U0126 [Ligand Id: 5282] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL34704 (U-0126)
  • mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
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  • mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507]
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  • Malate dehydrogenase in Thermus thermophilus [ChEMBL: CHEMBL4255] [UniProtKB: P10584]
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  • MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
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  • mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750]
ChEMBL Inhibition of Mitogen activated protein kinase kinase 1 (MKK1) B 4.89 pIC50 13000 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
ChEMBL Inhibition of recombinant full length human N-terminal GST-tagged C-terminal His6-tagged MEK1 expressed in Escherichia coli using myelin basic protein as substrate in presence of activated BRAF and ERK2 by ELISA B 7.05 pIC50 89 nM IC50 Bioorg Med Chem (2016) 24: 4652-4659 [PMID:27515719]
ChEMBL Inhibition of MEK1 B 7.14 pIC50 72 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of the dual specificity kinase MEK-1 B 7.15 pIC50 70 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2839-2844 [PMID:9873633]
ChEMBL Inhibitory potency against mitogen activated protein kinase kinase 1 B 7.15 pIC50 70 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 1483-1486 [PMID:15006386]
mitogen-activated protein kinase kinase 2/Dual specificity mitogen-activated protein kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2964] [GtoPdb: 2063] [UniProtKB: P36507]
ChEMBL Inhibition of the dual specificity kinase MEK-2 B 7.22 pIC50 60 nM IC50 Bioorg. Med. Chem. Lett. (1998) 8: 2839-2844 [PMID:9873633]
ChEMBL Inhibition of MEK2 B 7.24 pIC50 58 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
Malate dehydrogenase in Thermus thermophilus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4255] [UniProtKB: P10584]
ChEMBL Inhibitory activity against malate dehydrogenase (MDH) from Thermus flavus B 4 pIC50 100000 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
ChEMBL Inhibition of p38-regulated activated kinase (Protein kinase PRAK) B 4.3 pIC50 50000 nM IC50 J. Med. Chem. (2003) 46: 1478-1483 [PMID:12672248]
ChEMBL Inhibition of His-tagged human PRAK expressed in Sf9 cells B 4.3 pIC50 50000 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL Inhibition of His-tagged human SAPK2a/p38 expressed in Escherichia coli B 4.26 pIC50 55000 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.7 pIC50 1995.26 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.7 pIC50 1995.26 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of human PKBalpha expressed in SF9 cells B 4.22 pIC50 60000 nM IC50 Biochem. J. (2000) 351: 95-105 [PMID:10998351]
B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056]
ChEMBL Inhibition of N-terminal GST-tagged human BRAF/MEK1/RAF1 Y340D/Y341D double mutant measured after 2 hrs in presence of ATP by TR-FRET assay B 6.6 pIC50 250 nM IC50 Bioorg. Med. Chem. (2016) 24: 3472-3482 [PMID:27288186]

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, 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]