Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL2392553 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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]