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 (2013)

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]