AZ191 [Ligand Id: 9268] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3421968
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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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 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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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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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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  • Insulin-like growth factor I receptor in Human [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
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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 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of human recombinant full length C-terminal His6-tagged CDK2 expressed in baculovirus infected Sf21 insect cells using fluorescence substrate after 60 mins by caliper off-chip incubation mobility shift assay B 5.35 pIC50 4473 nM IC50 J Med Chem (2015) 58: 2834-2844 [PMID:25738750]
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 5.98 pIC50 1058 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 5.46 pIC50 3503 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 5 pIC50 >10000 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 6.39 pIC50 403.1 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 8.59 pKd 2.57 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of human DYRK1A incubated for 90 mins in presence of ATP by Z-LYTE based FRET assay B 8.36 pKi 4.4 nM Ki Bioorg Med Chem Lett (2022) 68: 128764-128764 [PMID:35504513]
ChEMBL Inhibition of Dyrk1A (unknown origin) B 4.52 pIC50 30000 nM IC50 J Med Chem (2015) 58: 2834-2844 [PMID:25738750]
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 6.7 pIC50 199.9 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of NanoLuc-fused human DYRK1A expressed in HEK293 cells using Nano-Glo as substrate incubated for 2 hrs by NanoBRET assay B 6.82 pIC50 153 nM IC50 Bioorg Med Chem Lett (2022) 68: 128764-128764 [PMID:35504513]
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 7.72 pIC50 19.1 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of DYRK1A (unknown origin) B 7.77 pIC50 17 nM IC50 Eur J Med Chem (2018) 158: 559-592 [PMID:30243157]
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 human DYRK1B incubated for 130 mins in presence of ATP by ADP-Glo kinase assay B 7.95 pKi 11.2 nM Ki Bioorg Med Chem Lett (2022) 68: 128764-128764 [PMID:35504513]
ChEMBL Inhibition of NanoLuc-fused human DYRK1B expressed in HEK293T cells using Nano-Glo as substrate incubated for 2 hrs by NanoBRET assay B 7.09 pIC50 81 nM IC50 Bioorg Med Chem Lett (2022) 68: 128764-128764 [PMID:35504513]
ChEMBL Inhibition of human full length C-terminal c-Myc tagged Dyrk1B phosphorylation overexpressed in monkey COS1 cells after 5 hrs by ELISA B 7.38 pIC50 42 nM IC50 J Med Chem (2015) 58: 2834-2844 [PMID:25738750]
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 7.75 pIC50 17.9 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of DYRK1B (unknown origin) B 7.77 pIC50 17 nM IC50 Eur J Med Chem (2018) 158: 559-592 [PMID:30243157]
GtoPdb - - 7.77 pIC50 17 nM IC50 J Med Chem (2015) 58: 2834-44 [PMID:25738750]
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 8.08 pIC50 8.3 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL Inhibition of recombinant Dyrk1B (unknown origin) using FITC-Asp-His-Thr-Gly-Phe-Leu-Thr-Glu-Tyr-Val-Ala-Thr-Arg-NH2 as substrate after 60 mins B 8.52 pIC50 3 nM IC50 J Med Chem (2015) 58: 2834-2844 [PMID:25738750]
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 6.12 pIC50 764.3 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 5.91 pIC50 1220 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 5.2 pIC50 6246 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 1/Dual specificty 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 8.13 pKd 7.35 nM Kd J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 6.25 pIC50 567.6 nM IC50 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 6.76 pIC50 175 nM IC50 J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 pKd >10000 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]
Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069]
ChEMBL Inhibition of human recombinant N-terminal His6-tagged IGF-1R using fluorescence substrate after 80 mins by caliper off-chip incubation mobility shift assay B 6.11 pIC50 779 nM IC50 J Med Chem (2015) 58: 2834-2844 [PMID:25738750]

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]