compound 26 [PMID: 34543009] [Ligand Id: 12810] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4850857
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
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  • calcium/calmodulin dependent serine protein kinase/Peripheral plasma membrane protein CASK in Human [ChEMBL: CHEMBL1908381] [GtoPdb: 1959] [UniProtKB: O14936]
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  • MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418]
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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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 tracer K5 binding to NanoLuc-fused CSNK1E (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay B 4.96 pIC50 10900 nM IC50 J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
calcium/calmodulin dependent serine protein kinase/Peripheral plasma membrane protein CASK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908381] [GtoPdb: 1959] [UniProtKB: O14936]
ChEMBL Binding affinity to recombinant N-terminal His-tagged CASK (1 to 337 residues) (unknown origin) expressed in Escherichia coli assessed as dissociation constant by isothermal titration calorimetry B 7.66 pKd 22 nM Kd J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
GtoPdb - - 7.66 pKd 22 nM Kd J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
ChEMBL Inhibition of tracer K5 binding to NanoLuc-fused CASK (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay B 7.96 pKi 11 nM Ki J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
ChEMBL Inhibition of tracer K5 binding to NanoLuc-fused CASK (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay B 7.1 pIC50 80 nM IC50 J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
GtoPdb - - 7.1 pIC50 80 nM IC50 J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
ChEMBL Inhibition of tracer K5 binding to NanoLuc-fused MERTK (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Inhibition of tracer K5 binding to NanoLuc-fused ABL1 (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418]
ChEMBL Inhibition of tracer K5 binding to NanoLuc-fused TYRO3 (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay B 5.42 pIC50 3790 nM IC50 J Med Chem (2021) 64: 14358-14376 [PMID:34543009]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Inhibition of tracer K5 binding to NanoLuc-fused AXL (unknown origin) expressed in HEK293T cells measured after 2 hrs by NanoBRET assay B 5 pIC50 >10000 nM IC50 J Med Chem (2021) 64: 14358-14376 [PMID:34543009]

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]