PF-06843195 [Ligand Id: 12720] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL4756555 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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]
