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Target
Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) 344D]
Ligand
BDBM420274
Substrate
n/a
Meas. Tech.
MKNK1 Kinase High ATP Assay
IC50
<1.000±n/a nM
Citation
 Giese, A; Klar, U; Graham, K; Kettschau, G; Sülzle, D; Lienau, P; Petersen, K; LeFranc, J; Schmidt, N Pyrazolopyridinamines as MKNK1 and MKNK2 inhibitors US Patent  US10487092 Publication Date 11/26/2019 
Target
Name:
Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) 344D]
Synonyms:
Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) 344D] | Isoform 2 of MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D] | MAP kinase signal-integrating kinase 1 (MNK1) (T344D) | MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1) | MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1) (T344D) | MAP kinase-interacting serine/threonine-protein kinase 1 (MKNK1)(T344D) | MAP kinase-interacting serine/threonine-protein kinase 1 (MNK1a) [T344D] | MAP kinase-interacting serine/threonine-protein kinase 1 (T344D) | MKNK1 | MKNK1 (aa 1-424) T344D | MKNK1_HUMAN | MNK1 | MNK1a
Type:
Protein
Mol. Mass.:
47416.00
Organism:
Homo sapiens (Human)
Description:
Q9BUB5-2 with T344D
Residue:
424
Sequence:
MVSSQKLEKPIEMGSSEPLPIADGDRRRKKKRRGRATDSLPGKFEDMYKLTSELLGEGAYAKVQGAVSLQNGKEYAVKIIEKQAGHSRSRVFREVETLYQCQGNKNILELIEFFEDDTRFYLVFEKLQGGSILAHIQKQKHFNEREASRVVRDVAAALDFLHTKGIAHRDLKPENILCESPEKVSPVKICDFDLGSGMKLNNSCTPITTPELTTPCGSAEYMAPEVVEVFTDQATFYDKRCDLWSLGVVLYIMLSGYPPFVGHCGADCGWDRGEVCRVCQNKLFESIQEGKYEFPDKDWAHISSEAKDLISKLLVRDAKQRLSAAQVLQHPWVQGQAPEKGLPDPQVLQRNSSTMDLTLFAAEAIALNRQLSQHEENELAEEPEALADGLCSMKLSPPCKSRLARRRALAQAGRGEDRSPPTAL
  
Inhibitor
Name:
BDBM420274
Synonyms:
(7S)-4-[(6-Methoxypyrazolo[1,5-a]pyridin-5-yl)amino]-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-7-yl[(1R,4R)-5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl]methanone | US10487092, Example 122
Type:
Small organic molecule
Emp. Form.:
C25H27N7O2S
Mol. Mass.:
489.593
SMILES:
COc1cn2nccc2cc1Nc1ncnc2sc3C[C@H](CCc3c12)C(=O)N1C[C@H]2C[C@@H]1CN2C |r,THB:34:33:27.28:30,25:27:32.33:30|
Structure:
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