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ChEMBL ligand: CHEMBL4850857 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]