paxalisib [Ligand Id: 10097] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3813842 (G-02441729, G02441729, GDC-0084, GDC0084, Paxalisib, Rg-7666, RG 7666, Sim-0395) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| mechanistic target of rapamycin kinase/mTORC1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296661] [GtoPdb: 2109] [UniProtKB: P42345, Q8N122, Q9BVC4] | ||||||||
| ChEMBL | Binding affinity to mTORC1 (unknown origin) assessed as apparent inhibition constant in presence of ATP by TR-FRET assay | B | 7.15 | pKi | 70 | nM | Ki | Eur J Med Chem (2024) 265: 116109-116109 [PMID:38183777] |
| GtoPdb | - | - | 7.15 | pIC50 | 70 | nM | IC50 | ACS Med Chem Lett (2016) 7: 351-6 [PMID:27096040] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| ChEMBL | Inhibition of recombinant PI3Kalpha (unknown origin) using dioctanoylglycerol-PIP2 as substrate incubated for 30 mins in presence of TAMRA-PIP3 by fluorescence polarization assay | B | 8.7 | pKi | 2 | nM | Ki | ACS Med Chem Lett (2016) 7: 351-356 [PMID:27096040] |
| ChEMBL | Inhibition of P13Kalpha (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440] |
| GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | ACS Med Chem Lett (2016) 7: 351-6 [PMID:27096040] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| ChEMBL | Inhibition of P13Kbeta (unknown origin) | B | 7.34 | pIC50 | 46 | nM | IC50 | Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
| ChEMBL | Inhibition of P13Kdelta (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| ChEMBL | Inhibition of P13Kgamma (unknown origin) | B | 8 | pIC50 | 10 | nM | IC50 | Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440] |
| 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 human recombinant mTOR (1360 to 2549 residues) expressed in insect cells assessed as inhibition of GFP-labeled 4-EBP1 phosphorylation at Thr-37/46 residues incubated for 30 mins by FRET assay | B | 7.15 | pKi | 70 | nM | Ki | ACS Med Chem Lett (2016) 7: 351-356 [PMID:27096040] |
| GtoPdb | - | - | 7.15 | pIC50 | 70 | nM | IC50 | ACS Med Chem Lett (2016) 7: 351-6 [PMID:27096040] |
| ChEMBL | Inhibition of mTOR (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2023) 246: 114971-114971 [PMID:36462440] |
ChEMBL data shown on this page come from version 36:
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]
