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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 (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]