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 GSK-3beta (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2023) 92: 117406-117406 [PMID:37536264] |
| 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 from NanoLuc-fused GSK-3-beta (unknown origin) transfected in HEK293 cells using tracer K8 incubated for 1 hr by NanoBRET assay | B | 8.38 | pIC50 | 4.19 | nM | IC50 | Eur J Med Chem (2022) 229: 114054-114054 [PMID:34959172] |
| ChEMBL | Inhibition of human wildtype full length GSK-3beta | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2023) 92: 117406-117406 [PMID:37536264] |
| ChEMBL | Inhibition of N-terminal His6-tagged GSK-3 beta (unknown origin) expressed in Rosetta 2DE3 cells | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem (2023) 92: 117406-117406 [PMID:37536264] |
| 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 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]
