KH-CB19 [Ligand Id: 8055] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1236620
  • 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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  • CDC like kinase 1/Dual specificty protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL Inhibition of human recombinant CLK3 (275 to 632 amino acids) expressed in Escherichia coli BL21(DE3) preincubated for 10 mins prior to substrate addition by LDH assay B 6.28 pIC50 530 nM IC50 Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479]
GtoPdb - - 6.28 pIC50 530 nM IC50 Chem Biol (2011) 18: 67-76 [PMID:21276940]
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) using YRASPSRPESPRPPA-NH2 as substrate preincubated for 10 mins prior to substrate addition by LDH assay B 7.26 pIC50 55 nM IC50 Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479]
ChEMBL Inhibition of DYRK1A (unknown origin) using YRASPSRPESPRPPA-amide as substrate preincubated for 10 mins followed by substrate addition and measured after 60 mins by caliper mobility shift assay B 7.26 pIC50 55 nM IC50 J Med Chem (2018) 61: 9791-9810 [PMID:29985601]
GtoPdb - - 7.26 pIC50 55.2 nM IC50 Chem Biol (2011) 18: 67-76 [PMID:21276940]
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL Inhibition of human recombinant CLK1 (148 to 484 amino acids) expressed in Escherichia coli BL21(DE3) using AFRREWSPGKEAKK as substrate preincubated for 10 mins prior to substrate addition by LDH assay B 7.7 pIC50 20 nM IC50 Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479]
GtoPdb - - 7.71 pIC50 19.7 nM IC50 Chem Biol (2011) 18: 67-76 [PMID:21276940]
ChEMBL Inhibition of recombinant human CLK1 (130 to end residues) using ERMRPRKRQGSVRRRV as substrate incubated for 40 mins in presence of [gamma33P-ATP] by scintillation counting analysis B 8.1 pIC50 8 nM IC50 Bioorg Med Chem (2021) 31: 115962-115962 [PMID:33422908]

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]