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Target
MAP kinase-interacting serine/threonine-protein kinase 1
Ligand
BDBM375313
Substrate
n/a
Meas. Tech.
ChEMBL_1754736 (CHEMBL4189496)
IC50
284±n/a nM
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 Chem 61:4348-4369 (2018) [PubMed]  Article
Target
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:
MVSSQKLEKPIEMGSSEPLPIADGDRRRKKKRRGRATDSLPGKFEDMYKLTSELLGEGAYAKVQGAVSLQNGKEYAVKIIEKQAGHSRSRVFREVETLYQCQGNKNILELIEFFEDDTRFYLVFEKLQGGSILAHIQKQKHFNEREASRVVRDVAAALDFLHTKDKVSLCHLGWSAMAPSGLTAAPTSLGSSDPPTSASQVAGTTGIAHRDLKPENILCESPEKVSPVKICDFDLGSGMKLNNSCTPITTPELTTPCGSAEYMAPEVVEVFTDQATFYDKRCDLWSLGVVLYIMLSGYPPFVGHCGADCGWDRGEVCRVCQNKLFESIQEGKYEFPDKDWAHISSEAKDLISKLLVRDAKQRLSAAQVLQHPWVQGQAPEKGLPTPQVLQRNSSTMDLTLFAAEAIALNRQLSQHEENELAEEPEALADGLCSMKLSPPCKSRLARRRALAQAGRGEDRSPPTAL
  
Inhibitor
Name:
BDBM375313
Synonyms:
(4-(3-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-6-yl)phenyl)(4-methylpiperazin-1-yl)methanone | US9908886, Example 1
Type:
Small organic molecule
Emp. Form.:
C24H23N5O2
Mol. Mass.:
413.4717
SMILES:
CN1CCN(CC1)C(=O)c1ccc(cc1)-c1cn2c(cnc2cn1)-c1ccc(O)cc1
Structure:
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