, GMartín, MALópez-Alvarado, PMenéndez, JC Tetrahydroisoquinoline-Derived Urea and 2,5-Diketopiperazine Derivatives as Selective Antagonists of the Transient Receptor Potential Melastatin 8 (TRPM8) Channel Receptor and Antiprostate Cancer Agents. J Med Chem59:5661-83 (2016) [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:Cmr1 | TRPM8_RAT | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential cation channel subfamily M member 8 | Trpm8
Type:Enzyme
Mol. Mass.:127633.53
Organism:Rattus norvegicus (Rat)
Description:Q8R455
Residue:1104
Sequence:
MSFEGARLSMRSRRNGTLGSTRTLYSSVSRSTDVSYSESDLVNFIQANFKKRECVFFTRD
SKAMESICKCGYAQSQHIEGTQINQNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYLRL
SCDTDSETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLIRNCDDEGHFSAQY
IMDDFMRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTSQDSNYGGKIP
IVCFAQGGGRETLKAINTSVKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSMVKEKLVR
FLPRTVSRLPEEEIESWIKWLKEILESPHLLTVIKMEEAGDEVVSSAISYALYKAFSTNE
QDKDNWNGQLKLLLEWNQLDLASDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLQKFLTNEVLTELFSTHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRSFWKEDR
SSREDLDVELHDASLTTRHPLQALFIWAILQNKKELSKVIWEQTKGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGLVSFRKKPIDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHTPELILYALVFVLFC
DEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDSTTYDFSHCTFSGNESKPLCVELDEYNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGIVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAY
FYMVVKKCFKCCCKEKNTESSACCFRNEDNETLAWEGVMKENYLVKINTKANDNAEEMRH
RFRQLDTKLNDLKGLLKEIANKIK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50535865
n/a
NameBDBM50535865
Synonyms:CHEMBL4543647
TypeSmall organic molecule
Emp. Form.C35H36N2O5
Mol. Mass.564.6707
SMILESCOc1cc2CCN([C@@H](c3ccccc3)c2cc1OC)C(=O)N1CCc2cc(OC)c(OC)cc2[C@@H]1c1ccccc1 |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: