| 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 | BDBM50463853 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1779571 (CHEMBL4236563) |
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| IC50 | 7.0±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: | Cmr1 | TRPM8_RAT | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential cation channel subfamily M member 8 | Trpm8 |
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| Type: | Enzyme |
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| Mol. Mass.: | 127633.53 |
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| Organism: | Rattus norvegicus (Rat) |
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| Description: | Q8R455 |
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| Residue: | 1104 |
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| Sequence: | MSFEGARLSMRSRRNGTLGSTRTLYSSVSRSTDVSYSESDLVNFIQANFKKRECVFFTRD
SKAMESICKCGYAQSQHIEGTQINQNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYLRL
SCDTDSETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLIRNCDDEGHFSAQY
IMDDFMRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTSQDSNYGGKIP
IVCFAQGGGRETLKAINTSVKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSMVKEKLVR
FLPRTVSRLPEEEIESWIKWLKEILESPHLLTVIKMEEAGDEVVSSAISYALYKAFSTNE
QDKDNWNGQLKLLLEWNQLDLASDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLQKFLTNEVLTELFSTHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRSFWKEDR
SSREDLDVELHDASLTTRHPLQALFIWAILQNKKELSKVIWEQTKGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGLVSFRKKPIDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHTPELILYALVFVLFC
DEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDSTTYDFSHCTFSGNESKPLCVELDEYNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGIVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAY
FYMVVKKCFKCCCKEKNTESSACCFRNEDNETLAWEGVMKENYLVKINTKANDNAEEMRH
RFRQLDTKLNDLKGLLKEIANKIK
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| BDBM50463853 |
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| n/a |
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| Name | BDBM50463853 |
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| Synonyms: | CHEMBL4237618 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H12F5N3O2 |
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| Mol. Mass. | 409.3095 |
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| SMILES | Fc1cccnc1[C@@H](NC(=O)c1ccc(=O)[nH]c1)c1ccc(c(F)c1)C(F)(F)F |r| |
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| Structure | 
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