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ChEMBL ligand: CHEMBL126077 (Indirubin-3'-Monooxime, Indirubin-3Monoxime, Indirubin-3-Monoxime, Indirubin-3-Oxime, Indirubin-3'-Oxime) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 32:
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]