indirubin-3'-monoxime [Ligand Id: 5989] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL126077 (Indirubin-3'-Monooxime, Indirubin-3-Monoxime, Indirubin-3Monoxime, Indirubin-3-Oxime, Indirubin-3'-Oxime)
  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • Cyclin-dependent kinase 5 regulatory subunit 1 in Human [ChEMBL: CHEMBL2783] [UniProtKB: Q15078]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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  • eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
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  • Protein kinase Pfmrk in Plasmodium falciparum [ChEMBL: CHEMBL4090] [UniProtKB: P90584]
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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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  • aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
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  • fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL Inhibition of human recombinant 5-LO assessed as product formation by cell-free assay relative to control B 4.82 pIC50 15000 nM IC50 J Med Chem (2014) 57: 3715-3723 [PMID:24697244]
ChEMBL Inhibition of 5-LO in human neutrophils assessed as product formation by cell-intact assay relative to control in presence of 2.5 uM A23187 ionophore B 4.95 pIC50 11100 nM IC50 J Med Chem (2014) 57: 3715-3723 [PMID:24697244]
ChEMBL Inhibition of 5-LO in human neutrophils assessed as product formation by cell-intact assay relative to control in presence of 20 uM A23187/AA ionophore B 5.09 pIC50 8200 nM IC50 J Med Chem (2014) 57: 3715-3723 [PMID:24697244]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750]
ChEMBL Inhibition of against CDK9/cyclinT1 (unknown origin) using Ulight-CFFKNIVTPRTPPPSQGK-amide substrate and ATP incubated for 90 mins by fluorescence based assay B 5.62 pIC50 2400 nM IC50 Bioorg Med Chem Lett (2015) 25: 2447-2451 [PMID:25908517]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Inhibition of Cdk1 B 6.74 pIC50 180 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7]
ChEMBL Inhibitory activity against cyclin dependent kinase 1-cyclinB from starfish (Marthasterias glacialis) oocytes B 6.74 pIC50 180 nM IC50 J Med Chem (2004) 47: 935-946 [PMID:14761195]
ChEMBL Inhibition of CDK1/cyclinB B 7.74 pIC50 18 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
ChEMBL Inhibition of against CDK2/cyclinE1 (unknown origin) using Ulight-CFFKNIVTPRTPPPSQGK-amide substrate and ATP incubated for 15 mins by fluorescence based assay B 6.15 pIC50 700 nM IC50 Bioorg Med Chem Lett (2015) 25: 2447-2451 [PMID:25908517]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL Inhibitory activity against Cyclin-dependent kinase 5-p35nck5a B 7 pIC50 100 nM IC50 J Med Chem (2004) 47: 935-946 [PMID:14761195]
ChEMBL Inhibition of cyclin-dependent kinase 5/p25 B 7 pIC50 100 nM IC50 J Med Chem (2005) 48: 671-679 [PMID:15689152]
ChEMBL Inhibition of mammalian CDK5/p25 B 7 pIC50 100 nM IC50 J Med Chem (2006) 49: 4638-4649 [PMID:16854069]
Cyclin-dependent kinase 5 regulatory subunit 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2783] [UniProtKB: Q15078]
ChEMBL Inhibition of Cdk5 B 7 pIC50 100 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
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 GSK3-beta B 7.66 pIC50 22 nM IC50 Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363]
ChEMBL Inhibition of human GSK3-beta B 7.66 pIC50 22 nM IC50 Eur J Med Chem (2009) 44: 2361-2371 [PMID:18929433]
ChEMBL Inhibition of GSK3-beta B 7.66 pIC50 22 nM IC50 Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249]
GtoPdb - - 7.66 pIC50 22 nM IC50 J Biol Chem (2001) 276: 251-60 [PMID:11013232]
eukaryotic translation initiation factor 2 alpha kinase 2/Interferon-induced, double-stranded RNA-activated protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5785] [GtoPdb: 2016] [UniProtKB: P19525]
ChEMBL Inhibition of human recombinant PKR autophosphorylation using poly[I:C] after 10 mins by luminescent assay B 7 pIC50 <100 nM IC50 Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.7 pIC50 1995.26 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.9 pIC50 1258.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Inhibitory activity against Plasmodium falciparum W2 F 5.96 pIC50 1100 nM IC50 J Med Chem (2003) 46: 3877-3882 [PMID:12930149]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 6 pIC50 1000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Inhibitory activity against Plasmodium falciparum D6 F 6.22 pIC50 600 nM IC50 J Med Chem (2003) 46: 3877-3882 [PMID:12930149]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 6.3 pIC50 501.19 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 6.3 pIC50 501.19 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 6.5 pIC50 316.23 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 6.5 pIC50 316.23 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
Protein kinase Pfmrk in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4090] [UniProtKB: P90584]
ChEMBL Inhibitory activity against Plasmodium falciparum cyclin dependent protein kinase, Pfmrk B 4.52 pIC50 30000 nM IC50 J Med Chem (2003) 46: 3877-3882 [PMID:12930149]
ChEMBL Inhibition of Plasmodium falciparum cyclin-dependent kinase B 4.52 pIC50 30000 nM IC50 J Med Chem (2004) 47: 5418-5426 [PMID:15481979]
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Inhibition of human recombinant aurora A kinase B 5.4 pIC50 4000 nM IC50 J Med Chem (2007) 50: 4027-4037 [PMID:17665890]
aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Inhibition of human recombinant aurora B kinase B 5.64 pIC50 2300 nM IC50 J Med Chem (2007) 50: 4027-4037 [PMID:17665890]
aurora kinase C/Serine/threonine-protein kinase Aurora-C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3935] [GtoPdb: 1938] [UniProtKB: Q9UQB9]
ChEMBL Inhibition of human recombinant aurora C kinase B 6.52 pIC50 300 nM IC50 J Med Chem (2007) 50: 4027-4037 [PMID:17665890]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL Inhibition of FLT3 by HTRF assay B 7.48 pIC50 33 nM IC50 Bioorg Med Chem Lett (2010) 20: 2033-2037 [PMID:20153646]

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]