CGP74514A [Ligand Id: 5945] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL367625 |
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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: 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 33:
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]
