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Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM50544503
Substrate
n/a
Meas. Tech.
ChEMBL_1993119 (CHEMBL4626854)
IC50
37±n/a nM
Citation
 Bertamino, A; Ostacolo, C; Medina, A; Di Sarno, V; Lauro, G; Ciaglia, T; Vestuto, V; Pepe, G; Basilicata, MG; Musella, S; Smaldone, G; Cristiano, C; Gonzalez-Rodriguez, S; Fernandez-Carvajal, A; Bifulco, G; Campiglia, P; Gomez-Monterrey, I; Russo, R Exploration of TRPM8 Binding Sites by ?-Carboline-Based Antagonists and Their In Vitro Characterization and In Vivo Analgesic Activities. J Med Chem 63:9672-9694 (2020) [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:
BDBM50544503
Synonyms:
CHEMBL4644158
Type:
Small organic molecule
Emp. Form.:
C19H18FN3O
Mol. Mass.:
323.3641
SMILES:
Fc1ccc(CNC(=O)[C@@H]2Cc3c(CN2)[nH]c2ccccc32)cc1 |r|
Structure:
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