MNK1 inhibitor [Ligand Id: 6010] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1240885 (CGP-57380)
  • BR serine/threonine kinase 2/BR serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3]
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  • casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
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  • dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
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  • LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BR serine/threonine kinase 2/BR serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3]
ChEMBL Inhibition of BRSK2 in the presence of 50uM ATP B 5.96 pIC50 1100 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730]
ChEMBL Inhibition of CK1delta in the presence of 20uM ATP B 6.29 pIC50 510 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
ChEMBL Inhibition of CDK9/cyclinT1 (unknown origin) using TAMRA-labeled eIF4E peptide as substrate incubated for 10 mins followed by addition of ATP measured after 90 mins by IMAP TR-FRET analysis B 5 pKi >10000 nM Ki Eur. J. Med. Chem. (2015) 103: 539-550 [PMID:26408454]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248P24941P78396]
ChEMBL Inhibition of CDK2/cyclinA (unknown origin) using TAMRA-labeled eIF4E peptide as substrate incubated for 10 mins followed by addition of ATP measured after 90 mins by IMAP TR-FRET analysis B 5 pKi >10000 nM Ki Eur. J. Med. Chem. (2015) 103: 539-550 [PMID:26408454]
dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
ChEMBL Inhibition of DYRK3 in the presence of 5uM ATP B 5.49 pIC50 3200 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 5.3 pIC50 5000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4108-4114 [PMID:21632247]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL Inhibition of Mnk1 (unknown origin) pre-incubated for 10 mins before eIF4E peptide substrate addition by ADP-Glo kinase assay B 6 pKi 1010 nM Ki Eur. J. Med. Chem. (2015) 95: 116-126 [PMID:25800647]
ChEMBL Inhibition of Mnk1a (unknown origin) using TAMRA-labeled eIF4E peptide as substrate incubated for 10 mins followed by addition of ATP measured after 90 mins by IMAP TR-FRET analysis B 6 pKi 1010 nM Ki Eur. J. Med. Chem. (2015) 103: 539-550 [PMID:26408454]
ChEMBL Inhibition of human MNK1 using CREBtide substrate by gamma-[32P]-ATP competitive inhibition assay B 5.56 pIC50 2740 nM IC50 Bioorg Med Chem (2019) 27: 2268-2279 [PMID:31014565]
GtoPdb - - 6.06 pIC50 870 nM IC50 J Med Chem (2010) 53: 6618-28 [PMID:20722422]
ChEMBL Inhibition of MNK1 in the presence of 50uM ATP B 6.06 pIC50 870 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of MNK1 B 6.06 pIC50 870 nM IC50 J. Med. Chem. (2010) 53: 6618-6628 [PMID:20722422]
ChEMBL Inhibition of Mnk1a (unknown origin) using TAMRA-labeled eIF4E peptide as substrate incubated for 10 mins followed by addition of ATP measured after 90 mins by IMAP TR-FRET analysis B 6.06 pIC50 870 nM IC50 Eur. J. Med. Chem. (2015) 103: 539-550 [PMID:26408454]
ChEMBL Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis B 6.06 pIC50 870 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL Inhibition of MNK1 (unknown origin) using S3 as substrate measured after 60 mins by HTRF assay B 6.07 pIC50 850 nM IC50 Bioorg Med Chem (2018) 26: 4602-4614 [PMID:30115493]
MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL Inhibition of Mnk2 (unknown origin) pre-incubated for 10 mins before eIF4E peptide substrate addition by ADP-Glo kinase assay B 6.06 pKi 880 nM Ki Eur. J. Med. Chem. (2015) 95: 116-126 [PMID:25800647]
ChEMBL Inhibition of human Mnk2a using TAMRA-labeled eIF4E peptide as substrate incubated for 10 mins followed by addition of ATP measured after 90 mins by IMAP TR-FRET analysis B 6.47 pKi 340 nM Ki Eur. J. Med. Chem. (2015) 103: 539-550 [PMID:26408454]
ChEMBL Inhibition of MNK2 in the presence of 50uM ATP B 5.8 pIC50 1600 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of MNK2 B 5.8 pIC50 1600 nM IC50 J. Med. Chem. (2010) 53: 6618-6628 [PMID:20722422]
ChEMBL Inhibition of human Mnk2a using TAMRA-labeled eIF4E peptide as substrate incubated for 10 mins followed by addition of ATP measured after 45 mins by ADP-Glo kinase assay B 5.8 pIC50 1600 nM IC50 Eur. J. Med. Chem. (2015) 103: 539-550 [PMID:26408454]
ChEMBL Inhibition of MNK2 (unknown origin) B 5.8 pIC50 1600 nM IC50 Bioorg Med Chem (2018) 26: 4602-4614 [PMID:30115493]
ChEMBL Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis B 5.8 pIC50 1600 nM IC50 Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
GtoPdb - - 5.8 pIC50 1600 nM IC50 J Med Chem (2010) 53: 6618-28 [PMID:20722422]
ChEMBL Inhibition of MNK2 (unknown origin) using S3 as substrate measured after 60 mins by HTRF assay B 5.82 pIC50 1530 nM IC50 Bioorg Med Chem (2018) 26: 4602-4614 [PMID:30115493]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of Aurora B in the presence of 20uM ATP B 5.6 pIC50 2500 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141]
ChEMBL Inhibition of SGK1 in the presence of 20uM ATP B 5.57 pIC50 2700 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]
ChEMBL Inhibition of SGK1 B 5.57 pIC50 2700 nM IC50 J. Med. Chem. (2010) 53: 6618-6628 [PMID:20722422]
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240]
ChEMBL Inhibition of Lck in the presence of 50uM ATP B 5.6 pIC50 2500 nM IC50 Biochem. J. (2007) 408: 297-315 [PMID:17850214]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]