Reaction Details |
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Target | Transient receptor potential cation channel subfamily M member 8 |
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Ligand | BDBM50383229 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_819359 (CHEMBL2032922) |
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IC50 | 560±n/a nM |
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Citation | Tamayo, NA; Bo, Y; Gore, V; Ma, V; Nishimura, N; Tang, P; Deng, H; Klionsky, L; Lehto, SG; Wang, W; Youngblood, B; Chen, J; Correll, TL; Bartberger, MD; Gavva, NR; Norman, MH Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists. J Med Chem55:1593-611 (2012) [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: | Cmr1 | TRPM8_RAT | Transient receptor potential M8 protein (TRPM8) | Transient receptor potential cation channel subfamily M member 8 | Trpm8 |
Type: | Enzyme |
Mol. Mass.: | 127633.53 |
Organism: | Rattus norvegicus (Rat) |
Description: | Q8R455 |
Residue: | 1104 |
Sequence: | MSFEGARLSMRSRRNGTLGSTRTLYSSVSRSTDVSYSESDLVNFIQANFKKRECVFFTRD
SKAMESICKCGYAQSQHIEGTQINQNEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYLRL
SCDTDSETLYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRNSEENIVAIGIAAWGMVSNRDTLIRNCDDEGHFSAQY
IMDDFMRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTSQDSNYGGKIP
IVCFAQGGGRETLKAINTSVKSKIPCVVVEGSGQIADVIASLVEVEDVLTSSMVKEKLVR
FLPRTVSRLPEEEIESWIKWLKEILESPHLLTVIKMEEAGDEVVSSAISYALYKAFSTNE
QDKDNWNGQLKLLLEWNQLDLASDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLQKFLTNEVLTELFSTHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRSFWKEDR
SSREDLDVELHDASLTTRHPLQALFIWAILQNKKELSKVIWEQTKGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGLVSFRKKPIDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHTPELILYALVFVLFC
DEVRQWYMNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDSTTYDFSHCTFSGNESKPLCVELDEYNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGIVQENNDQVWKFQRYFLVQEYCNRLNIPFPFVVFAY
FYMVVKKCFKCCCKEKNTESSACCFRNEDNETLAWEGVMKENYLVKINTKANDNAEEMRH
RFRQLDTKLNDLKGLLKEIANKIK
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BDBM50383229 |
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n/a |
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Name | BDBM50383229 |
Synonyms: | CHEMBL2032175 |
Type | Small organic molecule |
Emp. Form. | C20H17ClN2OS |
Mol. Mass. | 368.88 |
SMILES | Clc1ccc(cc1)C1N(CCc2sccc12)C(=O)Nc1ccccc1 |
Structure |
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