vardenafil [Ligand Id: 7320] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1520 (BAY-389456, BAY38-9456, Levitra, Vardenafil, Vivanza)
  • Kv4.3/A-type voltage-gated potassium channel KCND3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
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  • phosphodiesterase 10A/cAMP and cAMP-inhibited cGMP 3`,5`-cyclic phosphodiesterase 10A in Human [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
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  • phosphodiesterase 2A/cGMP-dependent 3`,5`-cyclic phosphodiesterase in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
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  • phosphodiesterase 5A/cGMP-specific 3`,5`-cyclic phosphodiesterase in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
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  • phosphodiesterase 11A/Dual 3`,5`-cyclic-AMP and -GMP phosphodiesterase 11A in Human [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
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  • phosphodiesterase 9A/High affinity cGMP-specific 3`,5`-cyclic phosphodiesterase 9A in Human [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
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  • Cav1.2/Voltage-dependent L-type calcium channel subunit alpha-1C in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
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  • Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv4.3/A-type voltage-gated potassium channel KCND3 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]
phosphodiesterase 10A/cAMP and cAMP-inhibited cGMP 3`,5`-cyclic 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 2A/cGMP-dependent 3`,5`-cyclic phosphodiesterase 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/cGMP-specific 3`,5`-cyclic phosphodiesterase 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 11A/Dual 3`,5`-cyclic-AMP and -GMP 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 9A/High affinity cGMP-specific 3`,5`-cyclic 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-dependent L-type calcium channel subunit alpha-1C 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]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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]

ChEMBL data shown on this page come from version 36:

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]