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TargetTransient receptor potential cation channel subfamily M member 8
LigandBDBM50383229
Substrate/Competitorn/a
Meas. Tech.ChEMBL_819359 (CHEMBL2032922)
IC50 560±n/a nM
Citation Tamayo, NABo, YGore, VMa, VNishimura, NTang, PDeng, HKlionsky, LLehto, SGWang, WYoungblood, BChen, JCorrell, TLBartberger, MDGavva, NRNorman, MH Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists. J Med Chem55:1593-611 (2012) [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:
BDBM50383229
n/a
NameBDBM50383229
Synonyms:CHEMBL2032175
TypeSmall organic molecule
Emp. Form.C20H17ClN2OS
Mol. Mass.368.88
SMILESClc1ccc(cc1)C1N(CCc2sccc12)C(=O)Nc1ccccc1
Structure
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