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Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM50365710
Substrate
n/a
Meas. Tech.
ChEMBL_805767 (CHEMBL1958510)
IC50
20±n/a nM
Citation
 Calvo, RR; Meegalla, SK; Parks, DJ; Parsons, WH; Ballentine, SK; Lubin, ML; Schneider, C; Colburn, RW; Flores, CM; Player, MR Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia. Bioorg Med Chem Lett 22:1903-7 (2012) [PubMed]  Article 
Target
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:
MSFEGARLSMRSRRNGTLGSTRTLYSSVSRSTDVSYSESDLVNFIQANFKKRECVFFTRDSKAMESICKCGYAQSQHIEGTQINQNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYLRLSCDTDSETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLIRNCDDEGHFSAQYIMDDFMRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTSQDSNYGGKIPIVCFAQGGGRETLKAINTSVKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSMVKEKLVRFLPRTVSRLPEEEIESWIKWLKEILESPHLLTVIKMEEAGDEVVSSAISYALYKAFSTNEQDKDNWNGQLKLLLEWNQLDLASDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLQKFLTNEVLTELFSTHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRSFWKEDRSSREDLDVELHDASLTTRHPLQALFIWAILQNKKELSKVIWEQTKGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGLVSFRKKPIDKHKKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHTPELILYALVFVLFCDEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIFRSVIYEPYLAMFGQVPSDVDSTTYDFSHCTFSGNESKPLCVELDEYNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGIVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAYFYMVVKKCFKCCCKEKNTESSACCFRNEDNETLAWEGVMKENYLVKINTKANDNAEEMRHRFRQLDTKLNDLKGLLKEIANKIK
  
Inhibitor
Name:
BDBM50365710
Synonyms:
CHEMBL1955989
Type:
Small organic molecule
Emp. Form.:
C22H21F3N2
Mol. Mass.:
370.4107
SMILES:
FC(F)(F)c1ccccc1-c1ccc2nc(C=CC3CCCCC3)[nH]c2c1 |w:16.16|
Structure:
Search PDB for entries with ligand similarity: