IC-87114 [Ligand Id: 9376] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1213082 |
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| 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 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]
