Reaction Details |
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Target | Mitogen-activated protein kinase 14 |
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Ligand | BDBM50327020 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_663513 (CHEMBL1251166) |
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IC50 | 3.9±n/a nM |
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Citation | Liu, C; Lin, J; Wrobleski, ST; Lin, S; Hynes, J; Wu, H; Dyckman, AJ; Li, T; Wityak, J; Gillooly, KM; Pitt, S; Shen, DR; Zhang, RF; McIntyre, KW; Salter-Cid, L; Shuster, DJ; Zhang, H; Marathe, PH; Doweyko, AM; Sack, JS; Kiefer, SE; Kish, KF; Newitt, JA; McKinnon, M; Dodd, JH; Barrish, JC; Schieven, GL; Leftheris, K Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38a MAP kinase inhibitor for the treatment of inflammatory diseases. J Med Chem53:6629-39 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Mitogen-activated protein kinase 14 |
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Name: | Mitogen-activated protein kinase 14 |
Synonyms: | CSAID-binding protein | CSBP | CSBP1 | CSBP2 | CSPB1 | Cytokine suppressive anti-inflammatory drug-binding protein | MAP kinase 14 | MAP kinase MXI2 | MAP kinase p38 alpha | MAPK 14 | MAPK14 | MAX-interacting protein 2 | MK14_HUMAN | MXI2 | Mitogen-activated protein kinase p38 alpha | SAPK2A | Stress-activated protein kinase 2a | p38 MAP kinase alpha/beta |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 41286.76 |
Organism: | Homo sapiens (Human) |
Description: | Q16539 |
Residue: | 360 |
Sequence: | MSQERPTFYRQELNKTIWEVPERYQNLSPVGSGAYGSVCAAFDTKTGLRVAVKKLSRPFQ
SIIHAKRTYRELRLLKHMKHENVIGLLDVFTPARSLEEFNDVYLVTHLMGADLNNIVKCQ
KLTDDHVQFLIYQILRGLKYIHSADIIHRDLKPSNLAVNEDCELKILDFGLARHTDDEMT
GYVATRWYRAPEIMLNWMHYNQTVDIWSVGCIMAELLTGRTLFPGTDHIDQLKLILRLVG
TPGAELLKKISSESARNYIQSLTQMPKMNFANVFIGANPLAVDLLEKMLVLDSDKRITAA
QALAHAYFAQYHDPDDEPVADPYDQSFESRDLLIDEWKSLTYDEVISFVPPPLDQEEMES
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BDBM50327020 |
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n/a |
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Name | BDBM50327020 |
Synonyms: | 4-(5-(Isoxazol-3-ylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide | 4-{[5-(isoxazol-3-ylcarbamoyl)-2-methylphenyl]amino}-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide | CHEMBL1230070 |
Type | Small organic molecule |
Emp. Form. | C22H23N7O3 |
Mol. Mass. | 433.4631 |
SMILES | CCCNC(=O)c1cn2ncnc(Nc3cc(ccc3C)C(=O)Nc3ccon3)c2c1C |
Structure |
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