CGP74514A [Ligand Id: 5945] activity data from GtoPdb and ChEMBL
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: CHEMBL367625 |
|---|
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 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 | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | In vitro inhibition of human CDK2/cyclin A. | - | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | In vitro inhibition of human CDK2/cyclin E. | - | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| cyclin dependent kinase 4/CDK4/Cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038472] [GtoPdb: 1976] [UniProtKB: P11802, P30281] | ||||||||
| GtoPdb | In vitro inhibition of human CDK4/cyclin D. | - | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| ChEMBL | Inhibition of human CDK4/cyclinD3 using Histone H1 as substrate in presence of [gamma-33P]ATP after 40 mins by scintillation counter method | B | 6.24 | pIC50 | 573 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| cyclin dependent kinase 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281, Q00534] | ||||||||
| ChEMBL | Inhibition of human CDK6/cyclinD3 using Histone H1 as substrate in presence of [gamma-33P]ATP after 40 mins by scintillation counter method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| 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 human CDK7/cyclin H. | - | 6.55 | pIC50 | 279 | 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 | 6.55 | pIC50 | 279 | 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 human CDK9/cyclin T. | - | 5.85 | pIC50 | 1400 | 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 | 5.85 | pIC50 | 1400 | 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 human CDK1/cyclin B. | - | 6.83 | pIC50 | 147 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| ChEMBL | Inhibitory activity against cyclin-dependent kinase 1 (CDK1) was determined | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-96 [PMID:9990463] |
| ChEMBL | Inhibitory activity against cyclin-dependent kinase 1 (CDK1) was determined | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-96 [PMID:9990463] |
| GtoPdb | - | - | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-6 [PMID:9990463] |
| ChEMBL | Inhibitory activity against cyclin-dependent kinase 1 (CDK1) was determined | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-96 [PMID:9990463] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| ChEMBL | Inhibition of human CDK1/cyclinB using Histone H1 as substrate in presence of [gamma-33P]ATP after 40 mins by scintillation counter method | B | 6.42 | pIC50 | 382 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| GtoPdb | In vitro inhibition of human CDK1/cyclin B. | - | 6.83 | pIC50 | 147 | 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 | 6.83 | pIC50 | 147 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| ChEMBL | Inhibition of CDK1/cyclin B1 (unknown origin) | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | - | - | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-6 [PMID:9990463] |
| 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 human CDK2/cyclin A. | - | 7.34 | pIC50 | 46 | 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 human CDK2/cyclin E. | - | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| ChEMBL | Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2017) 25: 6523-6535 [PMID:29089259] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| GtoPdb | In vitro inhibition of human CDK4/cyclin D. | - | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| 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 | 5.52 | pIC50 | 3000 | 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 | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| GtoPdb | In vitro inhibition of human CDK5/p25. | - | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2018) 61: 9105-9120 [PMID:30234987] |
| CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
| ChEMBL | Inhibition of human CLK2 using YRRAAVPPSPSLSRHSSPHQS(p)EDEEE as substrate in presence of [gamma-33P]ATP after 40 mins by scintillation counter method | B | 6.95 | pIC50 | 111 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761] | ||||||||
| ChEMBL | Inhibition of human CLK3 using ERMRPRKRQGSVRRRV as substrate in presence of [gamma-33P]ATP after 40 mins by scintillation counter method | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] | ||||||||
| ChEMBL | Inhibition of human CLK4 using YRRAAVPPSPSLSRHSSPHQS(p)EDEEE as substrate in presence of [gamma-33P]ATP after 40 mins by scintillation counter method | B | 6.98 | pIC50 | 104 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
| ChEMBL | Inhibition of human CLK1 using substrate ERMRPRKRQGSVRRRV in presence of [gamma-33P]ATP after 40 mins by scintillation counter method | B | 6.83 | pIC50 | 148 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| ChEMBL | Inhibition of CLK mediated SF3B1 activation in human SK-MEL-2 cells assessed as MDM2-pre mRNA exon skipping after 4 hrs by luciferase reporter gene assay relative to control | B | 5.38 | pEC50 | 4200 | nM | EC50 | Bioorg Med Chem Lett (2017) 27: 406-412 [PMID:28049589] |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibit of epidermal growth factor receptor (EGFR) | B | 5.29 | pIC50 | 5100 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-96 [PMID:9990463] |
| ChEMBL | Inhibit of epidermal growth factor receptor (EGFR) | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-96 [PMID:9990463] |
| 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 | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4108-4114 [PMID:21632247] |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Inhibition of recombinant human N-terminal GST-His6 tagged PDGFRalpha (Q551 to L1089 residues) expressed in Sf9 insect cells using poly(Ala,Glu,Lys,Tyr)6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2017) 25: 6523-6535 [PMID:29089259] |
| protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Inhibition of Protein kinase C alpha | B | 4.52 | pIC50 | 30000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-96 [PMID:9990463] |
| ChEMBL | Inhibition of Protein kinase C alpha | B | 4.87 | pIC50 | 13500 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 91-96 [PMID:9990463] |
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]
