izorlisib [Ligand Id: 7743] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1684984 (Ch 5132799, CH-5132799, CH5132799, Izorlisib, Pa-799, PA-799, PA799) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] | ||||||||
| ChEMBL | Inhibition of Vps34 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750] | ||||||||
| ChEMBL | Inhibition of PI3KC2beta | B | 5.28 | pIC50 | 5300 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443] | ||||||||
| ChEMBL | Inhibition of PI3KC2alpha | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| GtoPdb | - | - | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-72 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kalpha | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | WO-2020056269-A1. Methods for treating centronuclear myopathy (null) |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| ChEMBL | Inhibition of PI3Kbeta (unknown origin) | B | 6.3 | pIC50 | 500 | nM | IC50 | WO-2020056269-A1. Methods for treating centronuclear myopathy (null) |
| GtoPdb | - | - | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-72 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kbeta | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kbeta (unknown origin) | B | 6.92 | pIC50 | 120 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| GtoPdb | - | - | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-72 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kdelta | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 6.3 | pIC50 | 500 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 6.92 | pIC50 | 120 | nM | IC50 | WO-2020056269-A1. Methods for treating centronuclear myopathy (null) |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| GtoPdb | - | - | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-72 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kgamma | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | WO-2020056269-A1. Methods for treating centronuclear myopathy (null) |
| mechanistic target of rapamycin kinase/Serine/threonine-protein kinase mTOR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2842] [GtoPdb: 2109] [UniProtKB: P42345] | ||||||||
| ChEMBL | Inhibition of mTOR | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-1772 [PMID:21316229] |
| GtoPdb | - | - | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1767-72 [PMID:21316229] |
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]
