compound 17d [PMID: 23099093] [Ligand Id: 8196] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2207198
  • BR serine/threonine kinase 2/BR serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • microtubule affinity regulating kinase 3/Serine/threonine-protein kinase c-TAK1 in Human [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
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  • TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
  • TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Mouse [ChEMBL: CHEMBL2189160] [GtoPdb: 2237] [UniProtKB: Q9WUN2]
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  • mitogen-activated protein kinase kinase kinase 7 in Human [GtoPdb: 2082] [UniProtKB: O43318]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
BR serine/threonine kinase 2/BR serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3]
ChEMBL Inhibition of BRSK2 B 5.72 pIC50 1900 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 B 6.2 pIC50 630 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
GtoPdb - - 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-73 [PMID:23099093]
ChEMBL Inhibition of IKKepsilon B 7.52 pIC50 30 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase MNK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL Inhibition of MNK1 B 4.72 pIC50 19000 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of Aurora B B 6.15 pIC50 700 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
microtubule affinity regulating kinase 3/Serine/threonine-protein kinase c-TAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5600] [GtoPdb: 2099] [UniProtKB: P27448]
GtoPdb - - 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-73 [PMID:23099093]
ChEMBL Inhibition of MARK3 B 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
GtoPdb - - 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-73 [PMID:23099093]
ChEMBL Inhibition of TBK1 by radiometry B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189160] [GtoPdb: 2237] [UniProtKB: Q9WUN2]
ChEMBL Inhibition of TBK1-mediated RANTES release in LPS-stimulated mouse RAW264.7 cells compound incubated for 30 mins prior LPS challenge measured after 6 hrs by ELISA B 7.24 pIC50 58 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-7173 [PMID:23099093]
mitogen-activated protein kinase kinase kinase 7 in Human [GtoPdb: 2082] [UniProtKB: O43318]
GtoPdb - - 7.92 pIC50 12 nM IC50 Bioorg Med Chem Lett (2012) 22: 7169-73 [PMID:23099093]

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]