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 (2020) |
| ChEMBL | Inhibition of P13Kalpha (unknown origin) | B | 7.85 | pIC50 | 14 | nM | IC50 | Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440] |
| 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 (2020) |
| 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 (2020) |
| 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 (2020) |
| 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 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]
