AZD3458 [Ligand Id: 9997] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4126156 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 4.5 | pIC50 | 31622.78 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| phosphatidylinositol 3-kinase catalytic subunit type 3/Phosphatidylinositol 3-kinase catalytic subunit type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075165] [GtoPdb: 2152] [UniProtKB: Q8NEB9] | ||||||||
| ChEMBL | Inhibition of PI3KC3 (unknown origin) | B | 5.1 | pIC50 | 7943.28 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736] | ||||||||
| GtoPdb | In a biochemical enzyme activity assay. | - | 9.1 | pIC50 | 0.79 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189158] [GtoPdb: 2156] [UniProtKB: Q9JHG7] | ||||||||
| ChEMBL | Inhibition of PI3Kgamma in mouse RAW264 cells assessed as reduction in Akt phosphorylation at Ser473 residue preincubated for 15 mins followed by C5a stimulation measured after 3 mins by TR-FRET assay | B | 8.1 | pIC50 | 7.94 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| ChEMBL | Inhibition of PI3Kgamma in C5a-stimulated mouse RAW 264 cells assessed as inhibition of AKT phosphorylation at Ser473 residue Pretreated for 15 mins followed by C5a stimulation measured after 3 mins by HTRF assay | B | 8.1 | pIC50 | 7.94 | nM | IC50 | J Med Chem (2021) 64: 8053-8075 [PMID:34080862] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 beta/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5554] [GtoPdb: 2151] [UniProtKB: O00750] | ||||||||
| ChEMBL | Inhibition of PI3KC2beta (unknown origin) | B | 7.5 | pIC50 | 31.62 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075102] [GtoPdb: 2150] [UniProtKB: O00443] | ||||||||
| ChEMBL | Inhibition of PI3KC2alpha (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 gamma/Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163120] [GtoPdb: 2288] [UniProtKB: O75747] | ||||||||
| ChEMBL | Inhibition of PI3KC2gamma (unknown origin) | B | 5.5 | pIC50 | 3162.28 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| 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 recombinant human 6His-tagged PI3K p110delta/p85alpha using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay | B | 6.5 | pIC50 | 316.23 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| GtoPdb | In a biochemical enzyme activity assay. | - | 6.5 | pIC50 | 316 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| 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 PI3Kdelta in human JeKo1B cells assessed as reduction in AKT phosphorylation at ser473 residue preincubated for 60 mins followed by anti-IgM stimulation measured after 10 mins by TR-FRET assay | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| ChEMBL | Inhibition of PI3Kdelta in anti-IgM-stimulated human JeKo-1 cells assessed as inhibition of AKT phosphorylation at Ser473 residue incubated for 60 mins by TR-FRET assay | B | 6.1 | pIC50 | >794.33 | nM | IC50 | J Med Chem (2021) 64: 8053-8075 [PMID:34080862] |
| ChEMBL | Inhibition of recombinant human PI3Kdelta assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by substrate addition measured after 60 mins by ADP-glo assay | B | 6.5 | pIC50 | 316.23 | nM | IC50 | J Med Chem (2021) 64: 8053-8075 [PMID:34080862] |
| GtoPdb | In a biochemical enzyme activity assay. | - | 6.5 | pIC50 | 316 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| 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] | ||||||||
| GtoPdb | In a biochemical enzyme activity assay. | - | 9.1 | pIC50 | 0.79 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| ChEMBL | Inhibition of recombinant human 6His-tagged PI3Kgamma (144 to 1102 residues) using DiC8-PIP2 as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by ADP-Glo assay | B | 9.1 | pIC50 | <=0.79 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| ChEMBL | Inhibition of recombinant human PI3Kgamma assessed as reduction in ADP production using Dic8-PIP2 as substrate pre-treated for 15 mins followed by substrate addition measured after 60 mins by ADP-glo assay | B | 9.1 | pIC50 | 0.79 | nM | IC50 | J Med Chem (2021) 64: 8053-8075 [PMID:34080862] |
| P2Y1 receptor/Purinergic receptor P2Y1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4315] [GtoPdb: 323] [UniProtKB: P47900] | ||||||||
| ChEMBL | Binding affinity to human P2Y1 receptor | B | 6 | pKi | <1000 | nM | Ki | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha in Human [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
| GtoPdb | In a biochemical enzyme activity assay. | - | 5.1 | pIC50 | 7943 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
| phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta in Human [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
| GtoPdb | In a biochemical enzyme activity assay. | - | 4.5 | pIC50 | >31600 | nM | IC50 | J Med Chem (2018) 61: 5435-5441 [PMID:29852070] |
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]
