| Reaction Details |
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 | Report a problem with these data |
| Target | Mitogen-activated protein kinase 8 |
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| Ligand | BDBM50341342 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_742475 (CHEMBL1769123) |
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| Kd | 29±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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| Mitogen-activated protein kinase 8 |
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| Name: | Mitogen-activated protein kinase 8 |
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| Synonyms: | JNK-46 | JNK1 | JNK1-alpha-1 | MAPK8 | MK08_HUMAN | Mitogen-Activated Protein Kinase 8 (JNK1) | PRKM8 | SAPK1 | SAPK1C | Stress-activated protein kinase JNK1 | c-Jun N-terminal kinase 1 | c-Jun N-terminal kinase 1 (JNK1) | c-Jun N-terminal kinase 1(JNK1) | c-Jun N-terminal kinase 2 (JNK2) |
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| Type: | Enzyme |
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| Mol. Mass.: | 48297.57 |
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| Organism: | Homo sapiens (Human) |
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| Description: | JNK-1 was purchased from Upstate Cell Signaling Solutions (formerly Upstate Biotechnology). |
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| Residue: | 427 |
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| Sequence: | MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRP
FQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQ
MELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSF
MMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQ
LGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSK
MLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEV
MDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAA
GPLGCCR
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| BDBM50341342 |
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| n/a |
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| Name | BDBM50341342 |
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| Synonyms: | 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one | CHEMBL1230122 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H18F2N4O3 |
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| Mol. Mass. | 388.368 |
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| SMILES | Cn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O |
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| Structure | 
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