SU9516 [Ligand Id: 6045] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL258805 (Su-9516, SU-9516)
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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 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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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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  • platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
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  • ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
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  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
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  • kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/CDK2/Cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248P24941]
ChEMBL Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb In vitro inhibition of CDK2/cyclin A. - 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb In vitro inhibition of CDK2/cyclin E. - 7.59 pIC50 26 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK2/cyclin A complex used in assay - 7.66 pIC50 22 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613P51946P51948]
GtoPdb In vitro inhibition of CDK7/cyclin H. - 6.04 pIC50 905 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.04 pIC50 905 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563P50750]
GtoPdb In vitro inhibition of CDK9/cyclin T. - 5.82 pIC50 1500 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 5.82 pIC50 1500 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
GtoPdb In vitro inhibition of CDK1/cyclin B. - 6.77 pIC50 168 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of CDK1 B 7.26 pIC50 55 nM IC50 AAPS J (2006) 8: E204-E221 [PMID:16584130]
ChEMBL Inhibition of His-6-tagged CDK1 (unknown origin) expressed in baculovirus-infected insect cells using histone H1 as substrate after 1 hr by by liquid scintillation counting in presence of [gamma-33P]ATP B 7.4 pIC50 40 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
GtoPdb CDK1/cyclin B complex used in assay - 7.4 pIC50 40 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067P06493P14635Q8WWL7]
GtoPdb In vitro inhibition of CDK1/cyclin B. - 6.77 pIC50 168 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK1/cyclin B complex used in assay - 7.4 pIC50 40 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
ChEMBL Inhibition of CDK1/cyclinB B 7.66 pIC50 22 nM IC50 Trends Pharmacol. Sci. (2004) 25: 471-480 [PMID:15559249]
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493P14635]
GtoPdb In vitro inhibition of CDK1/cyclin B. - 6.77 pIC50 168 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 6.77 pIC50 168 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK1/cyclin B complex used in assay - 7.4 pIC50 40 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibitory activity against Cyclin-dependent kinase 2 B 6.96 pIC50 110 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1939-1942 [PMID:12749903]
ChEMBL Inhibition of CDK2 B 7.46 pIC50 35 nM IC50 AAPS J (2006) 8: E204-E221 [PMID:16584130]
GtoPdb In vitro inhibition of CDK2/cyclin A. - 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb In vitro inhibition of CDK2/cyclin E. - 7.59 pIC50 26 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of His-6-tagged CDK2 (unknown origin) expressed in baculovirus-infected insect cells using histone H1 as substrate after 1 hr by by liquid scintillation counting in presence of [gamma-33P]ATP B 7.66 pIC50 22 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
GtoPdb CDK2/cyclin A complex used in assay - 7.66 pIC50 22 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864P24941]
GtoPdb In vitro inhibition of CDK2/cyclin A. - 7.57 pIC50 27 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.59 pIC50 26 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb In vitro inhibition of CDK2/cyclin E. - 7.59 pIC50 26 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK2/cyclin A complex used in assay - 7.66 pIC50 22 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
GtoPdb In vitro inhibition of CDK4/cyclin D. - 5.77 pIC50 1700 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
ChEMBL Inhibition of CDK4 B 6.52 pIC50 300 nM IC50 AAPS J (2006) 8: E204-E221 [PMID:16584130]
ChEMBL Inhibition of His-6-tagged CDK4 (unknown origin) expressed in baculovirus-infected insect cells using GST-retinoblastoma as substrate after 1 hr by by liquid scintillation counting in presence of [gamma-33P]ATP B 6.7 pIC50 200 nM IC50 J. Med. Chem. (2014) 57: 578-599 [PMID:24417566]
GtoPdb CDK4/cyclin D1 complex used in assay - 6.7 pIC50 200 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802P24385]
ChEMBL Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 5.77 pIC50 1700 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb In vitro inhibition of CDK4/cyclin D. - 5.77 pIC50 1700 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb CDK4/cyclin D1 complex used in assay - 6.7 pIC50 200 nM IC50 Cancer Res (2001) 61: 6170-7 [PMID:11507069]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Inhibition of CDK5 B 7.19 pIC50 65 nM IC50 AAPS J (2006) 8: E204-E221 [PMID:16584130]
GtoPdb In vitro inhibition of CDK5/p25. - 7.66 pIC50 22 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535Q15078]
ChEMBL Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay B 7.66 pIC50 22 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
GtoPdb In vitro inhibition of CDK5/p25. - 7.66 pIC50 22 nM IC50 J Med Chem (2018) 61: 9105-9120 [PMID:30234987]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Inhibition of EGFR B 5 pIC50 >10000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
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 5.3 pIC50 5000 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 4.9 pIC50 12589.25 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 4.9 pIC50 12589.25 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 4.9 pIC50 12589.25 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 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 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 5.2 pIC50 6309.57 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
platelet derived growth factor receptor beta/Platelet-derived growth factor receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1913] [GtoPdb: 1804] [UniProtKB: P09619]
ChEMBL Inhibitory activity was tested against Platelet-derived growth factor receptor beta B 4.74 pIC50 18000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1939-1942 [PMID:12749903]
ChEMBL Inhibition of PDGFRbeta B 5 pIC50 >10000 nM IC50 Proc. Natl. Acad. Sci. U.S.A. (2007) 104: 20523-20528 [PMID:18077363]
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949]
ChEMBL Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells B 5.8 pIC50 1600 nM IC50 Bioorg. Med. Chem. (2010) 18: 1482-1496 [PMID:20117004]
SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL267] [GtoPdb: 2206] [UniProtKB: P12931]
ChEMBL Inhibitory activity was tested against Src protein tyrosine kinase B 4.96 pIC50 11000 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1939-1942 [PMID:12749903]
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968]
ChEMBL Inhibitory activity was tested against FLK kinase B 6.89 pIC50 130 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1939-1942 [PMID:12749903]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]