laduviglusib [Ligand Id: 8014] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL412142 (CHIR-911, CHIR-99021, CHR-00921, CHR00921, CT-99021, CT99021, FX03, Laduviglusib) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| ChEMBL | Inhibition of human PDK1 using unactivated AKT substrate in presence of COPC, DOPS and PIP3 activators after 1 hr by scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| ChEMBL | Inhibition of human CK1epsilon using biotin peptide substrate after 1 hr by scintillation counting method | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | Inhibition of human CDC2 using biotin histone H1 peptide substrate after 1 hr by scintillation counting method | B | 5.06 | pIC50 | 8800 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| GtoPdb | - | - | 5.06 | pIC50 | 8800 | nM | IC50 | Diabetes (2003) 52: 588-95 [PMID:12606497] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7] | ||||||||
| ChEMBL | Inhibition of CDK1/cyclinB | B | 5.06 | pIC50 | 8800 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| GtoPdb | - | - | 5.06 | pIC50 | 8800 | nM | IC50 | Diabetes (2003) 52: 588-95 [PMID:12606497] |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Inhibition of human bFGF receptor tyrosine kinase using KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2 peptide substrate after 1 hr by scintillation counting method | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Inhibition of GSK3alpha | B | 8 | pIC50 | 10 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| GtoPdb | - | - | 8.01 | pIC50 | 9.8 | nM | IC50 | Diabetes (2003) 52: 588-95 [PMID:12606497] |
| ChEMBL | Inhibition of human GSK3alpha using biotin-CREB peptide substrate after 1 hr by scintillation counting method | B | 8.11 | pIC50 | 7.8 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of GSK3-beta | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2012) 20: 1188-1200 [PMID:22261023] |
| ChEMBL | Inhibition of human recombinant GSK3-beta after 1 hr by KinaseGlo luciferase assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem (2012) 20: 1188-1200 [PMID:22261023] |
| ChEMBL | Inhibition of human recombinant GSK3beta using GSK3 peptide as substrate preincubated for 15 mins followed by ATP addition and measured after 90 mins by ADP-Glo kinase assay | B | 8 | pIC50 | 9.9 | nM | IC50 | Bioorg Med Chem (2021) 32: 115998-115998 [PMID:33440320] |
| ChEMBL | Inhibition of GSK3-beta | B | 8.15 | pIC50 | 7 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| ChEMBL | Inhibition of GSK3beta (unknown origin) | B | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2021) 210: 112949-112949 [PMID:33097303] |
| GtoPdb | - | - | 8.17 | pIC50 | 6.7 | nM | IC50 | Diabetes (2003) 52: 588-95 [PMID:12606497] |
| ChEMBL | Inhibition of human GSK3beta using biotin-CREB peptide substrate after 1 hr by scintillation counting method | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| ChEMBL | Inhibition of GSK3-beta in human HepG2 cells assessed as incorporation of [3H]glucose into glycogen after 3 hrs by liquid scintillation counting | B | 5.82 | pEC50 | 1500 | nM | EC50 | Bioorg Med Chem (2012) 20: 1188-1200 [PMID:22261023] |
| Insulin-like growth factor I receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1957] [GtoPdb: 1801] [UniProtKB: P08069] | ||||||||
| ChEMBL | Inhibition of human IGF1 receptor tyrosine kinase using biotin-GGGGKKKSPGEYVNIEFG-amide peptide substrate after 1 hr by scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of human insulin receptor tyrosine kinase after 1 hr by scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | >10000 | nM | IC50 | Diabetes (2003) 52: 588-95 [PMID:12606497] |
| ChEMBL | Inhibition of human ERK2 using myelin basic protein substrate after 1 hr by scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| protein kinase C zeta/Protein kinase C zeta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513] | ||||||||
| ChEMBL | Inhibition of human PKCzeta using biotin-PKC-86 peptide substrate after 30 mins in the presence of phosphatidylserine and diacylglycerol activators by scintillation counting | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition of human AKT1/PKB using phospho-AKT peptide substrate after 1 hr by scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Inhibition of human CHK1 using biotin-CDC25 peptide substrate after 1 hr by scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| TEK receptor tyrosine kinase/Tyrosine-protein kinase TIE-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4128] [GtoPdb: 1842] [UniProtKB: Q02763] | ||||||||
| ChEMBL | Inhibition of human Tie2 using biotin-GGGGAPDLYKDFLT peptide substrate after 1 hr by scintillation counting method | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| fms related receptor tyrosine kinase 1/Vascular endothelial growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1868] [GtoPdb: 1812] [UniProtKB: P17948] | ||||||||
| ChEMBL | Inhibition of human FLT1 using KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2 peptide substrate after 1 hr by scintillation counting method | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Inhibition of human KDR using KDRY1175 [B91616] biotin-GGGGQDGKDYIVLPI-NH2 peptide substrate after 1 hr by scintillation counting method | B | 5.3 | pIC50 | >5000 | nM | IC50 | J Med Chem (2017) 60: 8482-8514 [PMID:29016121] |
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]
