ChEMBL ligand: CHEMBL4211649 (Aum001, AUM-001, ETC1907206, Etc-206, Tinodasertib)
Eukaryotic translation initiation factor 4E in Human [ChEMBL: CHEMBL4848] [UniProtKB: P06730] There should be some charts here, you may need to enable JavaScript!
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5] There should be some charts here, you may need to enable JavaScript!
MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Eukaryotic translation initiation factor 4E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4848] [UniProtKB: P06730]
ChEMBL	Inhibition of eIF4E phosphorylation at ser209 residue in human HeLa cells incubated for 2 hrs by HTRF assay	B	6.19	pIC50	646.2	nM	IC50	J Med Chem (2024) 67: 5437-5457 [PMID:38564512]
ChEMBL	Inhibition of eIF4E phosphorylation in human HeLa cells	B	6.49	pIC50	321	nM	IC50	RSC Med Chem (2023) 14: 1060-1087 [PMID:37360400]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL	In Vitro Kinase Assay: MNK1 and MNK2 inhibitor activity was determined using recombinant kinase domains expressed in E. coli. MNK1 and MNK2 were expressed as GST fusion proteins and the GST tag was removed using PreScission protease. After concentration to 10-15 mg/ml the proteins were flash frozen in liquid nitrogen and stored at −80° C. MNK1 and MNK2 were activated using recombinant ERK2 which was activated using a constitutively active mutant of MEK1, both ERK2 and MEK1 were expressed in E. coli as N-terminally his tagged proteins. Recombinant ERK2 was activated by incubating 11.3 μM of the kinase with 1 μM MEK1 and 100 μM ATP. This reaction mixture was then used immediately for the activation of the MNKs. The activation of the MNK1 was performed by incubating 5.0 μM of MNK1 with 0.3 μM of activated ERK2 and 500 μM ATP at 30° C. for 6 hours. The activation of MNK2 was performed by incubating 50 μM of MNK2 with 3.0 μM of activated ERK2 and 500 μM ATP at 30° C. for 2 hours. The activated MNKs were stored at −20° C. until required for assay.	B	7	pIC50	<100	nM	IC50	US-9908886-B2. Bicyclic heterocyclic derivatives as MNK1 and MNK2 modulators and uses thereof (2018)
GtoPdb	-	-	7.19	pIC50	64	nM	IC50	J Med Chem (2018) 61: 4348-4369 [PMID:29683667]
ChEMBL	Inhibition of GST-tagged MNK1 (37 to 341 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using JH3 peptide as substrate preincubated for 10 mins followed by substrate and ATP addition measured after 60 mins	B	7.19	pIC50	64	nM	IC50	J Med Chem (2018) 61: 4348-4369 [PMID:29683667]
ChEMBL	Inhibition of MNK1 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis	B	7.19	pIC50	64	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL	Inhibition of MNK1 (unknown origin)	B	7.19	pIC50	64	nM	IC50	RSC Med Chem (2023) 14: 1060-1087 [PMID:37360400]
ChEMBL	Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	B	7.65	pIC50	22.4	nM	IC50	J Med Chem (2024) 67: 5437-5457 [PMID:38564512]
ChEMBL	Inhibition of N-terminal GST-fused human full length recombinant MNK1 (1 to 424 residues) expressed in baculovirus-infected Sf21 cells using TATKSGSTTKNR as substrate preincubated with enzyme and substrate for 10 mins followed by ATP addition and measured after 40 mins by ADP-glo luminescence assay	B	7.97	pIC50	10.6	nM	IC50	Bioorg Med Chem (2021) 40: 116186-116186 [PMID:33971490]
MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL	In Vitro Kinase Assay: MNK1 and MNK2 inhibitor activity was determined using recombinant kinase domains expressed in E. coli. MNK1 and MNK2 were expressed as GST fusion proteins and the GST tag was removed using PreScission protease. After concentration to 10-15 mg/ml the proteins were flash frozen in liquid nitrogen and stored at −80° C. MNK1 and MNK2 were activated using recombinant ERK2 which was activated using a constitutively active mutant of MEK1, both ERK2 and MEK1 were expressed in E. coli as N-terminally his tagged proteins. Recombinant ERK2 was activated by incubating 11.3 μM of the kinase with 1 μM MEK1 and 100 μM ATP. This reaction mixture was then used immediately for the activation of the MNKs. The activation of the MNK1 was performed by incubating 5.0 μM of MNK1 with 0.3 μM of activated ERK2 and 500 μM ATP at 30° C. for 6 hours. The activation of MNK2 was performed by incubating 50 μM of MNK2 with 3.0 μM of activated ERK2 and 500 μM ATP at 30° C. for 2 hours. The activated MNKs were stored at −20° C. until required for assay.	B	7	pIC50	<100	nM	IC50	US-9908886-B2. Bicyclic heterocyclic derivatives as MNK1 and MNK2 modulators and uses thereof (2018)
ChEMBL	Inhibition of GST-tagged MNK2 (72 to 385 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using JH3 peptide as substrate preincubated for 10 mins followed by substrate and ATP addition measured after 60 mins	B	7.07	pIC50	86	nM	IC50	J Med Chem (2018) 61: 4348-4369 [PMID:29683667]
ChEMBL	Inhibition of MNK2 (unknown origin) expressed in HEK293 cells assessed as decrease in eIF4E phosphorylation at Ser209 residues by Western blot analysis	B	7.07	pIC50	86	nM	IC50	Eur J Med Chem (2019) 163: 413-427 [PMID:30530193]
ChEMBL	Inhibition of MNK2 (unknown origin)	B	7.07	pIC50	86	nM	IC50	RSC Med Chem (2023) 14: 1060-1087 [PMID:37360400]
GtoPdb	-	-	7.07	pIC50	86	nM	IC50	J Med Chem (2018) 61: 4348-4369 [PMID:29683667]
ChEMBL	Inhibition of recombinant MNK2 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay	B	7.63	pIC50	23.5	nM	IC50	J Med Chem (2024) 67: 5437-5457 [PMID:38564512]
ChEMBL	Inhibition of N-terminal GST-fused human full length recombinant MNK2 (1 to 465 residues) expressed in baculovirus-infected Sf21 cells using TATKSGSTTKNR as substrate preincubated with enzyme and substrate for 10 mins followed by ATP addition and measured after 40 mins by ADP-glo luminescence assay	B	8.03	pIC50	9.4	nM	IC50	Bioorg Med Chem (2021) 40: 116186-116186 [PMID:33971490]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]