LEO 239652 [Ligand Id: 12725] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4747201 |
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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] | ||||||||
| ChEMBL | Inhibition of human PDE4A catalytic domain using cAMP and FAM-conjugated cAMP by IMAP FRET progressive binding assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2020) 63: 14502-14521 [PMID:33054196] |
| phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
| ChEMBL | Inhibition of human PDE4B catalytic domain using cAMP and FAM-conjugated cAMP by IMAP FRET progressive binding assay | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2020) 63: 14502-14521 [PMID:33054196] |
| phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493] | ||||||||
| ChEMBL | Inhibition of human PDE4C catalytic domain using cAMP and FAM-conjugated cAMP by IMAP FRET progressive binding assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2020) 63: 14502-14521 [PMID:33054196] |
| phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
| ChEMBL | Inhibition of PDE4D in human PBMC assessed as reduction in lipopolysaccharide-induced TNFalpha production pre-incubated for 30 mins before LPS stimulation for 18 hrs by AlphaLISA | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2020) 63: 14502-14521 [PMID:33054196] |
| GtoPdb | - | - | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2020) 63: 14502-14521 [PMID:33054196] |
| ChEMBL | Inhibition of human PDE4D catalytic domain using cAMP and FAM-conjugated cAMP by IMAP FRET progressive binding assay | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2020) 63: 14502-14521 [PMID:33054196] |
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]
