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ChEMBL ligand: CHEMBL259551 (FR-180204) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
GtoPdb | - | - | 6.39 | pKi | 410 | nM | Ki | Biochem Biophys Res Commun (2005) 336: 357-63 [PMID:16139248] |
ChEMBL | Inhibition of ERK1 | B | 6.51 | pKi | 310 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Binding affinity to ERK1 | B | 6.51 | pKi | 310 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
ChEMBL | Binding affinity to ERK2 (unknown origin) by isothermal titration calorimetry | B | 6.07 | pKd | 850 | nM | Kd | J Med Chem (2013) 56: 2155-2159 [PMID:23419007] |
ChEMBL | Inhibition of ERK2 | B | 6.51 | pKi | 310 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Binding affinity to ERK2 | B | 6.51 | pKi | 310 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
GtoPdb | - | - | 6.85 | pKi | 140 | nM | Ki | Biochem Biophys Res Commun (2005) 336: 357-63 [PMID:16139248] |
ChEMBL | Inhibitory activity against human ERK2 | B | 5.72 | pIC50 | 1900 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 55-58 [PMID:16242327] |
ChEMBL | Inhibition of phosphorylated ERK2 (unknown origin) using myelin basic protein as substrate after 2 hrs in presence of ATP by ADP-glo assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | ACS Med Chem Lett (2017) 8: 726-731 [PMID:28740606] |
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
ChEMBL | Inhibition of p38alpha | B | 6.51 | pKi | 310 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
mitogen-activated protein kinase 6/Mitogen-activated protein kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5121] [GtoPdb: 2092] [UniProtKB: Q16659] | ||||||||
ChEMBL | Binding affinity to LPP-dephosphorylated recombinant wild-type ERK3 (9 to 327 residues) (unknown origin) expressed in Escherichia coli by microscale thermophoresis assay | B | 5 | pKd | >10000 | nM | Kd | Bioorg Med Chem Lett (2020) 30: 127551-127551 [PMID:32927028] |
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]