D4476 [Ligand Id: 5940] 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: CHEMBL410456 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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 | 6.49 | pIC50 | 321 | nM | IC50 | US-11633415-B2. Compounds and methods useful for treating or preventing cancers (2023) |
| GtoPdb | - | - | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2012) 56: 30-8 [PMID:22944772] |
| ChEMBL | Inhibition of CK1 using KRRRALS(p)VASLPGL as substrate after 40 mins by scintillation counter | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2012) 56: 30-38 [PMID:22944772] |
| casein kinase 1 delta/Casein kinase I isoform delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| GtoPdb | - | - | 6.52 | pIC50 | 300 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| ChEMBL | Inhibition of CK1delta | B | 6.52 | pIC50 | 300 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of CK1delta in the presence of 100uM ATP | B | 6.52 | pIC50 | 300 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| ChEMBL | Inhibition of human CK1D using KRRRAL[pS]VASLPGL as substrate by [gamma-33P]-ATP assay | B | 6.77 | pIC50 | 171 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| ChEMBL | LanthaScreen Eu Kinase Binding Assay: Table 3: Small molecules were tested for their inhibitory activities towards casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ϵ). The in vitro LanthaScreen Eu kinase binding assay was used to determine the IC50 values for 15 of the synthesized compounds and 5 commercial inhibitors including SB203580 (Table 3). Tested compounds displayed a wide range of affinity between 6.8 nM (high affinity=strong inhibition) to values over 1000 nM (low affinity=very weak inhibition). | B | 6.8 | pIC50 | 157 | nM | IC50 | US-10865384-B2. 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis (2020) |
| casein kinase 1 delta/Casein kinase I isoform delta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4484] [GtoPdb: 1997] [UniProtKB: Q06486] | ||||||||
| ChEMBL | Inhibition of rat CK1delta in presence of 20 uM ATP | B | 6.45 | pIC50 | 353.3 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5578-5585 [PMID:24007918] |
| ChEMBL | Inhibition of GST-fused rat CK1delta expressed in Escherichia coli using phosphorylated peptide TFRPRTSpSNASTIS as substrate | B | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (2009) 52: 7618-7630 [PMID:19591487] |
| casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | Inhibition of human CK1E using KRRRAL[pS]VASLPGL as substrate by [gamma-33P]-ATP assay | B | 6.47 | pIC50 | 338 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| ChEMBL | LanthaScreen Eu Kinase Binding Assay: Table 3: Small molecules were tested for their inhibitory activities towards casein kinase 1 delta (CK1δ) and 1 epsilon (CK1ϵ). The in vitro LanthaScreen Eu kinase binding assay was used to determine the IC50 values for 15 of the synthesized compounds and 5 commercial inhibitors including SB203580 (Table 3). Tested compounds displayed a wide range of affinity between 6.8 nM (high affinity=strong inhibition) to values over 1000 nM (low affinity=very weak inhibition). | B | 7.06 | pIC50 | 88 | nM | IC50 | US-10865384-B2. 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis (2020) |
| Casein kinase II subunit alpha in Schizosaccharomyces pombe 972h- (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075255] [UniProtKB: P40231] | ||||||||
| ChEMBL | Inhibition of Schizosaccharomyces pombe CK1 | B | 6.7 | pIC50 | 200 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| mitogen-activated protein kinase 14/Mitogen-activated protein kinase 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Inhibition of p38alpha | B | 4.92 | pIC50 | 12000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of GST-fused human p38alpha expressed in Escherichia coli | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2009) 52: 7618-7630 [PMID:19591487] |
| ChEMBL | Inhibition of p38-alpha MAPK in the presence of 50uM ATP | B | 5.24 | pIC50 | 5800 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| ChEMBL | Inhibition of human p38alpha MAPK in presence of 50 uM ATP | B | 5.38 | pIC50 | 4154 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5578-5585 [PMID:24007918] |
| protein kinase D1/Serine/threonine-protein kinase D1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139] | ||||||||
| ChEMBL | Inhibition of PKD1 in the presence of 50uM ATP | B | 5.04 | pIC50 | 9100 | nM | IC50 | Biochem J (2007) 408: 297-315 [PMID:17850214] |
| transforming growth factor beta receptor 1/TGF-beta receptor type-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4439] [GtoPdb: 1788] [UniProtKB: P36897] | ||||||||
| ChEMBL | Inhibition of ALK5 | B | 6.3 | pIC50 | 500 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
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]
