compound 1 [PMID: 20005102] [Ligand Id: 8181] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL593490 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 phosphorylation in human BT474 cells | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
| ChEMBL | Inhibition of PDK1 | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| Rho associated coiled-coil containing protein kinase 1/Rho-associated protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3231] [GtoPdb: 1503] [UniProtKB: Q13464] | ||||||||
| ChEMBL | Inhibition of ROCK1 | B | 5.8 | pIC50 | 1580 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 673-678 [PMID:20006497] |
| ChEMBL | Inhibition of ROCK1 | B | 5.8 | pIC50 | 1580 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| ribosomal protein S6 kinase B1/Ribosomal protein S6 kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4501] [GtoPdb: 1525] [UniProtKB: P23443] | ||||||||
| GtoPdb | - | - | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102] |
| ChEMBL | Inhibition of P70S6K | B | 8.15 | pIC50 | 7 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| 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 AKT1 in human BT474 cells assessed as phosphorylation of GSK3 | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 673-678 [PMID:20006497] |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102] |
| ChEMBL | Inhibition of full length AKT1 | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 673-678 [PMID:20006497] |
| ChEMBL | Inhibition of AKT1 | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] | ||||||||
| GtoPdb | - | - | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102] |
| ChEMBL | Inhibition of AKT2 | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102] |
| ChEMBL | Inhibition of AKT3 | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153] | ||||||||
| GtoPdb | - | - | 7.3 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102] |
| ChEMBL | Inhibition of PAK1 | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-683 [PMID:20005102] |
| 3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
| GtoPdb | - | - | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102] |
| protein kinase A in Human [GtoPdb: 1694] | ||||||||
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 679-83 [PMID:20005102] |
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]
