| Reaction Details |
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 | Report a problem with these data |
| Target | Ribosomal protein S6 kinase alpha-4 |
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| Ligand | BDBM50314070 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_742527 (CHEMBL1769286) |
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| Kd | 150±n/a nM |
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| Citation |  Goldstein, DM; Soth, M; Gabriel, T; Dewdney, N; Kuglstatter, A; Arzeno, H; Chen, J; Bingenheimer, W; Dalrymple, SA; Dunn, J; Farrell, R; Frauchiger, S; La Fargue, J; Ghate, M; Graves, B; Hill, RJ; Li, F; Litman, R; Loe, B; McIntosh, J; McWeeney, D; Papp, E; Park, J; Reese, HF; Roberts, RT; Rotstein, D; San Pablo, B; Sarma, K; Stahl, M; Sung, ML; Suttman, RT; Sjogren, EB; Tan, Y; Trejo, A; Welch, M; Weller, P; Wong, BR; Zecic, H Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors J Med Chem54:2255-65 (2011) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Ribosomal protein S6 kinase alpha-4 |
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| Name: | Ribosomal protein S6 kinase alpha-4 |
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| Synonyms: | 90 kDa ribosomal protein S6 kinase 4 | KS6A4_HUMAN | MSK2 | Mitogen- and Stress-Activated Protein Kinase 2 (MSK2) | Nuclear mitogen- and stress-activated protein kinase 2 | RPS6KA4 | RPS6KA4(Kin.Dom.1 - N-terminal) | RSKB | Ribosomal protein S6 kinase | Ribosomal protein S6 kinase alpha 4 | Ribosomal protein S6 kinase alpha-4 | Ribosomal protein kinase B |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 85620.38 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Recombinant MSK2 was phosphorylated by incubation with active p38alpha before assays. |
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| Residue: | 772 |
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| Sequence: | MGDEDDDESCAVELRITEANLTGHEEKVSVENFELLKVLGTGAYGKVFLVRKAGGHDAGK
LYAMKVLRKAALVQRAKTQEHTRTERSVLELVRQAPFLVTLHYAFQTDAKLHLILDYVSG
GEMFTHLYQRQYFKEAEVRVYGGEIVLALEHLHKLGIIYRDLKLENVLLDSEGHIVLTDF
GLSKEFLTEEKERTFSFCGTIEYMAPEIIRSKTGHGKAVDWWSLGILLFELLTGASPFTL
EGERNTQAEVSRRILKCSPPFPPRIGPVAQDLLQRLLCKDPKKRLGAGPQGAQEVRNHPF
FQGLDWVALAARKIPAPFRPQIRSELDVGNFAEEFTRLEPVYSPPGSPPPGDPRIFQGYS
FVAPSILFDHNNAVMTDGLEAPGAGDRPGRAAVARSAMMQDSPFFQQYELDLREPALGQG
SFSVCRRCRQRQSGQEFAVKILSRRLEANTQREVAALRLCQSHPNVVNLHEVHHDQLHTY
LVLELLRGGELLEHIRKKRHFSESEASQILRSLVSAVSFMHEEAGVVHRDLKPENILYAD
DTPGAPVKIIDFGFARLRPQSPGVPMQTPCFTLQYAAPELLAQQGYDESCDLWSLGVILY
MMLSGQVPFQGASGQGGQSQAAEIMCKIREGRFSLDGEAWQGVSEEAKELVRGLLTVDPA
KRLKLEGLRGSSWLQDGSARSSPPLRTPDVLESSGPAVRSGLNATFMAFNRGKREGFFLK
SVENAPLAKRRKQKLRSATASRRGSPAPANPGRAPVASKGAPRRANGPLPPS
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| BDBM50314070 |
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| n/a |
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| Name | BDBM50314070 |
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| Synonyms: | 6-(2,4-difluorophenoxy)-2-{[3-hydroxy-1-(2-hydroxyethyl)propyl]amino}-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1090089 | pamapimod |
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| Type | Small organic molecule |
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| Emp. Form. | C19H20F2N4O4 |
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| Mol. Mass. | 406.3833 |
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| SMILES | Cn1c2nc(NC(CCO)CCO)ncc2cc(Oc2ccc(F)cc2F)c1=O |
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| Structure | 
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