dezapelisib [Ligand Id: 9728] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2216863 (Dezapelisib, INCB040093) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111367] [GtoPdb: 2503, 2153] [UniProtKB: P27986, P42336] | ||||||||
| ChEMBL | Inhibition of human N-terminal His-tagged PI3Kalpha/p85alpha expressed in Spodoptera frugiperda using phosphatidylinositol as substrate | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
| GtoPdb | - | - | 6.3 | pIC50 | >500 | nM | IC50 | WO2011008487. Pyrimidinones as PI3K inhibitors (2011) |
| 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 | The same value was obtained using an enzyme activity assay and a scintillation proximity assay. | - | 7.3 | pIC50 | <50 | nM | IC50 | WO2011008487. Pyrimidinones as PI3K inhibitors (2011) |
| ChEMBL | Inhibition of PI3Kdelta in B-cells by proliferation assay | B | 7.3 | pIC50 | <50 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
| ChEMBL | Inhibition of PI3Kdelta | B | 7.3 | pIC50 | <50 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 7.51 | pIC50 | 31 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
| ChEMBL | Inhibition of PI3Kdelta in basophil derived from B-cell malignant patient | B | 7.51 | pIC50 | 31 | nM | IC50 | J Med Chem (2019) 62: 4783-4814 [PMID:30582813] |
| ChEMBL | Inhibition of PI3Kdelta (unknown origin) using D-myophosphatidylinositol 4,5-bisphosphate as substrate incubated for 120 mins by [gamma-33P]ATP based SPA assay | B | 8.47 | pIC50 | 3.4 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1554-1560 [PMID:31749910] |
| 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] | ||||||||
| ChEMBL | Inhibition of PI3Kgamma in basophil derived from B-cell malignant patient | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (2019) 62: 4783-4814 [PMID:30582813] |
| ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 5.64 | pIC50 | 2297 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
| GtoPdb | - | - | 6.3 | pIC50 | >500 | nM | IC50 | WO2011008487. Pyrimidinones as PI3K inhibitors (2011) |
| phosphoinositide-3-kinase regulatory subunit 1/phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3K p110 beta/p85 alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038510] [GtoPdb: 2503, 2154] [UniProtKB: P27986, P42338] | ||||||||
| ChEMBL | Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells | B | 5.43 | pIC50 | 3751 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
| GtoPdb | - | - | 6.3 | pIC50 | >500 | nM | IC50 | WO2011008487. Pyrimidinones as PI3K inhibitors (2011) |
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]
