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Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM50465618
Substrate
n/a
Meas. Tech.
ChEMBL_1785280 (CHEMBL4256797)
IC50
1600±n/a nM
Citation
 Bertamino, A; Iraci, N; Ostacolo, C; Ambrosino, P; Musella, S; Di Sarno, V; Ciaglia, T; Pepe, G; Sala, M; Soldovieri, MV; Mosca, I; Gonzalez-Rodriguez, S; Fernandez-Carvajal, A; Ferrer-Montiel, A; Novellino, E; Taglialatela, M; Campiglia, P; Gomez-Monterrey, I Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem 61:6140-6152 (2018) [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:
BDBM50465618
Synonyms:
CHEMBL4291622
Type:
Small organic molecule
Emp. Form.:
C25H22N2O
Mol. Mass.:
366.455
SMILES:
O=C(CN1CCc2c([nH]c3ccccc23)C1c1ccccc1)c1ccccc1
Structure:
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