Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM50207662
Substrate
n/a
Meas. Tech.
ChEMBL_1632145 (CHEMBL3874851)
IC50
1700±n/a nM
Citation
 Kobayashi, JIHirasawa, HOzawa, TOzawa, TTakeda, HFujimori, YNakanishi, OKamada, NIkeda, T Synthesis and optimization of novela-phenylglycinamides as selective TRPM8 antagonists. Bioorg Med Chem 25:727-742 (2017) [PubMed]  Article 
Target
Name:
Transient receptor potential cation channel subfamily M member 8
Synonyms:
LTRPC6 | TRPM8 | TRPM8_HUMAN | TRPP8 | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential cation channel subfamily M member 8 | Transient receptor potential cation channel subfamily M member 8 (TRPM8)
Type:
Enzyme
Mol. Mass.:
127693.26
Organism:
Homo sapiens (Human)
Description:
Q7Z2W7
Residue:
1104
Sequence:
MSFRAARLSMRNRRNDTLDSTRTLYSSASRSTDLSYSESDLVNFIQANFKKRECVFFTKDSKATENVCKCGYAQSQHMEGTQINQSEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRLSCDTDAEILYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRSSEENIVAIGIAAWGMVSNRDTLIRNCDAEGYFLAQYLMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIPIVCFAQGGGKETLKAINTSIKNKIPCVVVEGSGQIADVIASLVEVEDALTSSAVKEKLVRFLPRTVSRLPEEETESWIKWLKEILECSHLLTVIKMEEAGDEIVSNAISYALYKAFSTSEQDKDNWNGQLKLLLEWNQLDLANDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLRKFLTHDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDRNGRDEMDIELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPVDKHKKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHPPELVLYSLVFVLFCDEVRQWYVNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIFRSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCSRLNIPFPFIVFAYFYMVVKKCFKCCCKEKNMESSVCCFKNEDNETLAWEGVMKENYLVKINTKANDTSEEMRHRFRQLDTKLNDLKGLLKEIANKIK
  
Inhibitor
Name:
BDBM50207662
Synonyms:
CHEMBL3943602
Type:
Small organic molecule
Emp. Form.:
C21H20N2O3S
Mol. Mass.:
380.46
SMILES:
COc1cccc(CN([C@@H](C(N)=O)c2ccccc2)C(=O)c2cccs2)c1 |r|
Structure:
Search PDB for entries with ligand similarity: