Target
Transient receptor potential cation channel subfamily M member 8
Ligand
BDBM151786
Substrate
n/a
Meas. Tech.
Inhibition Assay
Temperature
310.15±n/a K
IC50
1.6±n/a nM
Comments
extracted
Citation
 Tsuzuki, YSawamoto, DSakamoto, TKato, TNiwa, YAwai, N Sulfonamide compounds having TRPM8 antagonistic activity US Patent  US8987445 Publication Date 3/24/2015 
Target
Name:
Transient receptor potential cation channel subfamily M member 8
Synonyms:
LTRPC6 | TRPM8 | TRPM8_HUMAN | TRPP8 | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential cation channel subfamily M member 8 | Transient receptor potential cation channel subfamily M member 8 (TRPM8)
Type:
Enzyme
Mol. Mass.:
127693.26
Organism:
Homo sapiens (Human)
Description:
Q7Z2W7
Residue:
1104
Sequence:
MSFRAARLSMRNRRNDTLDSTRTLYSSASRSTDLSYSESDLVNFIQANFKKRECVFFTKDSKATENVCKCGYAQSQHMEGTQINQSEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRLSCDTDAEILYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWILTGGTHYGLMKYIGEVVRDNTISRSSEENIVAIGIAAWGMVSNRDTLIRNCDAEGYFLAQYLMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIPIVCFAQGGGKETLKAINTSIKNKIPCVVVEGSGQIADVIASLVEVEDALTSSAVKEKLVRFLPRTVSRLPEEETESWIKWLKEILECSHLLTVIKMEEAGDEIVSNAISYALYKAFSTSEQDKDNWNGQLKLLLEWNQLDLANDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLENGLNLRKFLTHDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDRNGRDEMDIELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKTLAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELAVEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPVDKHKKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHPPELVLYSLVFVLFCDEVRQWYVNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFTLRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIFRSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLVCIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCSRLNIPFPFIVFAYFYMVVKKCFKCCCKEKNMESSVCCFKNEDNETLAWEGVMKENYLVKINTKANDTSEEMRHRFRQLDTKLNDLKGLLKEIANKIK
  
Inhibitor
Name:
BDBM151786
Synonyms:
US8987445, 222
Type:
Small organic molecule
Emp. Form.:
C28H24ClF3N2O5S
Mol. Mass.:
593.014
SMILES:
COC(C)(c1ccc(CN(c2ncc3ccccc3c2C)S(=O)(=O)c2ccc(cc2)C(O)=O)cc1Cl)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: