Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL258805 (Su9516, Su-9516, SU-9516) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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: 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 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]