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ChEMBL ligand: CHEMBL4438249 (Amdizalisib, Hmpl-689, HMPL-689) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | - | - | 9.52 | pIC50 | 0.3 | nM | IC50 | WO2016045591A1. Novel imidazopyridazine compounds and their use (2016) |
ChEMBL | Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells after 80 mins by fluorescence polarization assay | B | 9.52 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2019) 62: 4783-4814 [PMID:30582813] |
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 | - | - | 7.42 | pIC50 | 38 | nM | IC50 | WO2016045591A1. Novel imidazopyridazine compounds and their use (2016) |
ChEMBL | Inhibition of recombinant N-terminal His-tagged full length human PI3Kgamma expressed in baculovirus expression system after 80 mins by fluorescence polarization assay | B | 7.42 | pIC50 | 38 | nM | IC50 | J Med Chem (2019) 62: 4783-4814 [PMID:30582813] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta in Human [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
GtoPdb | - | - | 7.06 | pIC50 | 87 | nM | IC50 | WO2016045591A1. Novel imidazopyridazine compounds and their use (2016) |
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]