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TargetTransient receptor potential cation channel subfamily M member 8
LigandBDBM50544520
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1993118 (CHEMBL4626853)
IC50 22900±n/a nM
Citation Bertamino, AOstacolo, CMedina, ADi Sarno, VLauro, GCiaglia, TVestuto, VPepe, GBasilicata, MGMusella, SSmaldone, GCristiano, CGonzalez-Rodriguez, SFernandez-Carvajal, ABifulco, GCampiglia, PGomez-Monterrey, IRusso, R Exploration of TRPM8 Binding Sites by ?-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities. J Med Chem63:9672-9694 (2020) [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:
BDBM50544520
n/a
NameBDBM50544520
Synonyms:CHEMBL4636809
TypeSmall organic molecule
Emp. Form.C25H27N3O3
Mol. Mass.417.5002
SMILES[H][C@]12Cc3c([nH]c4ccccc34)[C@H](CC(C)C)N1C(=O)N(Cc1ccc(OC)cc1)C2=O |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: