BRL50481 [Ligand Id: 5154] activity data from GtoPdb and ChEMBL
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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 |
|---|---|---|---|---|---|---|---|---|
| phosphodiesterase 1B/Phosphodiesterase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4425] [GtoPdb: 1295] [UniProtKB: Q01064] | ||||||||
| ChEMBL | Inhibition of human PDE1B | B | 4.21 | pIC50 | 62000 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| phosphodiesterase 1C/Phosphodiesterase 1C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4619] [GtoPdb: 1296] [UniProtKB: Q14123] | ||||||||
| ChEMBL | Inhibition of human PDE1C | B | 4.21 | pIC50 | 62000 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition of human PDE2 | B | 4.21 | pIC50 | 62000 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815] | ||||||||
| ChEMBL | Inhibition of human PDE4A | B | 4.21 | pIC50 | 62000 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| 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 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
| ChEMBL | Inhibition of human PDE5 | B | 4.21 | pIC50 | 62000 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| 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 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] |
| 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 human PDE7A1 | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
| 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 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] |
| 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 | Displacement of [3H]-cAMP from recombinant human PDE7A1 incubated for 20 mins by scintillation proximity assay | B | 7.05 | pIC50 | 90 | nM | IC50 | Eur J Med Chem (2022) 232: 114170-114170 [PMID:35144038] |
| 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 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]
