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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL4850857
  • casein kinase 1 epsilon/Casein kinase I epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
There should be some charts here, you may need to enable JavaScript!
  • calcium/calmodulin dependent serine protein kinase/Peripheral plasma membrane protein CASK in Human [ChEMBL: CHEMBL1908381] [GtoPdb: 1959] [UniProtKB: O14936]
There should be some charts here, you may need to enable JavaScript!
  • MER proto-oncogene, tyrosine kinase/Proto-oncogene tyrosine-protein kinase MER in Human [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
There should be some charts here, you may need to enable JavaScript!
  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
There should be some charts here, you may need to enable JavaScript!
  • TYRO3 protein tyrosine kinase/Tyrosine-protein kinase receptor TYRO3 in Human [ChEMBL: CHEMBL5314] [GtoPdb: 1836] [UniProtKB: Q06418]
There should be some charts here, you may need to enable JavaScript!
  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
There should be some charts here, you may need to enable JavaScript!
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 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]