| Reaction Details |
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 | Report a problem with these data |
| Target | Transient receptor potential cation channel subfamily M member 8 |
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| Ligand | BDBM50463867 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1779570 (CHEMBL4236562) |
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| IC50 | 35±n/a nM |
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| Citation |  Horne, DB; Biswas, K; Brown, J; Bartberger, MD; Clarine, J; Davis, CD; Gore, VK; Harried, S; Horner, M; Kaller, MR; Lehto, SG; Liu, Q; Ma, VV; Monenschein, H; Nguyen, TT; Yuan, CC; Youngblood, BD; Zhang, M; Zhong, W; Allen, JR; Chen, JJ; Gavva, NR Discovery of TRPM8 Antagonist ( S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic Acid (AMG 333), a Clinical Candidate for the Treatment of Migraine. J Med Chem61:8186-8201 (2018) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Transient receptor potential cation channel subfamily M member 8 |
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| Name: | Transient receptor potential cation channel subfamily M member 8 |
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| 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) |
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| Type: | Enzyme |
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| Mol. Mass.: | 127693.26 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q7Z2W7 |
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| Residue: | 1104 |
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| Sequence: | MSFRAARLSMRNRRNDTLDSTRTLYSSASRSTDLSYSESDLVNFIQANFKKRECVFFTKD
SKATENVCKCGYAQSQHMEGTQINQSEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRL
SCDTDAEILYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRSSEENIVAIGIAAWGMVSNRDTLIRNCDAEGYFLAQY
LMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIP
IVCFAQGGGKETLKAINTSIKNKIPCVVVEGSGQIADVIASLVEVEDALTSSAVKEKLVR
FLPRTVSRLPEEETESWIKWLKEILECSHLLTVIKMEEAGDEIVSNAISYALYKAFSTSE
QDKDNWNGQLKLLLEWNQLDLANDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLRKFLTHDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDR
NGRDEMDIELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPVDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHPPELVLYSLVFVLFC
DEVRQWYVNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCSRLNIPFPFIVFAY
FYMVVKKCFKCCCKEKNMESSVCCFKNEDNETLAWEGVMKENYLVKINTKANDTSEEMRH
RFRQLDTKLNDLKGLLKEIANKIK
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| BDBM50463867 |
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| n/a |
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| Name | BDBM50463867 |
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| Synonyms: | CHEMBL4249999 |
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| Type | Small organic molecule |
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| Emp. Form. | C20H13F6N3O |
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| Mol. Mass. | 425.3271 |
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| SMILES | FC(F)(F)c1ccc(cc1)[C@H](NC(=O)c1cccnc1)c1ncccc1C(F)(F)F |r| |
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| Structure | 
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