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

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ChEMBL ligand: CHEMBL258805 (Su-9516, Su9516, 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: Q00535, Q15078]
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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 A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
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: P50613, P51946, P51948]
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: O60563, P50750]
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: O95067, P06493, P14635, Q8WWL7]
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: P06493, P14635]
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: P24864, P24941]
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: P11802, P24385]
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: Q00535, Q15078]
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 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]