Reaction Details |
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Target | Transient receptor potential cation channel subfamily M member 8 |
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Ligand | BDBM50463876 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1779572 (CHEMBL4236564) |
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IC50 | 24±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 |
Synonyms: | LTrpC-6 | Long transient receptor potential channel 6 | Ltrpc6 | TRPM8_MOUSE | Transient receptor potential p8 | Trp-p8 | Trpm8 | Trpp8 |
Type: | PROTEIN |
Mol. Mass.: | 127713.99 |
Organism: | Mus musculus |
Description: | ChEMBL_107992 |
Residue: | 1104 |
Sequence: | MSFEGARLSMRSRRNGTMGSTRTLYSSVSRSTDVSYSDSDLVNFIQANFKKRECVFFTRD
SKAMENICKCGYAQSQHIEGTQINQNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYLRL
SCDTDSETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLIRSCDDEGHFSAQY
IMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTSQDSNYGGKIP
IVCFAQGGGRETLKAINTSVKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSMVKEKLVR
FLPRTVSRLPEEEIESWIKWLKEILESSHLLTVIKMEEAGDEIVSNAISYALYKAFSTNE
QDKDNWNGQLKLLLEWNQLDLASDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLQKFLTNEVLTELFSTHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRSFWKEDR
SSREDLDVELHDASLTTRHPLQALFIWAILQNKKELSKVIWEQTKGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSNDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGLVSFRKKPIDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHTPELILYALVFVLFC
DEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDSTTYDFSHCTFSGNESKPLCVELDEHNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGIVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAY
FYMVVKKCFKCCCKEKNMESNACCFRNEDNETLAWEGVMKENYLVKINTKANDNSEEMRH
RFRQLDSKLNDLKSLLKEIANNIK
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BDBM50463876 |
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n/a |
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Name | BDBM50463876 |
Synonyms: | CHEMBL4238921 |
Type | Small organic molecule |
Emp. Form. | C21H15F6N3O2 |
Mol. Mass. | 455.3531 |
SMILES | COc1ccc(cn1)C(=O)N[C@@H](c1ccc(cc1)C(F)(F)F)c1ncccc1C(F)(F)F |r| |
Structure |
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