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 MEK1 (unknown origin) | B | 7.14 | pIC50 | 72 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of MEK1 (unknown origin) | B | 7.14 | pIC50 | 72 | nM | IC50 | J Med Chem (2022) 65: 935-954 [PMID:33970631] |
| 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] |
| ChEMBL | Inhibition of MEK2 (unknown origin) | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| ChEMBL | Inhibition of MEK2 (unknown origin) | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2022) 65: 935-954 [PMID:33970631] |
| 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 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]
