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ChEMBL ligand: CHEMBL202721 (TCMDC-125873, ZM-447439) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]