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 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]