Reaction Details |
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Target | Transient receptor potential cation channel subfamily M member 8 |
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Ligand | BDBM50133817 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1785284 (CHEMBL4256801) |
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IC50 | 475±n/a nM |
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Citation | Bertamino, A; Iraci, N; Ostacolo, C; Ambrosino, P; Musella, S; Di Sarno, V; Ciaglia, T; Pepe, G; Sala, M; Soldovieri, MV; Mosca, I; Gonzalez-Rodriguez, S; Fernandez-Carvajal, A; Ferrer-Montiel, A; Novellino, E; Taglialatela, M; Campiglia, P; Gomez-Monterrey, I Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem61:6140-6152 (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: | 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: | MSFRAARLSMRNRRNDTLDSTRTLYSSASRSTDLSYSESDLVNFIQANFKKRECVFFTKD
SKATENVCKCGYAQSQHMEGTQINQSEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRL
SCDTDAEILYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRSSEENIVAIGIAAWGMVSNRDTLIRNCDAEGYFLAQY
LMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIP
IVCFAQGGGKETLKAINTSIKNKIPCVVVEGSGQIADVIASLVEVEDALTSSAVKEKLVR
FLPRTVSRLPEEETESWIKWLKEILECSHLLTVIKMEEAGDEIVSNAISYALYKAFSTSE
QDKDNWNGQLKLLLEWNQLDLANDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLRKFLTHDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDR
NGRDEMDIELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPVDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHPPELVLYSLVFVLFC
DEVRQWYVNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCSRLNIPFPFIVFAY
FYMVVKKCFKCCCKEKNMESSVCCFKNEDNETLAWEGVMKENYLVKINTKANDTSEEMRH
RFRQLDTKLNDLKGLLKEIANKIK
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BDBM50133817 |
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n/a |
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Name | BDBM50133817 |
Synonyms: | 4-(3-Chloro-pyridin-2-yl)-piperazine-1-carboxylic acid (4-tert-butyl-phenyl)-amide | BCTC | CHEMBL441472 | N-(4-tert-butylphenyl)-4-(3-chloropyridin-2-yl)piperazine-1-carboxamide |
Type | Small organic molecule |
Emp. Form. | C20H25ClN4O |
Mol. Mass. | 372.892 |
SMILES | CC(C)(C)c1ccc(NC(=O)N2CCN(CC2)c2ncccc2Cl)cc1 |
Structure |
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