Reaction Details Report a problem with these data
Target
Transient receptor potential M8 protein
Ligand
BDBM267459
Substrate
n/a
Meas. Tech.
Canine TRPM8 Functional Assay
Temperature
298.15±n/a K
IC50
3.20±n/a nM
Comments
extracted
Citation
 Player, MR; Calvo, R; Chen, J; Meegalla, S; Parks, DJ; Parsons, WJ; Ballentine, S; Branum, 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:
Dog
Description:
Q1A7N1
Residue:
1104
Sequence:
MSFEGARLSMRNRRNGTLDSTRTLYSSTSRSTDVSYSESDLVNFIQANFKKRECVFFTKDSKATENVCKCGYAQSQHIEGTQINSNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRLSCDTDAETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLLRNCDAEGYFSAQYIMDDFKRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIPIVCFAQGGGRETLKAINTSIKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSVVKEKLVRFLPRTVSRLPEEETESWIKWLKEILESSHLLTVIKMEEAGDEIVSNAISYALYKAFSTNEQDKDNWNGQLKLLLEWNQLDLANEEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLRKFLTNDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDRSSRDDIDVELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPIDKHKKILWYYVAFFTSPFVVFAWNVVFYIAFLLLFAYVLLMDFHSVPHSPELVLYALVFVLFCDEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHPSNKTSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEHRWRWIFRSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAYFYMVVKKCFGCCCREKHAEPSACCFRNEDNETLAWEGVMKENYLVKINTKANDTSQEMRHRFRQLDTKINDLKGLLKEIANKIK
  
Inhibitor
Name:
BDBM267459
Synonyms:
3-tert-Butyl-1-methyl-5-[4-morpholin-4-yl-6-(2-trifloromethyl-phenyl)- 3H-imidazo[4,5-c]pyridin-2-yl]-1H-pyrazole-4-carbonitrile | US9718820, Compound 65
Type:
Small organic molecule
Emp. Form.:
C26H26F3N7O
Mol. Mass.:
509.5261
SMILES:
Cn1nc(c(C#N)c1-c1nc2cc(nc(N3CCOCC3)c2[nH]1)-c1ccccc1C(F)(F)F)C(C)(C)C
Structure:
Search PDB for entries with ligand similarity: