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Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM50008721
Substrate
n/a
Meas. Tech.
ChEMBL_1335865 (CHEMBL3238730)
IC50
104±n/a nM
Citation
 Horne, DB; Tamayo, NA; Bartberger, MD; Bo, Y; Clarine, J; Davis, CD; Gore, VK; Kaller, MR; Lehto, SG; Ma, VV; Nishimura, N; Nguyen, TT; Tang, P; Wang, W; Youngblood, BD; Zhang, M; Gavva, NR; Monenschein, H; Norman, MH Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists. J Med Chem 57:2989-3004 (2014) [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:
BDBM50008721
Synonyms:
CHEMBL3235961
Type:
Small organic molecule
Emp. Form.:
C24H18F3N3O
Mol. Mass.:
421.4144
SMILES:
FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2ccccc12)C(=O)Nc1ccccc1C#N |r|
Structure:
Search PDB for entries with ligand similarity: