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ChEMBL ligand: CHEMBL2392553 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]