PF-06843195 [Ligand Id: 12720] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4756555 |
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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] | ||||||||
| GtoPdb | - | - | 10.74 | pKi | <0.02 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| ChEMBL | Inhibition of recombinant human full-length PI3K p110alpha/p85alpha (322 to 600) expressed in baculovirus infected Sf21 cells using phosphatidylinositol 4,5-bisphosphate as substrate preincubated for 15 mins followed by addition of ATP and measured after 30 mins by fluorescence polarisation assay | B | 10.74 | pKi | <0.02 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| 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] | ||||||||
| GtoPdb | - | - | 10.74 | pKi | <0.02 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| ChEMBL | Inhibition of recombinant human N-terminal Myr signal and C-terminal Flag-tagged PI3K p110alpha expressed in rat Rat1 cells | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| 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] | ||||||||
| GtoPdb | - | - | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| ChEMBL | Inhibition of recombinant human N-terminal Myr signal and C-terminal Flag-tagged PI3K p110beta expressed in rat Rat1 cells | B | 6.44 | pIC50 | 360 | nM | IC50 | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| 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] | ||||||||
| GtoPdb | - | - | 9.55 | pKi | <0.28 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| ChEMBL | Inhibition of recombinant human PI3K p110delta/p85alpha using phosphatidylinositol 4,5-bisphosphate as substrate preincubated for 15 mins followed by addition of ATP and measured after 30 mins by fluorescence polarisation assay | B | 9.55 | pKi | <0.28 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| 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 | - | - | 9.55 | pKi | <0.28 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| ChEMBL | Inhibition of recombinant human N-terminal Myr signal and C-terminal Flag-tagged PI3K p110delta expressed in rat Rat1 cells | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| 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 PI3K p110beta/p85alpha using phosphatidylinositol 4,5-bisphosphate as substrate preincubated for 15 mins followed by addition of ATP and measured after 30 mins by fluorescence polarisation assay | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| GtoPdb | - | - | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
| 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 mTOR in TSC1 null human MCF7 cells assessed as decrease in p70S6K phosphorylation at Thr389 residue incubated for 2 hrs by ELISA | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2021) 64: 644-661 [PMID:33356246] |
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]
