TGX-221 [Ligand Id: 8244] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1972466 |
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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 full length p110alpha/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay | B | 5.12 | pIC50 | 7600 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006] |
| 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 N-terminal ploy-His-tagged human PI3Kalpha expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2014) 57: 903-920 [PMID:24387221] |
| ChEMBL | Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| ChEMBL | Inhibition of human recombinant PI3Kalpha assessed as PIP3 production by AlphaScreen assay | B | 5.24 | pIC50 | 5800 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3936-3943 [PMID:25042253] |
| ChEMBL | Inhibition of human recombinant His6-tagged PI3K p110alpha expressed in baculovirus using DiC8-PI(4,5)P2 as substrate after 20 mins by AlphaScreen assay | B | 5.24 | pIC50 | 5700 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6665-6670 [PMID:23010274] |
| ChEMBL | Inhibition of N-terminal His-tagged human p110alpha expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem (2015) 23: 3796-3808 [PMID:25890698] |
| ChEMBL | Inhibition of PI3K p110alpha (unknown origin) | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2015) 58: 41-71 [PMID:25387153] |
| ChEMBL | Inhibition of human PI3Kalpha-mediated Akt phosphorylation at Ser473 residue expressed in human H460 cells after 0.5 to 2 hrs by Western blot analysis | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| 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 PI3K p110beta (unknown origin) | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2015) 58: 41-71 [PMID:25387153] |
| ChEMBL | Inhibition of PI3Kbeta (unknown origin) expressed in Escherichia coli-infected fall armyworm sf21 cells co-expressing p85 by kinase-glo luminescence assay | B | 7.28 | pIC50 | 52 | nM | IC50 | Eur J Med Chem (2016) 122: 339-351 [PMID:27387421] |
| ChEMBL | Inhibition of human recombinant His6-tagged PI3K p110beta expressed in baculovirus using DiC8-PI(4,5)P2 as substrate after 20 mins by AlphaScreen assay | B | 7.31 | pIC50 | 49 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6665-6670 [PMID:23010274] |
| ChEMBL | Inhibition of human recombinant PI3Kbeta assessed as PIP3 production by AlphaScreen assay | B | 7.31 | pIC50 | 49 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3936-3943 [PMID:25042253] |
| ChEMBL | Inhibition of N-terminal ploy-His-tagged human PI3Kbeta expressed in baculovirus-infected sf21 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2014) 57: 903-920 [PMID:24387221] |
| ChEMBL | Inhibition of N-terminus poly-His tagged human PI3Kbeta expressed in baculovirus infected insect S21 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| ChEMBL | Inhibition of PI3Kbeta in human MAD-MB-468 cells assessed as inhibition of Ser473 Akt phosphorylation by cellular potency assay | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3928-3935 [PMID:24992874] |
| ChEMBL | Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in mouse MEF-3T3 cells after 0.5 to 2 hrs by Western blot analysis | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| ChEMBL | Inhibition of PI3Kbeta-mediated Akt phosphorylation at S473 in PTEN-deficient human PC3 cells after 0.5 to 2 hrs by Immunoblotting assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2014) 57: 903-920 [PMID:24387221] |
| ChEMBL | Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | Nat Med (2005) 11: 507-14 [PMID:15834429] |
| ChEMBL | Inhibition of N-terminal His-tagged human p110beta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2015) 23: 3796-3808 [PMID:25890698] |
| ChEMBL | Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| 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 human p110delta catalytic subunit/p85alpha using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay | B | 6.3 | pIC50 | 500 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006] |
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | Nat Med (2005) 11: 507-14 [PMID:15834429] |
| 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] | ||||||||
| ChEMBL | Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay | B | 6.07 | pIC50 | 851 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| ChEMBL | Inhibition of N-terminal ploy-His-tagged human PI3Kdelta expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay | B | 6.07 | pIC50 | 851 | nM | IC50 | J Med Chem (2014) 57: 903-920 [PMID:24387221] |
| ChEMBL | Inhibition of human PI3Kdelta-mediated Akt phosphorylation at Ser473 residue expressed in mouse MEF-3T3 cells after 0.5 to 2 hrs by Western blot analysis | B | 6.6 | pIC50 | 252 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| ChEMBL | Inhibition of N-terminal His-tagged human p110delta expressed in Sf9 cells co-expressing p85alpha regulatory subunit using phosphatidylinositol substrate and [gamma-33P]-ATP by basic thin layer chromatography technique based lipid kinase assay | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem (2015) 23: 3796-3808 [PMID:25890698] |
| GtoPdb | - | - | 7 | pIC50 | 100 | nM | IC50 | Nat Med (2005) 11: 507-14 [PMID:15834429] |
| 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-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| ChEMBL | Inhibition of C-terminal ploy-His-tagged human PI3Kgamma expressed in baculovirus-infected sf9 cells using PI(4,5)P2 as substrate after 15 mins by HTRF assay | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2014) 57: 903-920 [PMID:24387221] |
| ChEMBL | Inhibition of human full length p110gamma using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006] |
| ChEMBL | Inhibition of human PI3Kgamma-mediated Akt phosphorylation at Ser473 residue expressed in mouse RAW264.7 cells after 0.5 to 2 hrs by Western blot analysis | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2012) 55: 4788-4805 [PMID:22524426] |
| 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 recombinant human full-length N-terminal His6-tagged p110beta/human recombinant full-length untagged p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate after 30 mins in presence of ATP at 2xKm concentration by TR-FRET assay | B | 7.2 | pIC50 | 63 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1236-1243 [PMID:32551006] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | Nat Med (2005) 11: 507-14 [PMID:15834429] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
