MK-0359 [Ligand Id: 9852] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL372575 (L-454560)
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  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
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  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
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  • phosphodiesterase 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
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  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of [35S]MK-499 from human ERG expressed in HEK293 cells B 4.3 pIC50 49900 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5554-5558 [PMID:18835163]
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
GtoPdb - - 8.8 pIC50 1.6 nM IC50 Biochem Pharmacol (2007) 73: 1971-81 [PMID:17428447]
ChEMBL Inhibitory activity against PDE4A B 8.85 pIC50 1.4 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]
ChEMBL Intrinsic inhibition of GST-fused human PDE4A expressed in SF9 cells B 8.85 pIC50 1.4 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5554-5558 [PMID:18835163]
ChEMBL Inhibition of human PDE4A B 8.85 pIC50 1.4 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 5502-5505 [PMID:20709547]
ChEMBL Inhibition of PDE4A B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6387-6393 [PMID:20933411]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL Inhibition of PDE4B B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6387-6393 [PMID:20933411]
GtoPdb - - 9.3 pIC50 0.5 nM IC50 Biochem Pharmacol (2007) 73: 1971-81 [PMID:17428447]
ChEMBL Inhibitory activity against PDE4B B 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]
ChEMBL Inhibition of human PDE4B B 9.3 pIC50 0.5 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 5502-5505 [PMID:20709547]
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
GtoPdb - - 8.04 pIC50 9.1 nM IC50 Biochem Pharmacol (2007) 73: 1971-81 [PMID:17428447]
ChEMBL Inhibitory activity against PDE4C B 8.04 pIC50 9.1 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]
ChEMBL Inhibition of human PDE4C B 8.04 pIC50 9.1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 5502-5505 [PMID:20709547]
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
GtoPdb - - 8.92 pIC50 1.2 nM IC50 Biochem Pharmacol (2007) 73: 1971-81 [PMID:17428447]
ChEMBL Inhibitory activity against PDE4D B 8.92 pIC50 1.2 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 5241-5246 [PMID:16168647]
ChEMBL Inhibition of human PDE4D B 8.92 pIC50 1.2 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 5502-5505 [PMID:20709547]
ChEMBL Inhibition of PDE4D B 9 pIC50 1 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 6387-6393 [PMID:20933411]

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]