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ChEMBL ligand: CHEMBL1673046 |
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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 | Inhibition of BRD4 (unknown origin) | B | 5.8 | pKd | 1600 | nM | Kd | Eur J Med Chem (2019) 178: 530-543 [PMID:31212132] |
ChEMBL | Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay | B | 6.1 | pKd | 800 | 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 ITC analysis | B | 6.13 | pKd | 735 | 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 | 6.69 | pKd | 205 | 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 ITC analysis | B | 5.38 | pKd | 4200 | 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 MST assay | B | 5.46 | pKd | 3500 | 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 | 6.17 | pKd | 675 | nM | Kd | J Med Chem (2021) 64: 15772-15786 [PMID:34710325] |
leucine rich repeat kinase 2/Leucine-rich repeat serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075104] [GtoPdb: 2059] [UniProtKB: Q5S007] | ||||||||
ChEMBL | Inhibition of recombinant human GST-tagged LRRK2 catalytic domain (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate measured after 1 hr by Alexa fluor-647 ADP tracer-based ADAPTA assay | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2020) 63: 7817-7826 [PMID:32530623] |
mitogen-activated protein kinase 7/Mitogen-activated protein kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5332] [GtoPdb: 2093] [UniProtKB: Q13164] | ||||||||
ChEMBL | In vitro Erk5 : In vitro Erk5 binding assay: Ambit Kd values in nanomolar. Kd values generated by Ambit binding assay over a concentration range of the compound. | B | 7.1 | pKd | 80 | nM | Kd | US-9266890-B2. Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders (2016) |
GtoPdb | - | - | 7.1 | pKd | 80 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
ChEMBL | Inhibition of ERK5 in human HeLa cells incubated for 15 mins prior to ATP addition by KiNativ profiling method | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2019) 178: 530-543 [PMID:31212132] |
ChEMBL | Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis | B | 6.62 | pIC50 | 240 | nM | IC50 | ACS Med Chem Lett (2011) 2: 195-200 [PMID:21412406] |
ChEMBL | Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin-Ahx-PPGDYSTTPGGTLFSTTPGGTRI peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by TR-FRET assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2019) 62: 928-940 [PMID:30563338] |
doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075] | ||||||||
ChEMBL | Inhibition of recombinant human N-terminal His6-tagged DCLK1 (G351 to H689 residues) expressed in Escherichia coli BL21 DE3 using 5-FAM-KKLRRTLSVA-COOH as substrate measured after 2 hrs by mobility shift assay | B | 6.15 | pIC50 | 716 | nM | IC50 | J Med Chem (2020) 63: 7817-7826 [PMID:32530623] |
doublecortin like kinase 2 in Human [GtoPdb: 2006] [UniProtKB: Q8N568] | ||||||||
GtoPdb | - | - | 6.72 | pKd | 190 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
polo like kinase 4 in Human [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
GtoPdb | - | - | 6.22 | pKd | 600 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
tyrosine kinase non receptor 1 in Human [GtoPdb: 2245] [UniProtKB: Q13470] | ||||||||
GtoPdb | - | - | 6.05 | pKd | 890 | nM | Kd | Cancer Cell (2010) 18: 258-67 [PMID:20832753] |
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]