piclamilast [Ligand Id: 11627] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL42126 (Piclamilast, RP-73041, RP 73401, RP-73401, RP73401, RPR-73401)
  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
  • Phosphodiesterase 4A in Pig [ChEMBL: CHEMBL3333] [UniProtKB: O77823]
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  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
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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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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
GtoPdb Inhibition of rolipram binding to human PDE4 - 8.82 pKi 1.5 nM Ki J Med Chem (1994) 37: 1696-703 [PMID:8201604]
ChEMBL Inhibition of human recombinant PDE4A B 8.4 pIC50 4 nM IC50 J Med Chem (2007) 50: 344-349 [PMID:17228876]
ChEMBL Evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase type 4A (PDE4A). B 8.8 pIC50 1.6 nM IC50 J Med Chem (1998) 41: 266-270 [PMID:9464356]
Phosphodiesterase 4A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3333] [UniProtKB: O77823]
ChEMBL Inhibitory potency against pig aortic PDE IV B 9 pIC50 1 nM IC50 J Med Chem (1994) 37: 1696-1703 [PMID:8201604]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL Inhibition of human recombinant PDE4B B 8.52 pIC50 3 nM IC50 J Med Chem (2007) 50: 344-349 [PMID:17228876]
ChEMBL Inhibition of human His6-tagged PDE4B (152-487) expressed in Escherichia coli BL21 (DE3) after 1 hr B 8.7 pIC50 2 nM IC50 Bioorg Med Chem Lett (2010) 20: 2928-2932 [PMID:20378348]
ChEMBL Inhibition of recombinant human Phosphodiesterase 4B B 9 pIC50 1 nM IC50 J Med Chem (1998) 41: 266-270 [PMID:9464356]
ChEMBL Inhibitory activity against recombinant phosphodiesterase 4B (PDE4B) of human mononuclear lymphocytes B 9.7 pIC50 0.2 nM IC50 Bioorg Med Chem Lett (2002) 12: 653-658 [PMID:11844693]
ChEMBL Inhibition of human PDE4B B 10.39 pIC50 0.04 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 10.39 pIC50 0.04 nM IC50 J Med Chem (2016) 59: 7029-7065 [PMID:26908025]
ChEMBL Inhibition of human PDE4B by scintillation counting method B 10.39 pIC50 0.04 nM IC50 J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
ChEMBL Inhibition of human recombinant PDE4C B 7.85 pIC50 14 nM IC50 J Med Chem (2007) 50: 344-349 [PMID:17228876]
ChEMBL Evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase 4C B 8.42 pIC50 3.8 nM IC50 J Med Chem (1998) 41: 266-270 [PMID:9464356]
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
ChEMBL Inhibition of human recombinant PDE4D B 8.7 pIC50 2 nM IC50 J Med Chem (2007) 50: 344-349 [PMID:17228876]
ChEMBL In vitro inhibitory activity on unpurified recombinant Phosphodiesterase 4D B 9.1 pIC50 0.8 nM IC50 J Med Chem (1998) 41: 266-270 [PMID:9464356]
ChEMBL Inhibition of human PDE4D B 10.68 pIC50 0.02 nM IC50 Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577]
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 10.68 pIC50 0.02 nM IC50 J Med Chem (2016) 59: 7029-7065 [PMID:26908025]
ChEMBL Inhibition of human PDE4D by scintillation counting method B 10.68 pIC50 0.02 nM IC50 J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
ChEMBL Inhibition of human PDE4D catalytic domain using [3H]-cAMP or [3H]-cGMP incubated for 30 mins by scintillation counting method B 10.7 pIC50 0.02 nM IC50 EP-2674161-A1. FMO3 inhibitors for treating pain (null)

ChEMBL data shown on this page come from version 33:

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]