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 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]
