ChEMBL ligand: CHEMBL259850 (AR-A014418)
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] There should be some charts here, you may need to enable JavaScript!
Cyclin-dependent kinase 5 regulatory subunit 1 in Human [ChEMBL: CHEMBL2783] [UniProtKB: Q15078] There should be some charts here, you may need to enable JavaScript!
autophagy related 4B cysteine peptidase/Cysteine protease ATG4B in Human [ChEMBL: CHEMBL1741221] [GtoPdb: 2329] [UniProtKB: Q9Y4P1] There should be some charts here, you may need to enable JavaScript!
glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] There should be some charts here, you may need to enable JavaScript!
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Mouse [ChEMBL: CHEMBL1075321] [GtoPdb: 2030] [UniProtKB: Q9WV60] 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
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 (2017)
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	Binding affinity to human full length GSK-3 beta transfected in Sf21 cells assessed as inhibition constant measured after 6 hrs by scintillation method	B	7.42	pKi	38	nM	Ki	Bioorg Med Chem (2023) 92: 117406-117406 [PMID:37536264]
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 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]