| Reaction Details |
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 | Report a problem with these data |
| Target | MAP kinase-interacting serine/threonine-protein kinase 1/2 |
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| Ligand | BDBM375315 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1754738 (CHEMBL4189498) |
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| IC50 | 130±n/a nM |
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| Citation |  Yang, H; Chennamaneni, LR; Ho, MWT; Ang, SH; Tan, ESW; Jeyaraj, DA; Yeap, YS; Liu, B; Ong, EH; Joy, JK; Wee, JLK; Kwek, P; Retna, P; Dinie, N; Nguyen, TTH; Tai, SJ; Manoharan, V; Pendharkar, V; Low, CB; Chew, YS; Vuddagiri, S; Sangthongpitag, K; Choong, ML; Lee, MA; Kannan, S; Verma, CS; Poulsen, A; Lim, S; Chuah, C; Ong, TS; Hill, J; Matter, A; Nacro, K Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia. J Med Chem61:4348-4369 (2018) [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 |
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| Synonyms: | n/a |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 1879554 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | MAP kinase-interacting serine/threonine-protein kinase 2 |
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| 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 |
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| Type: | Protein |
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| Mol. Mass.: | 51870.79 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q9HBH9 |
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| Residue: | 465 |
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| Sequence: | MVQKKPAELQGFHRSFKGQNPFELAFSLDQPDHGDSDFGLQCSARPDMPASQPIDIPDAK
KRGKKKKRGRATDSFSGRFEDVYQLQEDVLGEGAHARVQTCINLITSQEYAVKIIEKQPG
HIRSRVFREVEMLYQCQGHRNVLELIEFFEEEDRFYLVFEKMRGGSILSHIHKRRHFNEL
EASVVVQDVASALDFLHNKGIAHRDLKPENILCEHPNQVSPVKICDFDLGSGIKLNGDCS
PISTPELLTPCGSAEYMAPEVVEAFSEEASIYDKRCDLWSLGVILYILLSGYPPFVGRCG
SDCGWDRGEACPACQNMLFESIQEGKYEFPDKDWAHISCAAKDLISKLLVRDAKQRLSAA
QVLQHPWVQGCAPENTLPTPMVLQRNSCAKDLTSFAAEAIAMNRQLAQHDEDLAEEEAAG
QGQPVLVRATSRCLQLSPPSQSKLAQRRQRASLSSAPVVLVGDHA
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| Component 2 |
| Name: | MAP kinase-interacting serine/threonine-protein kinase 1 |
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| 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 |
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| Type: | Serine/threonine-protein kinase |
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| Mol. Mass.: | 51342.85 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q9BUB5 |
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| Residue: | 465 |
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| Sequence: | MVSSQKLEKPIEMGSSEPLPIADGDRRRKKKRRGRATDSLPGKFEDMYKLTSELLGEGAY
AKVQGAVSLQNGKEYAVKIIEKQAGHSRSRVFREVETLYQCQGNKNILELIEFFEDDTRF
YLVFEKLQGGSILAHIQKQKHFNEREASRVVRDVAAALDFLHTKDKVSLCHLGWSAMAPS
GLTAAPTSLGSSDPPTSASQVAGTTGIAHRDLKPENILCESPEKVSPVKICDFDLGSGMK
LNNSCTPITTPELTTPCGSAEYMAPEVVEVFTDQATFYDKRCDLWSLGVVLYIMLSGYPP
FVGHCGADCGWDRGEVCRVCQNKLFESIQEGKYEFPDKDWAHISSEAKDLISKLLVRDAK
QRLSAAQVLQHPWVQGQAPEKGLPTPQVLQRNSSTMDLTLFAAEAIALNRQLSQHEENEL
AEEPEALADGLCSMKLSPPCKSRLARRRALAQAGRGEDRSPPTAL
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| BDBM375315 |
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| n/a |
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| Name | BDBM375315 |
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| Synonyms: | (4-(3-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-6-yl)phenyl)(morpholino)methanone | US9908886, Example 2 |
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| Type | Small organic molecule |
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| Emp. Form. | C23H20N4O3 |
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| Mol. Mass. | 400.4299 |
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| SMILES | Oc1ccc(cc1)-c1cnc2cnc(cn12)-c1ccc(cc1)C(=O)N1CCOCC1 |
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| Structure | 
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