5Z-7-oxozeaenol [Ligand Id: 8077] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1077979 ((5Z)-7-Oxozeaenol, 5Z-7-Oxozeaenol) |
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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 MAP2K1 (unknown origin) using unphosphorylated GST-tagged ERK2 substrate protein assessed as phosphorylation by ELISA | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 593-596 [PMID:25529738] |
| ChEMBL | Inhibition of MEK1 | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2012) 55: 6243-6262 [PMID:22621397] |
| ChEMBL | Inhibition of full length recombinant human His-tagged MEK1 expressed in baculovirus expression system after 1 hr by TR-FRET based LanthaScreen assay | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem (2017) 25: 838-846 [PMID:28011204] |
| mitogen-activated protein kinase kinase 4/Dual specificity mitogen-activated protein kinase kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2897] [GtoPdb: 2065] [UniProtKB: P45985] | ||||||||
| ChEMBL | Inhibition of MKK4 | B | 5.52 | pIC50 | >3000 | nM | IC50 | J Med Chem (2012) 55: 6243-6262 [PMID:22621397] |
| mitogen-activated protein kinase kinase 7/Dual specificity mitogen-activated protein kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3530] [GtoPdb: 2068] [UniProtKB: O14733] | ||||||||
| ChEMBL | Inhibition of MAP2K7 (unknown origin) using unphosphorylated GST-tagged JNK1 substrate protein assessed as phosphorylation by ELISA | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 593-596 [PMID:25529738] |
| ChEMBL | Inhibition of MEK7 | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2012) 55: 6243-6262 [PMID:22621397] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Inhibition of ERK2 (unknown origin) using FITC-labeled substrate peptide assessed as phosphorylation | B | 5.17 | pIC50 | 6800 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 593-596 [PMID:25529738] |
| ChEMBL | Inhibition of full length recombinant human GST-tagged ERK2 expressed in Escherichia coli using Ser/Thr 03 as substrate after 1 hr by Z'-Lyte assay | B | 6.13 | pIC50 | 738 | nM | IC50 | Bioorg Med Chem (2017) 25: 838-846 [PMID:28011204] |
| ChEMBL | Inhibition of Erk2 | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2012) 55: 6243-6262 [PMID:22621397] |
| mitogen-activated protein kinase kinase kinase 7/Mitogen-activated protein kinase kinase kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5776] [GtoPdb: 2082] [UniProtKB: O43318] | ||||||||
| ChEMBL | Inhibition of TAK1 (unknown origin) using unphosphorylated GST-tagged MAP2K7 substrate protein assessed as phosphorylation by ELISA | B | 7.1 | pIC50 | 80 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 593-596 [PMID:25529738] |
| ChEMBL | Inhibition of TAK1 (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2015) 23: 6993-6999 [PMID:26481152] |
| ChEMBL | Inhibition of full length TAK1 (unknown origin) fused with TAB1 using biotin-MKK6 as substrate by AlphaScreen assay | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem (2016) 24: 4206-4217 [PMID:27448772] |
| GtoPdb | Assayed using TAK1/TAB1 (TAK1-binding protein 1) fusion protein for full enzymatic activity. Inhibition of kinase activity. | - | 8.05 | pIC50 | 9 | nM | IC50 |
ACS Chem Biol (2013) 8: 643-50 [PMID:23272696]; J Med Chem (2012) 55: 6243-62 [PMID:22621397] |
| ChEMBL | Inhibition of TAK1 (unknown origin) expressed in sf9 cells assessed as 32P level incorporation into myelin basic protein incubated for 5 mins at 30 degC by immunoprecipitation method | B | 8.09 | pIC50 | 8.1 | nM | IC50 | Bioorg Med Chem (2015) 23: 6993-6999 [PMID:26481152] |
| ChEMBL | Inhibition of full length recombinant human GST-tagged TAK1 expressed in baculovirus expression system after 1 hr by TR-FRET based LanthaScreen assay | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Bioorg Med Chem (2017) 25: 838-846 [PMID:28011204] |
| ChEMBL | Inhibition of TAK1 (unknown origin) by LanthaScreen assay | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Bioorg Med Chem (2017) 25: 1320-1328 [PMID:28038940] |
| Nuclear factor NF-kappa-B p65 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5533] [UniProtKB: Q04206] | ||||||||
| ChEMBL | Inhibition of NFkappa p65 isolated from nuclear extract of human HeLa cells by ELISA | B | 6.6 | pIC50 | 250 | nM | IC50 | J Nat Prod (2011) 74: 1126-1131 [PMID:21513293] |
| Phospholipase A-2-activating protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6114] [UniProtKB: Q9Y263] | ||||||||
| ChEMBL | Inhibition of TNFalpha-PLAP (unknown origin) | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2017) 60: 839-885 [PMID:27996267] |
| mitogen-activated protein kinase kinase kinase 7/TAK1/TAB1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038499] [GtoPdb: 2082] [UniProtKB: O43318, Q15750] | ||||||||
| ChEMBL | Inhibition of full length TAK1/TAB1 (unknown origin) using biotin-MKK6 as substrate by AlphaScreen assay | B | 8.05 | pIC50 | 9 | nM | IC50 | Eur J Med Chem (2019) 163: 660-670 [PMID:30576901] |
| GtoPdb | Assayed using TAK1/TAB1 (TAK1-binding protein 1) fusion protein for full enzymatic activity. Inhibition of kinase activity. | - | 8.05 | pIC50 | 9 | nM | IC50 |
ACS Chem Biol (2013) 8: 643-50 [PMID:23272696]; J Med Chem (2012) 55: 6243-62 [PMID:22621397] |
| ChEMBL | Competitive inhibition of recombinant TAK1-TAB1 assessed as [33P]gamma-ATP incorporation into substrate histone H1 peptide by filter plate assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1724-1727 [PMID:21316225] |
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]
