vardenafil [Ligand Id: 7320] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1520 (BAY-389456, BAY38-9456, Levitra, Vardenafil, Vivanza) |
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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 | Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform | F | 4.1 | pIC50 | 79432.82 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| ChEMBL | Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay | F | 4.5 | pIC50 | 31622.78 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
| ChEMBL | Inhibition of PDE10 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay | B | 6.06 | pIC50 | 880 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibitory concentration against human phosphodiesterase 10 | B | 6.1 | pIC50 | 790 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| phosphodiesterase 11A/Phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9] | ||||||||
| ChEMBL | Inhibition of PDE11 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay | B | 6.62 | pIC50 | 240 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibition of human phosphodiesterase 11 | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition of human phosphodiesterase 2 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| ChEMBL | Inhibition of PDE2 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay | B | 5.51 | pIC50 | 3100 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
| ChEMBL | Inhibition of human phosphodiesterase 5 | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2005) 48: 3449-3462 [PMID:15887951] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 9.15 | pKi | 0.7 | nM | Ki | Eur J Med Chem (2018) 158: 767-780 [PMID:30245400] |
| ChEMBL | Inhibition of PDE5 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibition of recombinant human PDE5A | B | 9.05 | pIC50 | 0.89 | nM | IC50 | J Med Chem (2016) 59: 8967-9004 [PMID:27606546] |
| ChEMBL | Inhibition of PDE5A (unknown origin) | B | 9.05 | pIC50 | 0.89 | nM | IC50 | Eur J Med Chem (2018) 150: 506-524 [PMID:29549837] |
| ChEMBL | Inhibition of PDE5 | B | 9.15 | pIC50 | 0.71 | nM | IC50 | Bioorg Med Chem (2008) 16: 7599-7606 [PMID:18656371] |
| ChEMBL | Inhibition of Phosphodiesterase 5 from human platelets | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2003) 46: 457-460 [PMID:12570368] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2018) 61: 6421-6467 [PMID:29620890] |
| ChEMBL | Inhibition of human phosphodiesterase 5 | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| GtoPdb | - | - | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-9 [PMID:15837326] |
| ChEMBL | Inhibition of PDE5A1 (unknwon origin) using [3H]cGMP as substrate after 30 mins by SPA | B | 9.77 | pIC50 | 0.17 | nM | IC50 | J Med Chem (2018) 61: 1001-1018 [PMID:29293004] |
| ChEMBL | Inhibition of human platelets derived PDE5 using [3H]-cGMP as substrate incubated for 60 min by scintillation proximity assay | B | 10.54 | pIC50 | 0.03 | nM | IC50 | J Med Chem (2020) 63: 14243-14275 [PMID:32870008] |
| phosphodiesterase 9A/Phosphodiesterase 9A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083] | ||||||||
| ChEMBL | Inhibition of PDE9 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay | B | 6.17 | pIC50 | 680 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibition of Phosphodiesterase 9 | B | 6.34 | pIC50 | 460 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform | F | 4.8 | pIC50 | 15848.93 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17] | ||||||||
| ChEMBL | Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform | F | 4.1 | pIC50 | 79432.82 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
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]
