HS-173 [Ligand Id: 8243] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1765463 |
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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 recombinant human full-length N-terminal His-tagged p110alpha/p85alpha expressed in baculovirus expression system using PIP2 as substrate measured after 1 hr by kinase-glo assay | B | 8.3 | pIC50 | >5 | nM | IC50 | J Med Chem (2020) 63: 3028-3046 [PMID:32069401] |
| ChEMBL | Inhibition of N-terminal His6-tagged recombinant full-length human p110alpha/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate by HTRF colorimetric assay | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Eur J Med Chem (2017) 139: 95-106 [PMID:28800461] |
| GtoPdb | - | - | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2011) 54: 2455-66 [PMID:21388141] |
| 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] | ||||||||
| ChEMBL | Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate incubated for 1 hr in presence of ATP by Kinase-Glo plus luminescent assay | B | 8.3 | pIC50 | >5 | nM | IC50 | Eur J Med Chem (2023) 247: 115030-115030 [PMID:36586298] |
| ChEMBL | Inhibition of PI3Kalpha after 180 mins by luminescent assay | B | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2011) 54: 2455-2466 [PMID:21388141] |
| GtoPdb | - | - | 9.1 | pIC50 | 0.8 | nM | IC50 | J Med Chem (2011) 54: 2455-66 [PMID:21388141] |
| 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) using PIP2 as substrate by HTRF colorimetric assay | B | 7.23 | pIC50 | 59 | nM | IC50 | Eur J Med Chem (2017) 139: 95-106 [PMID:28800461] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/phosphoinositide-3-kinase regulatory subunit 1/PI3-kinase p110-delta/p85-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111432] [GtoPdb: 2155, 2503] [UniProtKB: O00329, P27986] | ||||||||
| ChEMBL | Inhibition of p110delta/p85alpha (unknown origin) using PIP2 as substrate by HTRF colorimetric assay | B | 7.06 | pIC50 | 87 | nM | IC50 | Eur J Med Chem (2017) 139: 95-106 [PMID:28800461] |
| 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 N-terminal His6-tagged recombinant full-length human PI3Kgamma expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate by HTRF colorimetric assay | B | 6.98 | pIC50 | 104 | nM | IC50 | Eur J Med Chem (2017) 139: 95-106 [PMID:28800461] |
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]
