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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1520 (Vardenafil, Levitra, BAY-389456, BAY38-9456)
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 10A/Phosphodiesterase 10A in Human [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 11A/Phosphodiesterase 11A in Human [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 9A/Phosphodiesterase 9A in Human [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
There should be some charts here, you may need to enable JavaScript!
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
There should be some charts here, you may need to enable JavaScript!
  • Kv4.3/Voltage-gated potassium channel subunit Kv4.3 in Human [ChEMBL: CHEMBL1964] [GtoPdb: 554] [UniProtKB: Q9UK17]
There should be some charts here, you may need to enable JavaScript!
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 PDE5A (unknown origin) B 9.05 pIC50 0.89 nM IC50 Eur J Med Chem (2018) 150: 506-524 [PMID:29549837]
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 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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]