ZM447439 [Ligand Id: 8353] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL202721 (TCMDC-125873, ZM-447439)
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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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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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aurora kinase B-A in Xenopus laevis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176838] [UniProtKB: Q6DE08]
ChEMBL Inhibition of Xenopus laevis Aurora kinase B/INCEP complex using gamma-[32P]ATP incubated for 1 hr by autoradiography B 7.35 pIC50 45 nM IC50 J Med Chem (2012) 55: 7841-7848 [PMID:22920039]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Inhibition of in vitro CDK1 kinase activity B 5 pIC50 >10000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR (unknown origin) measured after 40 mins by Kinase Glo luminescence assay B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2017) 130: 393-405 [PMID:28279846]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Multi-Cycle Kinetic parameter establishment of 8 compounds to gain n=3Completed over 3 identical immbolized CM5 chips B 6.86 pKd 138.4 nM Kd K4DD drug target binding kinetics data
ChEMBL Multi-Cycle Kinetic parameter establishment of 8 compounds to gain n=3 Completed over 3 identical immbolized CM5 chips B 7.07 pKd 86.03 nM Kd K4DD drug target binding kinetics data
ChEMBL Inhibition of human Aurora kinase A/TPX2 complex using gamma-[32P]ATP incubated for 1 hr by autoradiography B 6.44 pIC50 360 nM IC50 J Med Chem (2012) 55: 7841-7848 [PMID:22920039]
ChEMBL Inhibition of Aurora-A (unknown origin) using STK substrate 2-biotin by HTRF-KinEASE-STK assay B 6.86 pIC50 138 nM IC50 Bioorg Med Chem (2014) 22: 5813-5823 [PMID:25270403]
ChEMBL Inhibition of aurora A kinase B 6.96 pIC50 110 nM IC50 J Med Chem (2009) 52: 2629-2651 [PMID:19320489]
ChEMBL Inhibitory activity against Aurora A B 6.96 pIC50 110 nM IC50 Bioorg Med Chem Lett (2006) 16: 1320-1323 [PMID:16337122]
ChEMBL Inhibition of Aurora A B 6.96 pIC50 110 nM IC50 J Med Chem (2006) 49: 4805-4808 [PMID:16884290]
ChEMBL Inhibition of human recombinant His6-tagged Aurora A expressed in baculovirus using Biotinyl-Ahx-tetra (LRRWSLG) as substrate incubated for 60 mins by beta scintillation counter B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2019) 170: 55-72 [PMID:30878832]
ChEMBL Inhibition of AURKA (unknown origin) B 6.96 pIC50 110 nM IC50 Bioorg Med Chem (2020) 28: 115525-115525 [PMID:32371117]
ChEMBL Inhibition of Aurora-A (unknown origin) B 6.96 pIC50 110 nM IC50 Bioorg Med Chem (2014) 22: 5813-5823 [PMID:25270403]
ChEMBL Inhibition of Aurora A kinase (unknown origin) B 6.96 pIC50 110 nM IC50 Eur J Med Chem (2017) 140: 1-19 [PMID:28918096]
GtoPdb - - 7 pIC50 100 nM IC50 J Cell Biol (2003) 161: 267-80 [PMID:12719470]
ChEMBL Inhibition of in vitro Aurora-A kinase activity B 7 pIC50 100 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
ChEMBL Inhibition of human Aurora A kinase B 7 pIC50 100 nM IC50 Eur J Med Chem (2021) 211: 113016-113016 [PMID:33243532]
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 (unknown origin) using STK substrate 2-biotin by HTRF-KinEASE-STK assay B 6.81 pIC50 156 nM IC50 Bioorg Med Chem (2014) 22: 5813-5823 [PMID:25270403]
ChEMBL Inhibition of Aurora B (unknown origin) measured after 40 mins by Kinase Glo luminescence assay B 6.81 pIC50 156 nM IC50 Eur J Med Chem (2017) 130: 393-405 [PMID:28279846]
ChEMBL Inhibition of AURKB (unknown origin) B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2020) 28: 115525-115525 [PMID:32371117]
ChEMBL Inhibition of human recombinant His6-tagged Aurora B expressed in baculovirus using Biotinyl-Ahx-tetra (LRRWSLG) as substrate incubated for 60 mins by beta scintillation counter B 6.89 pIC50 130 nM IC50 Eur J Med Chem (2019) 170: 55-72 [PMID:30878832]
ChEMBL Inhibition of Aurora-B (unknown origin) B 6.89 pIC50 130 nM IC50 Bioorg Med Chem (2014) 22: 5813-5823 [PMID:25270403]
ChEMBL Inhibition of recombinant aurora B (unknown origin) B 6.89 pIC50 130 nM IC50 Eur J Med Chem (2017) 140: 1-19 [PMID:28918096]
ChEMBL Inhibition of aurora B kinase B 6.89 pIC50 130 nM IC50 J Med Chem (2009) 52: 2629-2651 [PMID:19320489]
GtoPdb - - 7 pIC50 100 nM IC50 J Cell Biol (2003) 161: 267-80 [PMID:12719470]
ChEMBL Inhibition of human Aurora B kinase B 7 pIC50 100 nM IC50 Eur J Med Chem (2021) 211: 113016-113016 [PMID:33243532]
ChEMBL Inhibition of in vitro Aurora-B kinase activity B 7 pIC50 100 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]
ChEMBL Inhibition of human Aurora kinase B/INCEP complex expressed in Escherichia coli BL21 (DE3) using gamma-[32P]ATP incubated for 1 hr by autoradiography B 7.29 pIC50 51 nM IC50 J Med Chem (2012) 55: 7841-7848 [PMID:22920039]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
ChEMBL Inhibition of in vitro Plk1 kinase activity B 5 pIC50 >10000 nM IC50 J Med Chem (2006) 49: 955-970 [PMID:16451062]

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]