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ChEMBL ligand: CHEMBL511115 (Ariflo, Cilomilast, SB 207499, SB-207499, SB207499) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Class 1 phosphodiesterase PDEB1 in Trypanosoma brucei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010636] [UniProtKB: Q8WQX9] | ||||||||
ChEMBL | Inhibition of Trypanosoma brucei recombinant PDEB1 pre-incubated for 5 mins prior to substrate addition | B | 4.8 | pIC50 | 16000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4084-4089 [PMID:25127163] |
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
ChEMBL | Inhibition of human Phosphodiesterase 2 from peripheral blood mononuclear cells | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 233-235 [PMID:11755362] |
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815] | ||||||||
ChEMBL | Inhibitory concentration of compound against LPS- induced TNF-alpha production in whole human blood assay | F | 4.74 | pIC50 | 18000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1457-1461 [PMID:12031319] |
ChEMBL | Inhibitory activity against Phosphodiesterase 4A (PDE4A) from human source expressed in Saccharomyces cerevisiae | B | 6.39 | pIC50 | 410 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
ChEMBL | Inhibition of human recombinant PDE4A | B | 6.4 | pIC50 | 398 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
ChEMBL | Inhibition of human Phosphodiesterase 4A from peripheral blood mononuclear cells | B | 6.4 | pIC50 | 398 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 233-235 [PMID:11755362] |
ChEMBL | Inhibition of PDE4A (unknown origin) | B | 6.8 | pIC50 | 160 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
ChEMBL | Inhibition of human recombinant PDE4A | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2007) 50: 344-349 [PMID:17228876] |
ChEMBL | Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells | B | 7.21 | pIC50 | 62 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4308-4314 [PMID:23806553] |
ChEMBL | Inhibition of human Phosphodiesterase 4A isoform using construct representing the common region of spliced variants expressed as GST-fusion proteins in Sf9 cells. | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 3009-3013 [PMID:12270195] |
ChEMBL | Inhibitory concentration against human PDE4A isoform using a construct representing the common region of spliced variants expressed as GST-fusion protein in Sf9 cells | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1457-1461 [PMID:12031319] |
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
ChEMBL | Inhibition of human Phosphodiesterase 4B from peripheral blood mononuclear cells | B | 6.54 | pIC50 | 288 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 233-235 [PMID:11755362] |
ChEMBL | Inhibition of human recombinant PDE4B | B | 6.54 | pIC50 | 288 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
ChEMBL | Inhibition of human recombinant PDE4B2 assessed as inhibition of cAMP hydrolysis by colorimetric assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734] |
ChEMBL | Inhibition of PDE4B (unknown origin) | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
ChEMBL | Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1523-1526 [PMID:22297114] |
ChEMBL | Inhibition of human recombinant PDE4B by liquid scintillation counter method | B | 7.02 | pIC50 | 95 | nM | IC50 | Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823] |
ChEMBL | Inhibition of PDE4B2 (unknown origin) | B | 7.02 | pIC50 | 95 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734] |
ChEMBL | Inhibition of human recombinant PDE4B | B | 7.08 | pIC50 | 84 | nM | IC50 | J Med Chem (2007) 50: 344-349 [PMID:17228876] |
ChEMBL | Inhibitory activity against recombinant phosphodiesterase 4B (PDE4B) of human mononuclear lymphocytes | B | 7.15 | pIC50 | 71 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 653-658 [PMID:11844693] |
ChEMBL | Inhibition of human PDE4B1 incubated for 10 mins using cAMP and [3H]cAMP substrates | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3174-3176 [PMID:19447034] |
ChEMBL | Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
ChEMBL | Inhibition of human PDE4B | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577] |
phosphodiesterase 4B/Phosphodiesterase 4B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3382] [GtoPdb: 1301] [UniProtKB: P14646] | ||||||||
ChEMBL | Inhibitory activity against Phosphodiesterase 4B (PDE4B) from rat source expressed in Saccharomyces cerevisiae | B | 6.51 | pIC50 | 310 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493] | ||||||||
ChEMBL | Inhibition of PDE4C (unknown origin) | B | 5.06 | pIC50 | 8700 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
ChEMBL | Inhibitory activity against Phosphodiesterase 4C (PDE4C) from human source expressed in Saccharomyces cerevisiae | B | 6.08 | pIC50 | 840 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
ChEMBL | Inhibition of human Phosphodiesterase 4C from peripheral blood mononuclear cells | B | 6.09 | pIC50 | 813 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 233-235 [PMID:11755362] |
ChEMBL | Inhibition of human recombinant PDE4C | B | 6.09 | pIC50 | 813 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
ChEMBL | Inhibition of human recombinant PDE4C | B | 6.21 | pIC50 | 610 | nM | IC50 | J Med Chem (2007) 50: 344-349 [PMID:17228876] |
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
ChEMBL | Inhibition of human recombinant PDE4D3 using FAM-cAMP as substrate measured after 1 hr by IMAP TR-FRET assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
ChEMBL | Inhibition of PDE4D (unknown origin) using cAMP as substrate | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2019) 62: 5579-5593 [PMID:31099559] |
ChEMBL | Inhibitory activity against Phosphodiesterase 4D (PDE4D) from human source expressed in Saccharomyces cerevisiae | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
ChEMBL | Inhibition of human recombinant PDE4D | B | 7.2 | pIC50 | 63 | nM | IC50 | J Med Chem (2021) 64: 1786-1815 [PMID:33569941] |
ChEMBL | Inhibition of human Phosphodiesterase 4D from peripheral blood mononuclear cells | B | 7.2 | pIC50 | 63 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 233-235 [PMID:11755362] |
ChEMBL | Inhibition of human recombinant PDE4D | B | 7.41 | pIC50 | 39 | nM | IC50 | J Med Chem (2007) 50: 344-349 [PMID:17228876] |
ChEMBL | Inhibition of human PDE4D3 incubated for 10 mins using cAMP and [3H]cAMP substrates | B | 7.57 | pIC50 | 27 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3174-3176 [PMID:19447034] |
ChEMBL | Inhibition of PDE4D (unknown origin) | B | 7.89 | pIC50 | 13 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
ChEMBL | Inhibition of human PDE4D | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577] |
ChEMBL | Inhibition of human PDE4D catalytic domain using [3H]-cAMP or [3H]-cGMP incubated for 30 mins by scintillation counting method | B | 7.96 | pIC50 | 11 | nM | IC50 | EP-2674161-A1. FMO3 inhibitors for treating pain (2013) |
ChEMBL | Inhibition of human His-tagged PDE4D catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method | B | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
ChEMBL | Inhibition of human Phosphodiesterase 5 from peripheral blood mononuclear cells | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 233-235 [PMID:11755362] |
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]