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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 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]