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ChEMBL ligand: CHEMBL42126 (Piclamilast, RP-73041, RP 73401, RP-73401, RP73401, RPR-73401) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]