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 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]