Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL32442 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 [3H]-R-rolipram binding to recombinant human PDE-4 isoenzyme | - | 8.01 | pKi | 9.7 | nM | Ki | Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241] |
ChEMBL | Inhibition of recombinant human PDE4A expressed in Sf9 cells | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2000) 43: 3820-3823 [PMID:11052785] |
ChEMBL | Inhibitory concentration of compound against LPS- induced TNF-alpha production in whole human blood assay | F | 4.8 | pIC50 | 16000 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1457-1461 [PMID:12031319] |
ChEMBL | Inhibition of recombinant human PDE4A expressed in Sf9 cells | B | 5 | pIC50 | 10000 | nM | IC50 | J Med Chem (2000) 43: 3820-3823 [PMID:11052785] |
ChEMBL | In vitro inhibitory activity was determined against human Phosphodiesterase 4 isoform using a construct representing the common region of spliced variants expressed as a GST-fusion protein in Sf 9 cells | B | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (2003) 46: 2413-2426 [PMID:12773045] |
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 | 8.37 | pIC50 | 4.3 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1457-1461 [PMID:12031319] |
ChEMBL | Inhibition of GST-tagged PDE4A | B | 8.38 | pIC50 | 4.2 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
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 | 8.38 | pIC50 | 4.2 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 3009-3013 [PMID:12270195] |
ChEMBL | Inhibition of Phosphodiesterase-4A (PDE4) | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1923-1926 [PMID:12749899] |
ChEMBL | Inhibition of human recombinant phosphodiesterase 4A | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 1451-1456 [PMID:12031318] |
ChEMBL | Inhibitory activity against PDE4A | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5241-5246 [PMID:16168647] |
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
GtoPdb | Inhibition of [3H]-R-rolipram binding to recombinant human PDE4B2 isoenzyme | - | 8.07 | pKi | 8.5 | nM | Ki | Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241] |
ChEMBL | Inhibitory activity against PDE4B | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5241-5246 [PMID:16168647] |
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493] | ||||||||
GtoPdb | Inhibition of [3H]-R-rolipram binding to recombinant human PDE4C2 isoenzyme | - | 7.72 | pKi | 18.9 | nM | Ki | Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241] |
ChEMBL | Inhibitory activity against PDE4C | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5241-5246 [PMID:16168647] |
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
GtoPdb | Inhibition of [3H]-R-rolipram binding to recombinant human PDE4D3 isoenzyme | - | 8.15 | pKi | 7.1 | nM | Ki | Cell Biochem Biophys (1998) 29: 113-32 [PMID:9631241] |
ChEMBL | Inhibitory activity against PDE4D | B | 8.68 | pIC50 | 2.1 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 5241-5246 [PMID:16168647] |
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]