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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
