cirtuvivint [Ligand Id: 12620] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4784318
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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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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  • 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 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
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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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  • dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
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  • dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
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  • dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
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  • dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
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  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5.52 pIC50 3015 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 recombinant human CDK5/p25 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5.4 pIC50 3960 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 10.74 pKd 0.02 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human CLK1 expressed in Sf9 insect cells using myelin basic protein as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 8.04 pIC50 9.1 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of CLK1 (unknown origin) by Z'-LYTE assay B 8.1 pIC50 8 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
ChEMBL Inhibition of recombinant human CLK1 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.15 pIC50 7.1 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.44 pIC50 3.6 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of CLK2 (unknown origin) by Z'-LYTE kinase assay B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2022) 70: 116921-116921 [PMID:35863237]
ChEMBL Inhibition of CLK2 (unknown origin) by Z'-LYTE assay B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
ChEMBL Inhibition of human CLK2 B 8.7 pIC50 2 nM IC50 J Med Chem (2021) 64: 13191-13211 [PMID:34519506]
GtoPdb - - 9 pIC50 1 nM IC50 WO2020150552A2. Methods of treating cartilage disorders through inhibition of clk and dyrk (2020)
ChEMBL Inhibition of recombinant CLK2 (unknown origin) using Ser/Thr 6 peptide as substrate incubated for 1 hr in presence of ATP by FRET assay B 9 pEC50 1 nM EC50 WO-2020150552-A2. Methods of treating cartilage disorders through inhibition of clk and dyrk (2020)
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Inhibition of recombinant human CLK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.51 pIC50 30.9 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of CLK3 (unknown origin) by Z'-LYTE kinase assay B 7.66 pIC50 22 nM IC50 Bioorg Med Chem (2022) 70: 116921-116921 [PMID:35863237]
ChEMBL Inhibition of CLK3 (unknown origin) by Z'-LYTE assay B 7.7 pIC50 20 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
GtoPdb - - 7.92 pIC50 12 nM IC50 WO2020150552A2. Methods of treating cartilage disorders through inhibition of clk and dyrk (2020)
ChEMBL Inhibition of human CLK3 B 8.66 pIC50 2.2 nM IC50 J Med Chem (2021) 64: 13191-13211 [PMID:34519506]
ChEMBL Inhibition of recombinant CLK3 (unknown origin) using Ser/Thr 18 peptide as substrate incubated for 1 hr in presence of ATP by FRET assay B 7.92 pEC50 12 nM EC50 WO-2020150552-A2. Methods of treating cartilage disorders through inhibition of clk and dyrk (2020)
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.37 pIC50 4.3 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of CLK4 (unknown origin) by Z'-LYTE assay B 9 pIC50 1 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
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 Binding affinity to human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 9.79 pKd 0.16 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 8.33 pIC50 4.7 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of DYRK1A (unknown origin) B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
ChEMBL Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 8.85 pIC50 1.4 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
GtoPdb Determined in a non-radioactive fluorescence resonance energy transfer (FRET) assay for kinase activity. - 9 pIC50 1 nM IC50 WO2020150552A2. Methods of treating cartilage disorders through inhibition of clk and dyrk (2020)
ChEMBL Inhibition of recombinant DYRK1A (unknown origin) using Ser/Thr 18 peptide as substrate incubated for 1 hr in presence of ATP by FRET assay B 9 pEC50 1 nM EC50 WO-2020150552-A2. Methods of treating cartilage disorders through inhibition of clk and dyrk (2020)
dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463]
ChEMBL Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.65 pIC50 22.4 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay B 8.44 pIC50 3.6 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of DYRK1B (unknown origin) B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630]
ChEMBL Inhibition of recombinant human DYRK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.39 pIC50 40.7 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of DYRK2 (unknown origin) B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
dual specificity tyrosine phosphorylation regulated kinase 3/Dual-specificity tyrosine-phosphorylation regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
ChEMBL Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5.68 pIC50 2104 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
ChEMBL Inhibition of recombinant human DYRK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 7.06 pIC50 86.4 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of DYRK4 (unknown origin) B 8.7 pIC50 2 nM IC50 Bioorg Med Chem (2022) 70: 116914-116914 [PMID:35872347]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Binding affinity to human GSK-3beta assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay B 5.93 pKd 1183 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant human GSK-3beta expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis B 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]

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]