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ChEMBL ligand: CHEMBL484928 (BRL-50481) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
ChEMBL | Inhibition of human recombinant PDE4B2 assessed after 60 mins by IMAP fluorescence polarization assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2014) 57: 8590-8607 [PMID:25264825] |
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
ChEMBL | Inhibition of human recombinant PDE4D3 assessed after 60 mins by IMAP fluorescence polarization assay | B | 5.89 | pIC50 | 1280 | nM | IC50 | J Med Chem (2014) 57: 8590-8607 [PMID:25264825] |
phosphodiesterase 7A/Phosphodiesterase 7A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946] | ||||||||
ChEMBL | Inhibition of human recombinant PDE7A using cAMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assay | B | 5.63 | pIC50 | 2320 | nM | IC50 | Eur J Med Chem (2021) 209: 112854-112854 [PMID:33022582] |
ChEMBL | Inhibition of human recombinant PDE7A1 expressed in baculovirus-infected insect Sf9 cells by modified two-step method | B | 5.66 | pIC50 | 2200 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 2129-2132 [PMID:19303290] |
ChEMBL | Inhibition of human GST-tagged PDE7A expressed in baculovirus infected Sf9 insect cells using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | Eur J Med Chem (2018) 146: 381-394 [PMID:29407965] |
ChEMBL | Inhibition of recombinant human PDE7A using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay | B | 5.68 | pIC50 | 2100 | nM | IC50 | Eur J Med Chem (2018) 158: 517-533 [PMID:30245393] |
GtoPdb | - | - | 6.8 | pIC50 | - | - | - |
Mol Pharmacol (2004) 66: 1679-89 [PMID:15371556]; J Biomol Screen (2010) 15: 359-67 [PMID:20228279] |
ChEMBL | Inhibition of human recombinant PDE7A1-mediated [3H]cAMP hydrolysis after 20 mins by scintillation proximity assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2012) 55: 3274-3284 [PMID:22385507] |
ChEMBL | Inhibition of human recombinant PDE7A1 assessed as inhibition of hydrolysis of [3H]cAMP after 20 mins by scintillation proximity assay | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2014) 57: 8590-8607 [PMID:25264825] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
phosphodiesterase 7B in Human [GtoPdb: 1306] [UniProtKB: Q9NP56] | ||||||||
GtoPdb | - | - | 4.9 | pIC50 | - | - | - | J Biomol Screen (2010) 15: 359-67 [PMID:20228279] |
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]