BX-795 [Ligand Id: 8006] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL577784 (BX-795)
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  • inhibitor of nuclear factor kappa B kinase subunit epsilon/Inhibitor of nuclear factor kappa B kinase epsilon subunit in Human [ChEMBL: CHEMBL3529] [GtoPdb: 2040] [UniProtKB: Q14164]
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  • pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118]
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  • TANK binding kinase 1/Serine/threonine-protein kinase TBK1 in Human [ChEMBL: CHEMBL5408] [GtoPdb: 2237] [UniProtKB: Q9UHD2]
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  • unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385]
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  • unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8]
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  • 3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530]
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  • protein kinase A in Human [GtoPdb: 1694]
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  • kinase insert domain receptor in Human [GtoPdb: 1813] [UniProtKB: P35968]
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  • cyclin dependent kinase 2 in Human [GtoPdb: 1973] [UniProtKB: P24941]
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  • checkpoint kinase 1 in Human [GtoPdb: 1987] [UniProtKB: O14757]
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  • glycogen synthase kinase 3 beta in Human [GtoPdb: 2030] [UniProtKB: P49841]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]
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]
ChEMBL Competitive inhibition of TBK1 (unknown origin) by immunoprecipitation method B 8.22 pIC50 6 nM IC50 MedChemComm (2019) 10: 1999-2023
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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]