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

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ChEMBL ligand: CHEMBL4784318
  • 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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  • 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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
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 (null)
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
GtoPdb - - 7.92 pIC50 12 nM IC50 WO2020150552A2. Methods of treating cartilage disorders through inhibition of clk and dyrk (2020)
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 (null)
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]
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 (null)

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]