Target
Transient receptor potential M8 protein
Ligand
BDBM241653
Substrate
n/a
Meas. Tech.
Canine TRPM8 Functional Assay
Temperature
298.15±n/a K
IC50
37.0±n/a nM
Comments
extracted
Citation
 Player, MRCalvo, RChen, JMeegalla, SParks, DJParsons, WJBallentine, SBranum, S Substituted aza-bicyclic imidazole derivatives useful TRPM8 receptor modulators US Patent  US9718820 Publication Date 8/1/2017 
Target
Name:
Transient receptor potential M8 protein
Synonyms:
Cold-menthol receptor (TRPM8) | TRPM8 Receptor | Transient receptor potential M8 protein | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential melastatin subfamily, type 8 (TRPM8)
Type:
Enzyme
Mol. Mass.:
127589.43
Organism:
Canis lupus familiaris (Dog)
Description:
Q1A7N1
Residue:
1104
Sequence:
MSFEGARLSMRNRRNGTLDSTRTLYSSTSRSTDVSYSESDLVNFIQANFKKRECVFFTKDSKATENVCKCGYAQSQHIEGTQINSNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRLSCDTDAETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLLRNCDAEGYFSAQYIMDDFKRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIPIVCFAQGGGRETLKAINTSIKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSVVKEKLVRFLPRTVSRLPEEETESWIKWLKEILESSHLLTVIKMEEAGDEIVSNAISYALYKAFSTNEQDKDNWNGQLKLLLEWNQLDLANEEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLRKFLTNDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDRSSRDDIDVELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPIDKHKKILWYYVAFFTSPFVVFAWNVVFYIAFLLLFAYVLLMDFHSVPHSPELVLYALVFVLFCDEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHPSNKTSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEHRWRWIFRSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAYFYMVVKKCFGCCCREKHAEPSACCFRNEDNETLAWEGVMKENYLVKINTKANDTSQEMRHRFRQLDTKINDLKGLLKEIANKIK
  
Inhibitor
Name:
BDBM241653
Synonyms:
US9409915, 44 | US9718820, Compound 44
Type:
Small organic molecule
Emp. Form.:
C21H19FN6
Mol. Mass.:
374.4142
SMILES:
Cn1nc(c(C#N)c1-c1nc2cc(ncc2[nH]1)-c1ccccc1F)C(C)(C)C
Structure:
Search PDB for entries with ligand similarity: