romaciclib [Ligand Id: 13753] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4225966 (Sel-120 free base)
  • casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
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  • casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784]
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  • cyclin dependent kinase 19/Cyclin-dependent kinase 19 in Human [ChEMBL: CHEMBL6002] [GtoPdb: 1972] [UniProtKB: Q9BWU1]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • cyclin dependent kinase 8/Cyclin-dependent kinase 8 in Human [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336]
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  • cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
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  • CDC like kinase 1/Dual specificity protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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  • CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
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  • CDC like kinase 4/Dual specificity protein kinase CLK4 in Human [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
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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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  • homeodomain interacting protein kinase 3/Homeodomain-interacting protein kinase 3 in Human [ChEMBL: CHEMBL4577] [GtoPdb: 2035] [UniProtKB: Q9H422]
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  • mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08]
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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]
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  • histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76]
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  • Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
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  • TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729]
ChEMBL Inhibition of CSNK1A1 (unknown origin) by ADP-Glo assay B 5.86 pIC50 1390 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
casein kinase 2, alpha prime polypeptide subunit/Casein kinase II subunit alpha` in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784]
ChEMBL Inhibition of CSNK2A2 (unknown origin) by ADP-Glo assay B 6.55 pIC50 278.9 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941]
ChEMBL Inhibition of CDK2/cyclinA2 (unknown origin) by ADP-Glo chemiluminescence assay B 8.33 pIC50 4.7 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948]
ChEMBL Inhibition of CDK7/cyclinH/MAT1 (unknown origin) by ADP-Glo chemiluminescence assay B 7.29 pIC50 50.97 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
cyclin dependent kinase 8/CDK8/Cyclin C in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038474] [GtoPdb: 1980] [UniProtKB: P24863, P49336]
GtoPdb Binding dissociation constant for hCDK8 protein - 8.52 pKd 3 nM Kd Oncotarget (2017) 8: 33779-33795 [PMID:28422713]
ChEMBL Inhibition of CDK8/CyclinC (unknown origin) by ADP-Glo chemiluminescence assay B 7.76 pIC50 17.5 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
ChEMBL Inhibition of His tagged human recombinant CDK8/Cyclin C expressed in baculovirus expression system incubated for 15 mins by FRET-based LanthaScreen binding competition assay B 7.85 pIC50 14.11 nM IC50 J Med Chem (2023) 66: 5439-5452 [PMID:37029334]
ChEMBL Displacement of tracer 236 from CDK8/cyclin C (unknown origin) preincubated for 15 mins followed by tracer addition and measured after 60 mins by FRET based lanthascreen assay B 7.85 pIC50 14.1 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
ChEMBL Inhibition of CDK8/Cyclin C (unknown origin) B 8.36 pIC50 4.4 nM IC50 J Med Chem (2022) 65: 6390-6418 [PMID:35485642]
ChEMBL Inhibition of CDK8/CyclinC (unknown origin) incubated for 60 mins in presence of ATP by scintillation counting method B 8.36 pIC50 4.4 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
GtoPdb Inhibition of CDK8/CycC kinase activity - 8.36 pIC50 4.4 nM IC50 Oncotarget (2017) 8: 33779-33795 [PMID:28422713]
ChEMBL Inhibition of CDK8/Cyclin-C (unknown origin) in presence of [gamma33P]ATP by radiometric method B 8.4 pIC50 4 nM IC50 J Med Chem (2018) 61: 5073-5092 [PMID:29266937]
cyclin dependent kinase 19/Cyclin-C/Cyclin-dependent kinase 19 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3883323] [GtoPdb: 1972] [UniProtKB: P24863, Q9BWU1]
GtoPdb Inhibition of CDK19/CycC kinase activity - 7.98 pIC50 10.4 nM IC50 Oncotarget (2017) 8: 33779-33795 [PMID:28422713]
ChEMBL Inhibition of CDK19/Cyclin C (unknown origin) B 7.98 pIC50 10.4 nM IC50 J Med Chem (2022) 65: 6390-6418 [PMID:35485642]
