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 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]
