RG-1530 [Ligand Id: 10361] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1980391 (Rg-1530, R-1530, RG-1530)
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
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  • polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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  • KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721]
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  • fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888]
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  • fms related receptor tyrosine kinase 1 in Human [GtoPdb: 1812] [UniProtKB: P17948]
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  • Janus kinase 2 in Human [GtoPdb: 2048] [UniProtKB: O60674]
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  • ret proto-oncogene in Human [GtoPdb: 2185] [UniProtKB: P07949]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of CDK2 (unknown origin) B 5.88 pIC50 1330 nM IC50 ACS Med. Chem. Lett. (2013) 4: 259-263 [PMID:24900658]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
ChEMBL Inhibition of CDK4 (unknown origin) B 5 pIC50 >10000 nM IC50 ACS Med. Chem. Lett. (2013) 4: 259-263 [PMID:24900658]
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 FGFR1 (unknown origin) B 7.55 pIC50 28 nM IC50 ACS Med. Chem. Lett. (2013) 4: 259-263 [PMID:24900658]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
GtoPdb - - 7.02 pKd 96 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]
ChEMBL Inhibition of aurora-A (unknown origin) B 7.24 pIC50 58 nM IC50 ACS Med. Chem. Lett. (2013) 4: 259-263 [PMID:24900658]
checkpoint kinase 2/Serine/threonine-protein kinase Chk2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2527] [GtoPdb: 1988] [UniProtKB: O96017]
ChEMBL Inhibition of CHK2 (unknown origin) B 7.62 pIC50 24 nM IC50 ACS Med. Chem. Lett. (2013) 4: 259-263 [PMID:24900658]
polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444]
GtoPdb - - 7.96 pKd 11 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]
ChEMBL Inhibition of human PLK4 B 7.96 pKi 11 nM Ki J. Med. Chem. (2013) 56: 6069-6087 [PMID:23829549]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
GtoPdb - - 7.82 pKd 15 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]
ChEMBL Inhibition of KDR (unknown origin) B 8 pIC50 10 nM IC50 ACS Med. Chem. Lett. (2013) 4: 259-263 [PMID:24900658]
KIT proto-oncogene, receptor tyrosine kinase in Human [GtoPdb: 1805] [UniProtKB: P10721]
GtoPdb - - 7.59 pKd 26 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]
fms related receptor tyrosine kinase 3 in Human [GtoPdb: 1807] [UniProtKB: P36888]
GtoPdb - - 7.96 pKd 11 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]
fms related receptor tyrosine kinase 1 in Human [GtoPdb: 1812] [UniProtKB: P17948]
GtoPdb - - 8.05 pKd 9 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]
Janus kinase 2 in Human [GtoPdb: 2048] [UniProtKB: O60674]
GtoPdb - - 7.54 pKd 29 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]
ret proto-oncogene in Human [GtoPdb: 2185] [UniProtKB: P07949]
GtoPdb - - 7.66 pKd 22 nM Kd Cell Cycle (2010) 9: 3364-75 [PMID:20814247]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]