ChEMBL ligand: CHEMBL1240885 (CGP-57380)
BR serine/threonine kinase 2/BR serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3] There should be some charts here, you may need to enable JavaScript!
casein kinase 1 delta/Casein kinase I delta in Human [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 9/CDK9/cyclin T1 in Human [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] There should be some charts here, you may need to enable JavaScript!
dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781] There should be some charts here, you may need to enable JavaScript!
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525] 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 MNK1 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 signal-integrating kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] There should be some charts here, you may need to enable JavaScript!
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] There should be some charts here, you may need to enable JavaScript!
serum/glucocorticoid regulated kinase 1/Serine/threonine-protein kinase Sgk1 in Human [ChEMBL: CHEMBL2343] [GtoPdb: 1534] [UniProtKB: O00141] There should be some charts here, you may need to enable JavaScript!
LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Mouse [ChEMBL: CHEMBL2480] [GtoPdb: 2053] [UniProtKB: P06240] 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
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]