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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 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]