ChEMBL Inhibition of CDK19/Cyclin C (unknown origin) B 7.98 pIC50 10.4 nM IC50 Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525]
ChEMBL Inhibition of CDK19/CyclinC (unknown origin) incubated for 60 mins in presence of ATP by scintillation counting method B 7.98 pIC50 10.4 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
ChEMBL Inhibition of CDK19/Cyclin-C (unknown origin) in presence of [gamma33P]ATP by radiometric method B 8 pIC50 10 nM IC50 J Med Chem (2018) 61: 5073-5092 [PMID:29266937]
cyclin dependent kinase 19/Cyclin-dependent kinase 19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6002] [GtoPdb: 1972] [UniProtKB: Q9BWU1]
ChEMBL Inhibition of CDK19 (unknown origin) by ADP-Glo assay B 7.6 pIC50 25.1 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
ChEMBL Inhibition of CDK19 (unknown origin) by HTRF assay B 7.72 pIC50 19.13 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
GtoPdb Inhibition of CDK19/CycC kinase activity - 7.98 pIC50 10.4 nM IC50 Oncotarget (2017) 8: 33779-33795 [PMID:28422713]
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
ChEMBL Inhibition of CDK2/cyclinE1 (unknown origin) by ADP-Glo chemiluminescence assay B 9.01 pIC50 0.97 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
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 CDK5/p25NCK (unknown origin) by ADP-Glo chemiluminescence assay B 8.78 pIC50 1.66 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
ChEMBL Inhibition of CDK5/p35NCK (unknown origin) by ADP-Glo chemiluminescence assay B 8.87 pIC50 1.34 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
cyclin dependent kinase 8/Cyclin-dependent kinase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5719] [GtoPdb: 1980] [UniProtKB: P49336]
GtoPdb Binding dissociation constant for hCDK8 protein - 8.52 pKd 3 nM Kd Oncotarget (2017) 8: 33779-33795 [PMID:28422713]
ChEMBL Inhibition of CDK8 (unknown origin) in presence of ATP by ADP-Glo assay B 7.43 pIC50 37.2 nM IC50 Eur J Med Chem (2023) 251: 115214-115214 [PMID:36889252]
ChEMBL Inhibition of CDK8 (unknown origin) by ADP-Glo assay B 7.76 pIC50 17.5 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
ChEMBL Inhibition of CDK8 (unknown origin) by HTRF assay B 7.84 pIC50 14.5 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
ChEMBL Inhibition of CDK8 (unknown origin) B 8.36 pIC50 4.4 nM IC50 Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525]
GtoPdb Inhibition of CDK8/CycC kinase activity - 8.36 pIC50 4.4 nM IC50 Oncotarget (2017) 8: 33779-33795 [PMID:28422713]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL Inhibition of CDK9 (unknown origin) in presence of [gamma33P]ATP by radiometric method B 5.97 pIC50 1070 nM IC50 J Med Chem (2018) 61: 5073-5092 [PMID:29266937]
CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Inhibition of CLK1 (unknown origin) by ADP-Glo assay B 8.28 pIC50 5.3 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Inhibition of CLK2 (unknown origin) by ADP-Glo assay B 7.68 pIC50 21 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL Inhibition of CLK4 (unknown origin) by ADP-Glo assay B 8.57 pIC50 2.7 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
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 Inhibition of DYRK1A (unknown origin) by ADP-Glo assay B 6.48 pIC50 332.2 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
homeodomain interacting protein kinase 3/Homeodomain-interacting protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4577] [GtoPdb: 2035] [UniProtKB: Q9H422]
ChEMBL Inhibition of HIPK3 (unknown origin) by ADP-Glo assay B 6.88 pIC50 131.8 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
mitogen-activated protein kinase 15/Mitogen-activated protein kinase 15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5198] [GtoPdb: 2090] [UniProtKB: Q8TD08]
ChEMBL Inhibition of ERK8 (unknown origin) by ADP-Glo assay B 5.87 pIC50 1344 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
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 Inhibition of ROCK1 (unknown origin) by ADP-Glo assay B 6.14 pIC50 717.5 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76]
ChEMBL Inhibition of HASPIN (unknown origin) by ADP-Glo assay B 7.34 pIC50 46 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9]
ChEMBL Inhibition of PIM2 (unknown origin) by ADP-Glo assay B 6.53 pIC50 298.2 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]
TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
ChEMBL Inhibition of TAOK1 (unknown origin) by ADP-Glo assay B 5 pIC50 >10000 nM IC50 J Med Chem (2024) 67: 8161-8171 [PMID:38690856]

ChEMBL data shown on this page come from version 36:

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]