MNK1 inhibitor [Ligand Id: 6010] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1240885 (CGP-57380) |
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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: O60563, P50750] | ||||||||
| 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: P20248, P24941, P78396] | ||||||||
| 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 MKN1 (unknown origin) in presence of ATP by HTRF assay | B | 6.06 | pIC50 | 870 | nM | IC50 | J Med Chem (2021) 64: 13719-13735 [PMID:34515481] |
| 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 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 (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 (unknown origin) | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem (2018) 26: 4602-4614 [PMID:30115493] |
| 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 in the presence of 50uM ATP | B | 5.8 | pIC50 | 1600 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| ChEMBL | Inhibition of MKN2 (unknown origin) in presence of ATP by HTRF assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2021) 64: 13719-13735 [PMID:34515481] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
