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: 3125, 3139, 3206, 3261] [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 A1/Ribosomal protein S6 kinase alpha 1 in Human [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
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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]
ChEMBL Inhibition of CDK2 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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]
ChEMBL Inhibition of DYRK1A (unknown origin) B 5.31 pIC50 4900 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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: 3125, 3139, 3206, 3261] [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]
ChEMBL Inhibition of ROCK1 (unknown origin) B 7 pIC50 100 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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 A1/Ribosomal protein S6 kinase alpha 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418]
ChEMBL Inhibition of RSK1 (unknown origin) B 6.81 pIC50 155 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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]
ChEMBL Inhibition of MSK-1 (unknown origin) B 9.3 pIC50 0.5 nM IC50 J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
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 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]