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ChEMBL ligand: CHEMBL502124 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of CDK2/cyclin A | B | 4.8 | pIC50 | >16000 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
ChEMBL | Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
ChEMBL | Inhibition of N-terminal flag-tagged Aurora A T217E mutant expressed in Escherichia coli BL21-DE3 | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
ChEMBL | Inhibition of Aurora A in human HCT116 cells assessed as complete failure of centrosome seperation by immunofluorescence assay | B | 6.41 | pIC50 | 390 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
ChEMBL | Inhibition of N-terminal flag-tagged Aurora A expressed in Escherichia coli BL21-DE3 by ELISA | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
ChEMBL | Inhibition of Aurora A kinase (unknown origin) | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2017) 140: 1-19 [PMID:28918096] |
ChEMBL | Inhibition of recombinant GST-tagged N-terminal truncated human Aurora A (123 to 401 residues) expressed in Sf9 insect cell using tetra-LRRASLG peptide as substrate incubated for 20 mins by Kinase-Glo plus luminescent kinase assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2021) 64: 7312-7330 [PMID:34009981] |
GtoPdb | - | - | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2009) 52: 3300-7 [PMID:19402633] |
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 in human HCT116 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
ChEMBL | Inhibition of Aurora B in human HT29 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay | B | 4.57 | pIC50 | >27000 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
ChEMBL | Inhibition of N-terminal flag-tagged Aurora B expressed in Escherichia coli BL21-DE3 by ELISA | B | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
GtoPdb | - | - | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2009) 52: 3300-7 [PMID:19402633] |
ChEMBL | Inhibition of N-terminal flag-tagged Aurora B E161T mutant expressed in Escherichia coli BL21-DE3 | B | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (2009) 52: 3300-3307 [PMID:19402633] |
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]