RG-1530 [Ligand Id: 10361] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1980391 (R-1530, Rg-1530, RG-1530) |
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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] |
| ChEMBL | Inhibition of Aurora A (unknown origin) | B | 7.24 | pIC50 | 58 | nM | IC50 | Eur J Med Chem (2022) 238: 114424-114424 [PMID:35576702] |
| 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] |
| ChEMBL | Inhibition of CHK2 (unknown origin) | B | 7.62 | pIC50 | 24 | nM | IC50 | Eur J Med Chem (2022) 238: 114424-114424 [PMID:35576702] |
| 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] |
| ChEMBL | Inhibition of PLK4 (unknown origin) | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2022) 238: 114424-114424 [PMID:35576702] |
| 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] |
| ChEMBL | Inhibition of VEGFR2 (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2022) 238: 114424-114424 [PMID:35576702] |
| 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 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]
