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

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ChEMBL ligand: CHEMBL511115 (SB 207499, Cilomilast, SB-207499)
  • 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 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 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 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 PDE4B B 7.6 pIC50 25 nM IC50 Bioorg. Med. Chem. (2010) 18: 2204-2218 [PMID:20188577]
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 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]
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 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 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 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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]