SB-747651A [Ligand Id: 8130] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL188434 (SB-747651, SB-747651A)
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
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  • CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 [ChEMBL: CHEMBL4523582] [GtoPdb: 3125313932063261] [UniProtKB: P0DTD1]
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  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
  • Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Rat [ChEMBL: CHEMBL5509] [GtoPdb: 1503] [UniProtKB: Q63644]
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  • ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
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  • ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
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  • AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibitory concentration against selected kinase CDK2 B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3407-3411 [PMID:15955699]
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627]
ChEMBL Inhibitory concentration against selected kinase DYRK1-alpha B 5.31 pIC50 4900 nM IC50 Bioorg Med Chem Lett (2005) 15: 3407-3411 [PMID:15955699]
CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125313932063261] [UniProtKB: P0DTD1]
ChEMBL SARS-CoV-2 3CL-Pro protease inhibition IC50 determined by FRET kind of response from peptide substrate F 5.68 pIC50 2070 nM IC50 Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464]
ChEMBL Inhibitory concentration against selected kinase ROCK1 B 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2005) 15: 3407-3411 [PMID:15955699]
Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5509] [GtoPdb: 1503] [UniProtKB: Q63644]
ChEMBL Inhibition of rat ROCK1 B 7.42 pIC50 38 nM IC50 J Med Chem (2008) 51: 5663-5679 [PMID:18800763]
ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443]
ChEMBL Inhibitory concentration against selected kinase p70S6K B 6.57 pIC50 270 nM IC50 Bioorg Med Chem Lett (2005) 15: 3407-3411 [PMID:15955699]
ribosomal protein S6 kinase A5/Ribosomal protein S6 kinase alpha 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4237] [GtoPdb: 1523] [UniProtKB: O75582]
ChEMBL Inhibition of MSK1 B 8.1 pIC50 8 nM IC50 J Med Chem (2008) 51: 5663-5679 [PMID:18800763]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2005) 15: 3407-11 [PMID:15955699]
ChEMBL Inhibitory concentration against MSK-1 B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem Lett (2005) 15: 3407-3411 [PMID:15955699]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of human AKT1 B 6.7 pIC50 200 nM IC50 J Med Chem (2008) 51: 5663-5679 [PMID:18800763]
AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
ChEMBL Inhibition of human AKT2 B 6.13 pIC50 741 nM IC50 J Med Chem (2008) 51: 5663-5679 [PMID:18800763]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL Inhibition of human AKT3 B 6.19 pIC50 646 nM IC50 J Med Chem (2008) 51: 5663-5679 [PMID:18800763]

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]