SAR405 [Ligand Id: 9353] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3622372 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma/Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163120] [GtoPdb: 2288] [UniProtKB: O75747] | ||||||||
| ChEMBL | Inhibition of PI3KC2gamma (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| 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] | ||||||||
| GtoPdb | - | - | 8.82 | pKd | 1.52 | nM | Kd | Nat Chem Biol (2014) 10: 1013-9 [PMID:25326666] |
| ChEMBL | Competitive inhibition of VPS34 (unknown origin) incubated for 15 mins in presence of ATP by ELISA | B | 7.42 | pIC50 | 38 | nM | IC50 | Eur J Med Chem (2023) 256: 115467-115467 [PMID:37178482] |
| ChEMBL | Inhibition of Vps34 in human HeLa cells expressing GFP-FYVE | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| ChEMBL | Inhibition of recombinant human Vps34 by TR-FRET analysis | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2015) 58: 7611-7633 [PMID:26086931] |
| ChEMBL | Competitive inhibition of recombinant human VPS34 in presence of ATP by TR-FRET assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | Eur J Med Chem (2023) 256: 115467-115467 [PMID:37178482] |
| ChEMBL | Inhibition of Vps34 (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| ChEMBL | Inhibition of Vps34 (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| ChEMBL | Inhibition of human PIK3C3 using PI as substrate by ADP-Glo assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2024) 267: 116117-116117 [PMID:38295689] |
| ChEMBL | Inhibition of human VPS34 assessed as reduction in PIP3 product complex formation | B | 8.92 | pEC50 | 1.2 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| ChEMBL | Inhibition of human VPS34 assessed as reduction in PIP3 product complex formation measured after 30 mins in presence of ATP by quantitative PI3P ELISA assay | B | 8.95 | pEC50 | 1.11 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| 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 human PI3Kalpha by TR-FRET analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7611-7633 [PMID:26086931] |
| ChEMBL | Inhibition of PI3K p110alpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 4656-4687 [PMID:29211480] |
| ChEMBL | Inhibition of PI3K alpha (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| 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 recombinant human PI3Kbeta by TR-FRET analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7611-7633 [PMID:26086931] |
| ChEMBL | Inhibition of PI3K beta (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| ChEMBL | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation measured after 30 mins in presence of ATP by quantitative PI3P ELISA assay | B | 8 | pEC50 | >10 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| ChEMBL | Inhibition of human PI3Kbeta assessed as reduction in PIP3 product complex formation | B | 8 | pEC50 | >10 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| 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 recombinant human PI3Kdelta by TR-FRET analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7611-7633 [PMID:26086931] |
| 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 recombinant human PI3Kgamma by TR-FRET analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7611-7633 [PMID:26086931] |
| ChEMBL | Inhibition of PI3K gamma (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| 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 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| ChEMBL | Inhibition of PIK3C2A (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750] | ||||||||
| ChEMBL | Inhibition of PI3KC2beta (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2017) 60: 47-65 [PMID:27644332] |
| ChEMBL | Inhibition of PIK3C2B (unknown origin) | B | 5 | pEC50 | >10000 | nM | EC50 | Biochemistry (2017) 56: 4326-4334 [PMID:28719179] |
| 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 recombinant human mTOR by TR-FRET analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2015) 58: 7611-7633 [PMID:26086931] |
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]
