U0126 [Ligand Id: 5282] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL34704 (U-0126) |
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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 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]
