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Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM50544500
Substrate
n/a
Meas. Tech.
ChEMBL_1993118 (CHEMBL4626853)
IC50
90±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:
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:
BDBM50544500
Synonyms:
CHEMBL4649195
Type:
Small organic molecule
Emp. Form.:
C26H26N2O2
Mol. Mass.:
398.4968
SMILES:
COC(=O)C(Cc1c[nH]c2ccccc12)N(Cc1ccccc1)Cc1ccccc1
Structure:
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