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| ChEMBL ligand: CHEMBL2069623 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| casein kinase 1 alpha 1/Casein kinase I isoform alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| ChEMBL | Identification of CSNK1A1 Inhibitors: In order to identify inhibitors of CSNK1A1, the CSNK1A1 knockdown signatures in CMap were compared to all CMap compound signatures, and resultant compounds were ranked by strength of signature similarity. The top ranked compound from this analysis (compound 1) was predicted to act as a CSNK1A1 inhibitor.The CMap prediction was confirmed using Kinomescan (FIG. 1 ). Compound 1 bound to only six out of over 400 kinases tested in the assay, including CSNK1A1. | B | 6.07 | pIC50 | 857 | nM | IC50 | US-11633415-B2. Compounds and methods useful for treating or preventing cancers (2023) |
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | Inhibition of CK1delta | B | 6.15 | pIC50 | 711 | nM | IC50 | Eur J Med Chem (2012) 56: 30-38 [PMID:22944772] |
| ChEMBL | Inhibition of Casein kinase 1 delta | B | 6.15 | pIC50 | 711 | nM | IC50 | J Med Chem (2012) 55: 10307-10311 [PMID:23106386] |
| ChEMBL | Inhibition of human CK1delta in presence of [gamma33P]-ATP | B | 6.15 | pIC50 | 711 | nM | IC50 | Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711] |
| ChEMBL | Inhibition of CK1delta (unknown origin) | B | 6.15 | pIC50 | 711 | nM | IC50 | J Med Chem (2023) 66: 7162-7178 [PMID:37204207] |
| GtoPdb | - | - | 6.15 | pIC50 | 711 | nM | IC50 | J Pharmacol Exp Ther (2009) 330: 430-9 [PMID:19458106] |
| ChEMBL | Inhibition of human full length CK1delta1 (2 to 415 residues) using PLSRTLpSVASLPGL as substrate after 2 hrs by kinase-glo assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| GtoPdb | - | - | 7.49 | pIC50 | 32 | nM | IC50 | J Pharmacol Exp Ther (2009) 330: 430-9 [PMID:19458106] |
| ChEMBL | Inhibition of CK1epsilon | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2012) 56: 30-38 [PMID:22944772] |
| ChEMBL | Inhibition of Casein kinase 1 epsilon | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2012) 55: 10307-10311 [PMID:23106386] |
| ChEMBL | Inhibition of human full length polyhistidine-tagged CK1epsilon expressed in Escherichia coli BL21-Codon-Plus (DE3)-RIL using PLSRTLpSVASLPGL as substrate after 2 hrs by kinase-glo assay | B | 7.49 | pIC50 | 32 | nM | IC50 | Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261] |
| ChEMBL | Inhibition of human CK1epsilon in presence of [gamma33P]-ATP | B | 7.49 | pIC50 | 32 | nM | IC50 | Eur J Med Chem (2019) 181: 111581-111581 [PMID:31400711] |
| ChEMBL | Inhibition of CK1epsilon (unknown origin) | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (2023) 66: 7162-7178 [PMID:37204207] |
| ChEMBL | Inhibition of recombinant human full-length N-terminal GST-tagged CK1epsilon expressed in baculovirus infected Sf9 insect cells using casein as substrate measured after 60 mins by ADP-glo kinase assay | B | 8.13 | pEC50 | 7.4 | nM | EC50 | Blood (2017) 129: 88-99 [PMID:27784673] |
ChEMBL data shown on this page come from version 36:
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]