Reaction Details |
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Target | MAP kinase-interacting serine/threonine-protein kinase 1/2 |
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Ligand | BDBM50500932 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1573191 (CHEMBL3803169) |
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EC50 | 50±n/a nM |
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Citation | Han, W; Ding, Y; Xu, Y; Pfister, K; Zhu, S; Warne, B; Doyle, M; Aikawa, M; Amiri, P; Appleton, B; Stuart, DD; Fanidi, A; Shafer, CM Discovery of a Selective and Potent Inhibitor of Mitogen-Activated Protein Kinase-Interacting Kinases 1 and 2 (MNK1/2) Utilizing Structure-Based Drug Design. J Med Chem59:3034-45 (2016) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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MAP kinase-interacting serine/threonine-protein kinase 1/2 |
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Name: | MAP kinase-interacting serine/threonine-protein kinase 1/2 |
Synonyms: | n/a |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 1879554 |
Components: | This complex has 2 components. |
Component 1 |
Name: | MAP kinase-interacting serine/threonine-protein kinase 2 |
Synonyms: | GPRK7 | MAP kinase signal-integrating kinase 2 | MAP kinase-interacting serine/threonine-protein kinase 2 (MKNK2) | MAP kinase-interacting serine/threonine-protein kinase 2 (MnK2) | MAP-kinase interacting kinase 2 (MNK2) | MKNK2 | MKNK2_HUMAN | MNK2 |
Type: | Protein |
Mol. Mass.: | 51870.79 |
Organism: | Homo sapiens (Human) |
Description: | Q9HBH9 |
Residue: | 465 |
Sequence: | MVQKKPAELQGFHRSFKGQNPFELAFSLDQPDHGDSDFGLQCSARPDMPASQPIDIPDAK
KRGKKKKRGRATDSFSGRFEDVYQLQEDVLGEGAHARVQTCINLITSQEYAVKIIEKQPG
HIRSRVFREVEMLYQCQGHRNVLELIEFFEEEDRFYLVFEKMRGGSILSHIHKRRHFNEL
EASVVVQDVASALDFLHNKGIAHRDLKPENILCEHPNQVSPVKICDFDLGSGIKLNGDCS
PISTPELLTPCGSAEYMAPEVVEAFSEEASIYDKRCDLWSLGVILYILLSGYPPFVGRCG
SDCGWDRGEACPACQNMLFESIQEGKYEFPDKDWAHISCAAKDLISKLLVRDAKQRLSAA
QVLQHPWVQGCAPENTLPTPMVLQRNSCAKDLTSFAAEAIAMNRQLAQHDEDLAEEEAAG
QGQPVLVRATSRCLQLSPPSQSKLAQRRQRASLSSAPVVLVGDHA
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Component 2 |
Name: | MAP kinase-interacting serine/threonine-protein kinase 1 |
Synonyms: | MAP Kinase-Interacting Protein Kinase (MNK1) | MAP kinase signal-integrating kinase 1 | MAP kinase-interacting serine/threonine-protein kinase 1 (MnK1) | MAP kinase-interacting serine/threonine-protein kinase MNK1 | MAP-kinase interacting kinase 1 (MNK1) | MAPK signal-integrating kinase 1 | MKNK1 | MKNK1_HUMAN | MNK1 |
Type: | Serine/threonine-protein kinase |
Mol. Mass.: | 51342.85 |
Organism: | Homo sapiens (Human) |
Description: | Q9BUB5 |
Residue: | 465 |
Sequence: | MVSSQKLEKPIEMGSSEPLPIADGDRRRKKKRRGRATDSLPGKFEDMYKLTSELLGEGAY
AKVQGAVSLQNGKEYAVKIIEKQAGHSRSRVFREVETLYQCQGNKNILELIEFFEDDTRF
YLVFEKLQGGSILAHIQKQKHFNEREASRVVRDVAAALDFLHTKDKVSLCHLGWSAMAPS
GLTAAPTSLGSSDPPTSASQVAGTTGIAHRDLKPENILCESPEKVSPVKICDFDLGSGMK
LNNSCTPITTPELTTPCGSAEYMAPEVVEVFTDQATFYDKRCDLWSLGVVLYIMLSGYPP
FVGHCGADCGWDRGEVCRVCQNKLFESIQEGKYEFPDKDWAHISSEAKDLISKLLVRDAK
QRLSAAQVLQHPWVQGQAPEKGLPTPQVLQRNSSTMDLTLFAAEAIALNRQLSQHEENEL
AEEPEALADGLCSMKLSPPCKSRLARRRALAQAGRGEDRSPPTAL
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BDBM50500932 |
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n/a |
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Name | BDBM50500932 |
Synonyms: | CHEMBL3798066 |
Type | Small organic molecule |
Emp. Form. | C24H26N8O |
Mol. Mass. | 442.5162 |
SMILES | CN(C)C(=O)c1cccc(c1)-c1cnc(N)c(n1)-c1nc2cccc(N3CCNCC3)c2[nH]1 |
Structure |
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