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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 |
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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 initation factor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4848] [UniProtKB: P06730] | ||||||||
ChEMBL | Inhibition of eIF4E phosphorylation in HEK293 cells incubated for 60 mins by Western blot assay | B | 5.52 | pIC50 | 3000 | nM | IC50 | Eur J Med Chem (2021) 219: 113420-113420 [PMID:33892273] |
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] |
ChEMBL | Inhibition of MNK1 in HEK293 cells | B | 5.66 | pIC50 | 2200 | nM | IC50 | Eur J Med Chem (2021) 219: 113420-113420 [PMID:33892273] |
ChEMBL | Inhibition of human recombinant full length GST-tagged MNK1 expressed in baculovirus expression system using S6 peptide as substrate in presence of [gamma-33P]-ATP incubated for 60 mins by radiometric scintillation counting method | B | 5.82 | pIC50 | 1520 | nM | IC50 | J Med Chem (2022) 65: 6070-6087 [PMID:35417652] |
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 (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 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 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 MNK1 (unknown origin) using eIF4E as a substrate in presence of ATP | B | 6.06 | pIC50 | 870 | nM | IC50 | Eur J Med Chem (2021) 219: 113420-113420 [PMID:33892273] |
ChEMBL | Inhibition of human His6-tagged Mnk1 expressed in Escherichia coli assessed as phosphorylation of eukaryotic translation initiation factor 4E | B | 6.06 | pIC50 | 870 | nM | IC50 | J Med Chem (2022) 65: 983-1007 [PMID:34533957] |
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 human recombinant full length GST-tagged MNK2 expressed in insect cells using S6 peptide as substrate in presence of [gamma-33P]-ATP incubated for 60 mins by by radiometric scintillation counting method | B | 5.2 | pIC50 | 6270 | nM | IC50 | J Med Chem (2022) 65: 6070-6087 [PMID:35417652] |
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 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) using eIF4E as a substrate in presence of ATP | B | 5.8 | pIC50 | 1600 | nM | IC50 | Eur J Med Chem (2021) 219: 113420-113420 [PMID:33892273] |
ChEMBL | Inhibition of human His6-tagged Mnk2 expressed in Escherichia coli assessed as phosphorylation of eukaryotic translation initiation factor 4E | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2022) 65: 983-1007 [PMID:34533957] |
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 34:
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]