Reaction Details  Report a problem with these data
Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM50465611
Substrate
n/a
Meas. Tech.
ChEMBL_1785280 (CHEMBL4256797)
IC50
600±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:
BDBM50465611
Synonyms:
CHEMBL4284808
Type:
Small organic molecule
Emp. Form.:
C24H30N2
Mol. Mass.:
346.5084
SMILES:
C(Cc1c[nH]c2ccccc12)N(CC1CCCCC1)Cc1ccccc1
Structure:
Search PDB for entries with ligand similarity: