ZM447439 [Ligand Id: 8353] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL202721 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| aurora kinase A/Aurora kinase 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 recombinant Aurora A (unknown origin) expressing NH2-terminal His6-tag in baculovirus expression system using Biotinyl-Ahx-tetra (LRRWSLG) as substrate incubated for 60 mins measured by betaplate counter analysis | B | 6.96 | pIC50 | 110 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| ChEMBL | Inhibition of Aurora A | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2006) 49: 4805-4808 [PMID:16884290] |
| ChEMBL | Inhibition of N terminal his tagged recombinant Aurora A (unknown origin) expressed in baculovirus expression system incubated for 60 mins in presence of ATP | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2024) 268: 116255-116255 [PMID:38401190] |
| 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] |
| ChEMBL | Inhibition of AURKA (unknown origin) | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2020) 28: 115525-115525 [PMID:32371117] |
| 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/Aurora kinase 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 recombinant Aurora B (unknown origin) expressing NH2-terminal His6-tag in baculovirus expression system using Biotinyl-Ahx-tetra (LRRWSLG) as substrate incubated for 60 mins measured by betaplate counter analysis | B | 6.89 | pIC50 | 130 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| 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 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 AURKB (unknown origin) | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem (2020) 28: 115525-115525 [PMID:32371117] |
| ChEMBL | Inhibition of N terminal his tagged recombinant Aurora B (unknown origin) expressed in baculovirus expression system incubated for 60 mins in presence of ATP | B | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2024) 268: 116255-116255 [PMID:38401190] |
| 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] |
| 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 B kinase | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2021) 211: 113016-113016 [PMID:33243532] |
| 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] |
| 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] |
| ChEMBL | Inhibition of recombinant CDK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of recombinant CDK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Inhibition of recombinant CDK4 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| mitogen-activated protein kinase kinase 1/Dual specificity mitogen-activated protein kinase kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3587] [GtoPdb: 2062] [UniProtKB: Q02750] | ||||||||
| ChEMBL | Inhibition of recombinant MEK1 (unknown origin) | B | 5.75 | pIC50 | 1790 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Inhibition of MPS1 in human taxol-arrested U2OS cells assessed as effect on histone H3 phosphorylation at ser10 residue incubated for 2 hrs by arrayscan analysis | B | 5.64 | pEC50 | 2280 | nM | EC50 | Cancer Res (2010) 70: 10255-10264 [PMID:21159646] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Binding affinity to human partial length EGFR (R669 to V1011 residues) L858R mutant expressed in bacterial expression system assessed as dissociation constant by DiscoverX kinomescan assay | B | 6.06 | pKd | 880 | nM | Kd | Bioorg Med Chem Lett (2024) 100: 129612-129612 [PMID:38199330] |
| ChEMBL | Binding affinity to wild type human EGFR partial length (R669 to V1011 residues) expressed in bacterial expression system assessed as dissociation constant by DiscoverX kinomescan assay | B | 6.66 | pKd | 220 | nM | Kd | Bioorg Med Chem Lett (2024) 100: 129612-129612 [PMID:38199330] |
| 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] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of recombinant FLT2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Inhibition of recombinant FAK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa-B kinase subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111] | ||||||||
| ChEMBL | Inhibition of recombinant IKK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
| ChEMBL | Inhibition of recombinant IKK2 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| SRC proto-oncogene, non-receptor tyrosine kinase/Proto-oncogene tyrosine-protein kinase Src in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931] | ||||||||
| ChEMBL | Inhibition of recombinant SRC (unknown origin) | B | 6.06 | pIC50 | 880 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of recombinant CHK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| 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 | Inhibition of recombinant PLK1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Inhibition of recombinant LCK (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of recombinant ZAP70 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Cell Biol (2003) 161: 267-280 [PMID:12719470] |
ChEMBL data shown on this page come from version 36:
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]
