BX-795 [Ligand Id: 8006] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL577784 (BX-795) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Cyclic GMP-AMP synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105728] [GtoPdb: 3165] [UniProtKB: Q8N884] | ||||||||
| ChEMBL | Inhibition of cGAS in human THP1 cells assessed as reduction in salmon sperm dsDNA-induced IFN-beta expression preincubated for 1 hr followed by dsDNA stimulation for 12 hrs by luciferase reporter gene assay | B | 7.22 | pIC50 | 60 | nM | IC50 | PLoS One (2017) 12: e0184843-null [PMID:28934246] |
| inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164] | ||||||||
| GtoPdb | - | - | 7.39 | pIC50 | 41 | nM | IC50 | J Biol Chem (2009) 284: 14136-46 [PMID:19307177] |
| ChEMBL | Inhibition of recombinant full length human C-terminal GST-tagged IKKepsilon expressed in baculovirus expression system using biotin-labelled Ahx-GDEDFSSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubated for 30 mins in presence of 10 uM of ATP by TR-FRET assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2020) 63: 601-612 [PMID:31859507] |
| pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
| ChEMBL | Inhibition of recombinant PDK1 (unknown origin) using PDK1tide substrate incubated for 7 mins | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem (2015) 23: 5483-5488 [PMID:26275681] |
| TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2] | ||||||||
| ChEMBL | Binding affinity to TBK1 in human Ramos cell lysate incubated for 45 mins by kinobeads based assay | B | 6.8 | pKd | 158.49 | nM | Kd | ACS Med Chem Lett (2019) 10: 780-785 [PMID:31097999] |
| ChEMBL | Binding affinity to phosphorylated TBK1 in calyculin A stimulated human Ramos cell lysate incubated for 45 mins by kinobeads based assay | B | 7.4 | pKd | 39.81 | nM | Kd | ACS Med Chem Lett (2019) 10: 780-785 [PMID:31097999] |
| ChEMBL | Binding affinity to TBK1 in human HEK293/K562/placenta/HepG2 cell lysate mixture incubated for 45 mins by kinobeads based assay | B | 7.7 | pKd | 19.95 | nM | Kd | ACS Med Chem Lett (2019) 10: 780-785 [PMID:31097999] |
| ChEMBL | Inhibition of recombinant full length human N-terminal His-tagged TBK1 using biotin-labelled Ahx-GDEDFSSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubated for 30 mins in presence of 1 mM of ATP by TR-FRET assay | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2020) 63: 601-612 [PMID:31859507] |
| ChEMBL | Inhibition of recombinant full length human N-terminal His-tagged TBK1 using biotin-labelled Ahx-GDEDFSSFAEPG peptide as substrate preincubated with enzyme for 15 mins followed by substrate addition and further incubated for 30 mins in presence of 10 uM of ATP by TR-FRET assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2020) 63: 601-612 [PMID:31859507] |
| GtoPdb | - | - | 8.22 | pIC50 | 6 | nM | IC50 | J Biol Chem (2009) 284: 14136-46 [PMID:19307177] |
| ChEMBL | Competitive inhibition of TBK1 (unknown origin) by immunoprecipitation method | B | 8.22 | pIC50 | 6 | nM | IC50 | Medchemcomm (2019) 10: 1999-2023 [PMID:32206239] |
| unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385] | ||||||||
| ChEMBL | Inhibition of SUMO-tagged ULK1 (unknown origin) kinase domain expressed in KRX cells using [32P]-gamma-ATP and myelin basic protein substrate incubated for 7 mins | B | 7.06 | pIC50 | 87 | nM | IC50 | Bioorg Med Chem (2015) 23: 5483-5488 [PMID:26275681] |
| unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8] | ||||||||
| ChEMBL | Inhibition of SUMO-tagged ULK2 (unknown origin) kinase domain expressed in KRX cells using [32P]-gamma-ATP and myelin basic protein substrate incubated for 7 mins | B | 6.51 | pIC50 | 310 | nM | IC50 | Bioorg Med Chem (2015) 23: 5483-5488 [PMID:26275681] |
| 3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| GtoPdb | In a direct kinase activity measuring phosphorylation od a small peptide substrate mimetic | - | 7.96 | pIC50 | 11 | nM | IC50 | J Biol Chem (2005) 280: 19867-74 [PMID:15772071] |
| protein kinase A in Human [GtoPdb: 1694] | ||||||||
| GtoPdb | - | - | 6.08 | pIC50 | 840 | nM | IC50 | J Biol Chem (2005) 280: 19867-74 [PMID:15772071] |
| kinase insert domain receptor in Human [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| GtoPdb | - | - | 5.96 | pIC50 | 1100 | nM | IC50 | J Biol Chem (2005) 280: 19867-74 [PMID:15772071] |
| aurora kinase B in Human [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| GtoPdb | - | - | 7.51 | pIC50 | 31 | nM | IC50 | J Biol Chem (2009) 284: 14136-46 [PMID:19307177] |
| cyclin dependent kinase 2 in Human [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| GtoPdb | - | - | 6.37 | pIC50 | 430 | nM | IC50 | J Biol Chem (2005) 280: 19867-74 [PMID:15772071] |
| checkpoint kinase 1 in Human [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| GtoPdb | - | - | 6.29 | pIC50 | 510 | nM | IC50 | J Biol Chem (2005) 280: 19867-74 [PMID:15772071] |
| glycogen synthase kinase 3 beta in Human [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| GtoPdb | - | - | 6.21 | pIC50 | 620 | nM | IC50 | J Biol Chem (2005) 280: 19867-74 [PMID:15772071] |
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]
