cilomilast [Ligand Id: 7407] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL511115 (Ariflo, Cilomilast, SB 207499, SB-207499, SB207499)
  • Class 1 phosphodiesterase PDEB1 in Trypanosoma brucei [ChEMBL: CHEMBL2010636] [UniProtKB: Q8WQX9]
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  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
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  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
  • phosphodiesterase 4B/Phosphodiesterase 4B in Rat [ChEMBL: CHEMBL3382] [GtoPdb: 1301] [UniProtKB: P14646]
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  • phosphodiesterase 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
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  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]