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: CHEMBL514800 (Apremilast, CC10004, CC-10004, Otezla) |
---|
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 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
ChEMBL | Inhibition of human PDE4B using [3H]cAMP as substrate incubated for 5 mins followed by substrate addition and measured after 10 mins by scintillation proximity assay | B | 7.13 | pIC50 | 74 | nM | IC50 | Bioorg Med Chem (2016) 24: 5702-5716 [PMID:27713015] |
ChEMBL | Inhibition of recombinant human PDE4B2 expressed in African green monkey COS7 cells using cAMP as substrate | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2018) 61: 2472-2489 [PMID:29502405] |
ChEMBL | Inhibition of PDE4B (unknown origin) | B | 7.57 | pIC50 | 27 | nM | IC50 | Eur J Med Chem (2019) 174: 198-215 [PMID:31035240] |
GtoPdb | Potency against recombinant human PDE4B1 and B2 isoforms in a TR-FRET assay. | - | 7.57 | pIC50 | 27 | nM | IC50 | Cell Signal (2014) 26: 2016-29 [PMID:24882690] |
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
ChEMBL | Inhibition of PDE4D2 (unknown origin) | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2020) 63: 3370-3380 [PMID:32115956] |
ChEMBL | Inhibition of PDE4D (unknown origin) using cAMP as substrate | B | 7.13 | pIC50 | 74 | nM | IC50 | J Med Chem (2019) 62: 5579-5593 [PMID:31099559] |
ChEMBL | Inhibition of human PDE4D catalytic domain (86 to 413 residues) expressed in Escherichia coli BL21 (DE3) cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay | B | 7.32 | pIC50 | 47.6 | nM | IC50 | J Nat Prod (2020) 83: 1229-1237 [PMID:32100544] |
GtoPdb | Potency against recombinant human PDE4D2 isoform in a TR-FRET assay. | - | 7.48 | pIC50 | 33 | nM | IC50 | Cell Signal (2014) 26: 2016-29 [PMID:24882690] |
ChEMBL | Inhibition of PDE4D (unknown origin) | B | 7.48 | pIC50 | 33 | nM | IC50 | Eur J Med Chem (2019) 174: 198-215 [PMID:31035240] |
phosphodiesterase 4A in Human [GtoPdb: 1300] [UniProtKB: P27815] | ||||||||
GtoPdb | Potency against recombinant human PDE4A1A isoform in a TR-FRET assay. | - | 7.85 | pIC50 | 14 | nM | IC50 | Cell Signal (2014) 26: 2016-29 [PMID:24882690] |
phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493] | ||||||||
GtoPdb | Potency against recombinant human PDE4C1 isoform in a TR-FRET assay. | - | 6.93 | pIC50 | 118 | nM | IC50 | Cell Signal (2014) 26: 2016-29 [PMID:24882690] |
ChEMBL data shown on this page come from version 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]