Target
Transient receptor potential M8 protein
Ligand
BDBM241637
Substrate
n/a
Meas. Tech.
Functional Assay
Temperature
310.15±n/a K
IC50
0.95±n/a nM
Comments
extracted
Citation
 Player, MRCalvo, RChen, JMeegalla, SParks, DJParsons, WJBallentine, SBranum, S Substituted aza-bicyclic imidazole derivatives useful as TRPM8 receptor modulators US Patent  US9409915 Publication Date 8/9/2016 
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:
BDBM241637
Synonyms:
US9409915, 20 | US9718820, Compound 20
Type:
Small organic molecule
Emp. Form.:
C24H25ClF3N5O2
Mol. Mass.:
507.936
SMILES:
COCCOc1nc(cc2nc([nH]c12)-c1c(Cl)c(nn1C)C(C)(C)C)-c1ccccc1C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: