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: CHEMBL1213082 |
---|
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 |
---|---|---|---|---|---|---|---|---|
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) | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
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) | B | 4.12 | pIC50 | 75000 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
ChEMBL | Inhibition of p110beta | B | 4.8 | pIC50 | 16000 | nM | IC50 | Nat Chem Biol (2010) 6: 117-124 [PMID:20081827] |
ChEMBL | Inhibition of PI3Kbeta in presence of 10 uM ATP | B | 4.8 | pIC50 | 16000 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
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 | - | - | 7.7 | pKi | ~20 | nM | Ki | Chem Biol (2005) 12: 621-37 [PMID:15975507] |
ChEMBL | Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PI:PS as substrate after 60 mins by ADP-Glo assay | B | 7.7 | pKi | 19.95 | nM | Ki | J Med Chem (2017) 60: 4304-4315 [PMID:28489362] |
ChEMBL | Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110delta/p85alpha expressed in baculovirus infected Sf9 insect cells using PI:PS as substrate after 60 mins by ADP-Glo assay | B | 7.9 | pKi | 12.59 | nM | Ki | J Med Chem (2017) 60: 4304-4315 [PMID:28489362] |
GtoPdb | - | - | 6.3 | pIC50 | 500 | nM | IC50 | J Immunol (2003) 170: 2647-54 [PMID:12594293] |
ChEMBL | Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay | B | 6.89 | pIC50 | 130 | nM | IC50 | ACS Med Chem Lett (2017) 8: 118-123 [PMID:28105286] |
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 p110delta | B | 7.7 | pKi | 20 | nM | Ki | Chem Biol (2005) 12: 621-637 [PMID:15975507] |
GtoPdb | - | - | 7.7 | pKi | ~20 | nM | Ki | Chem Biol (2005) 12: 621-37 [PMID:15975507] |
GtoPdb | - | - | 6.3 | pIC50 | 500 | nM | IC50 | J Immunol (2003) 170: 2647-54 [PMID:12594293] |
ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 6.3 | pIC50 | 500 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
ChEMBL | Inhibition of PI3Kdelta in presence of 200 uM ATP | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
ChEMBL | Inhibition of PI3K-delta (unknown origin) by cell free biochemical assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1005-1010 [PMID:29486969] |
ChEMBL | Inhibition of p110delta | B | 6.89 | pIC50 | 130 | nM | IC50 | Nat Chem Biol (2010) 6: 117-124 [PMID:20081827] |
ChEMBL | Inhibition of PI3Kdelta in presence of 10 uM ATP | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
ChEMBL | Inhibition of PI3K-delta (unknown origin) expressed in baculovirus infected Sf9 insect cells after 10 mins in presence of [gamma-32P]ATP by radioligand binding assay | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1005-1010 [PMID:29486969] |
ChEMBL | Inhibition of PI3Kdelta in human PBMC assessed as reduction in anti-human CD28 antibody stimulated IL-6 secretion levels after 72 hrs by ELISA | B | 7.3 | pIC50 | 50.12 | nM | IC50 | J Med Chem (2017) 60: 4304-4315 [PMID:28489362] |
ChEMBL | Inhibition of PI3Kdelta in human PBMC assessed as reduction in anti-human CD28 antibody stimulated IL-6 secretion levels after 72 hrs by ELISA | B | 7.6 | pIC50 | 25.12 | nM | IC50 | J Med Chem (2017) 60: 4304-4315 [PMID:28489362] |
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 PI3K-gamma (unknown origin) by cell free biochemical assay | B | 4.15 | pIC50 | 70000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1005-1010 [PMID:29486969] |
ChEMBL | Inhibition of p110gamma | B | 4.21 | pIC50 | 61000 | nM | IC50 | Nat Chem Biol (2010) 6: 117-124 [PMID:20081827] |
ChEMBL | Inhibition of PI3Kgamma in presence of 10 uM ATP | B | 4.21 | pIC50 | 61000 | nM | IC50 | J Med Chem (2012) 55: 8559-8581 [PMID:22924688] |
ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 4.54 | pIC50 | 29000 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
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]