Reaction Details |
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Target | Mitogen-activated protein kinase 8 |
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Ligand | BDBM241338 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1779811 (CHEMBL4236803) |
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IC50 | 92±n/a nM |
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Citation | Woodward, HL; Innocenti, P; Cheung, KJ; Hayes, A; Roberts, J; Henley, AT; Faisal, A; Mak, GW; Box, G; Westwood, IM; Cronin, N; Carter, M; Valenti, M; De Haven Brandon, A; O'Fee, L; Saville, H; Schmitt, J; Burke, R; Broccatelli, F; van Montfort, RLM; Raynaud, FI; Eccles, SA; Linardopoulos, S; Blagg, J; Hoelder, S Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N J Med Chem61:8226-8240 (2018) [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 |
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) |
Type: | Enzyme |
Mol. Mass.: | 48297.57 |
Organism: | Homo sapiens (Human) |
Description: | JNK-1 was purchased from Upstate Cell Signaling Solutions (formerly Upstate Biotechnology). |
Residue: | 427 |
Sequence: | MSRSKRDNNFYSVEIGDSTFTVLKRYQNLKPIGSGAQGIVCAAYDAILERNVAIKKLSRP
FQNQTHAKRAYRELVLMKCVNHKNIIGLLNVFTPQKSLEEFQDVYIVMELMDANLCQVIQ
MELDHERMSYLLYQMLCGIKHLHSAGIIHRDLKPSNIVVKSDCTLKILDFGLARTAGTSF
MMTPYVVTRYYRAPEVILGMGYKENVDLWSVGCIMGEMVCHKILFPGRDYIDQWNKVIEQ
LGTPCPEFMKKLQPTVRTYVENRPKYAGYSFEKLFPDVLFPADSEHNKLKASQARDLLSK
MLVIDASKRISVDEALQHPYINVWYDPSEAEAPPPKIPDKQLDEREHTIEEWKELIYKEV
MDLEERTKNGVIRGQPSPLGAAVINGSQHPSSSSSVNDVSSMSTDPTLASDTDSSLEAAA
GPLGCCR
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BDBM241338 |
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n/a |
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Name | BDBM241338 |
Synonyms: | US10479788, Example 182 | US11046688, Example 182 | US9409907, 182 |
Type | Small organic molecule |
Emp. Form. | C24H30N8O |
Mol. Mass. | 446.548 |
SMILES | CCOc1cc(ccc1Nc1ncc2cc(C)nc(NCC(C)(C)C)c2n1)-c1nncn1C |
Structure |
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