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ChEMBL ligand: CHEMBL511115 (Ariflo, Cilomilast, SB 207499, SB-207499) |
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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 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 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 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 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 | 6.21 | 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 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 (null) |
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 32:
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]