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ChEMBL ligand: CHEMBL259850 (AR-A014418) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836] | ||||||||
ChEMBL | Inhibition of mouse AChE using acetylthiocholine iodide as substrate incubated for 20 mins by Ellman's method | B | 4.4 | pIC50 | >40000 | nM | IC50 | J Med Chem (2021) 64: 7483-7506 [PMID:34024109] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of Cdk2 | B | 4 | pIC50 | >100000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of CDK2 at 10 mM | B | 4 | pIC50 | 100000 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
ChEMBL | Inhibition of CDK5 at 10 mM | B | 4 | pIC50 | 100000 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
Cyclin-dependent kinase 5 regulatory subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2783] [UniProtKB: Q15078] | ||||||||
ChEMBL | Inhibition of Cdk5 | B | 4 | pIC50 | >100000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
autophagy related 4B cysteine peptidase/Cysteine protease ATG4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741221] [GtoPdb: 2329] [UniProtKB: Q9Y4P1] | ||||||||
ChEMBL | Inhibition of ATG4B (unknown origin) incubated up to 1 hr in presence of fluorescent protein substrate by FRET-based-LC3 cleavage assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | WO-2017027984-A1. Compounds and methods for treatment of cancer by inhibiting atg4b and blocking autophagy (null) |
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
ChEMBL | Inhibition of human GSK3alpha activity using Ser/Thr 11 peptide as substrate by FRET assay | B | 4.15 | pIC50 | 70000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5610-5615 [PMID:21807510] |
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
ChEMBL | Inhibition of GSK-3beta using phospho-glycogen synthase peptide-2 as substrate after 10 mins by liquid scintillation counting | B | 6.11 | pKi | 770 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 2099-2101 [PMID:22321216] |
GtoPdb | - | - | 7.42 | pKi | 38 | nM | Ki | J Biol Chem (2003) 278: 45937-45 [PMID:12928438] |
ChEMBL | Inhibition of GSK3-beta | B | 7.42 | pKi | 38 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of human GSK-3beta using biotin-AAEELDSRAGS(PO3H2)PQL as substrate after 20 mins by liquid scintillation counting | B | 7.42 | pKi | 38 | nM | Ki | Bioorg Med Chem Lett (2012) 22: 2099-2101 [PMID:22321216] |
ChEMBL | Inhibition of human recombinant GSK-3beta using prephosphorylated polypeptide as substrate incubated for 30 mins in presence of ATP by Kinase-Glo luminescence assay | B | 6.31 | pIC50 | 490 | nM | IC50 | J Med Chem (2021) 64: 7483-7506 [PMID:34024109] |
ChEMBL | Inhibition of human GSK-3beta using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE substrate peptide and [gamma-33P-ATP] incubated for 40 mins by scintillation counting method | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 160-166 [PMID:29208522] |
ChEMBL | Inhibition of human recombinant GSK3beta | B | 6.98 | pIC50 | 104 | nM | IC50 | J Med Chem (2011) 54: 8461-8470 [PMID:22050263] |
ChEMBL | Inhibition of GSK3beta | B | 6.98 | pIC50 | 104 | nM | IC50 | J Med Chem (2012) 55: 9107-9119 [PMID:22489897] |
ChEMBL | Inhibition of GSK3-beta | B | 6.98 | pIC50 | 104 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of GSK3-beta | B | 6.98 | pIC50 | 104 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
ChEMBL | Inhibition of recombinant full length human GSK3beta expressed in Sf21 insect cells using biotinylated-AAEELDSRAGS(PO3H2)PQL peptide as substrate preincubated enzyme-substrate mixture for 15 to 20 mins followed by [gamma-33P]ATP addition and measured after 20 mins by scintillation proximity assay | B | 6.98 | pIC50 | 104 | nM | IC50 | ACS Med Chem Lett (2020) 11: 825-831 [PMID:32435391] |
ChEMBL | Inhibition of human GSK3-beta | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2009) 44: 2361-2371 [PMID:18929433] |
ChEMBL | Inhibition of recombinant human GSK3beta using biotin-AAEELDSRAGS(PO3H2)PQL as substrate preincubated for 10 to 15 mins followed by [gamma33P]ATP addition after 20 mins by scintillation proximity assay | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2017) 125: 464-477 [PMID:27689729] |
ChEMBL | Inhibition of recombinant human GSK3beta using prephosphorylated peptide as substrate measured after 30 mins by Kinase-glo luminescence assay | B | 7.14 | pIC50 | 72 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1597-1600 [PMID:31054862] |
ChEMBL | Inhibition of human GSK3-beta by scintillation counting | B | 7.38 | pIC50 | 41.8 | nM | IC50 | J Med Chem (2009) 52: 1853-1863 [PMID:19338355] |
ChEMBL | Inhibition of recombinant full length human His-tagged GSK3beta expressed in baculovirus expression system using ser/thr-9 peptide as substrate measured after 1 hr by Z'-Lyte assay | B | 8.68 | pIC50 | 2.07 | nM | IC50 | Medchemcomm (2018) 9: 1472-1490 [PMID:30288222] |
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075321] [GtoPdb: 2030] [UniProtKB: Q9WV60] | ||||||||
ChEMBL | Inhibition of human GSK-3beta in mouse 3T3 fibroblasts stably expressing four-repeat tau protein assessed as reduction in tau S396 phosphorylation after 4 hrs post dose by Western blot | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 160-166 [PMID:29208522] |
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]