MK-0359 [Ligand Id: 9852] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL372575 (L-454560) |
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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 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]
