Ro3280 [Ligand Id: 9403] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2392553
  • bromodomain containing 4/Bromodomain-containing protein 4 in Human [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
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  • bromodomain testis associated/Bromodomain testis-specific protein in Human [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
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  • polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
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  • FER tyrosine kinase in Human [GtoPdb: 2022] [UniProtKB: P16591]
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  • TTK protein kinase in Human [GtoPdb: 2264] [UniProtKB: P33981]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis B 6.57 pKd 267 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay B 6.59 pKd 260 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay B 6.92 pKd 120 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
bromodomain testis associated/Bromodomain testis-specific protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795185] [GtoPdb: 2729] [UniProtKB: Q58F21]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by MST assay B 5.72 pKd 1900 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by ITC analysis B 5.74 pKd 1800 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
ChEMBL Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay B 6.41 pKd 390 nM Kd J Med Chem (2021) 64: 15772-15786 [PMID:34710325]
polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350]
GtoPdb Ambit selectivity screen at 1μM Ro3280. - 10.05 pKd 0.09 nM Kd Bioorg Med Chem Lett (2012) 22: 1247-50 [PMID:22172702]
ChEMBL Inhibition of PLK1 (unknown origin) using biotin-AGAGTVPESIHSFIGDGLV as substrate by TR-FRET assay B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2013) 23: 3662-3666 [PMID:23664874]
GtoPdb In a biochemical enzymatic assay. - 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2012) 22: 1247-50 [PMID:22172702]
FER tyrosine kinase in Human [GtoPdb: 2022] [UniProtKB: P16591]
GtoPdb Ambit selectivity screen at 1μM Ro3280. - 7.28 pKd 53 nM Kd Bioorg Med Chem Lett (2012) 22: 1247-50 [PMID:22172702]
TTK protein kinase in Human [GtoPdb: 2264] [UniProtKB: P33981]
GtoPdb Ambit selectivity screen at 1μM Ro3280. - 7.29 pKd 51 nM Kd Bioorg Med Chem Lett (2012) 22: 1247-50 [PMID:22172702]

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]