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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 | 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 | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2006) 49: 4805-4808 [PMID:16884290] |
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 (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] |
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] |
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] |
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 Aurora-B (unknown origin) | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem (2014) 22: 5813-5823 [PMID:25270403] |
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 aurora B kinase | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2009) 52: 2629-2651 [PMID:19320489] |
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 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] |
GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | J Cell Biol (2003) 161: 267-80 [PMID:12719470] |
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 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]