tadalafil [Ligand Id: 7299] 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: CHEMBL779 (Tadalafil, Cialis, IC351, LY450190, Adcirca, IC-351, LY-450190)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Rat [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
There should be some charts here, you may need to enable JavaScript!
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 1A/Phosphodiesterase 1A in Human [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
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 3B/Phosphodiesterase 3B in Human [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
  • Phosphodiesterase 3B in Bovine [ChEMBL: CHEMBL5129] [UniProtKB: E1BN64]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
  • Phosphodiesterase 5A in Bovine [ChEMBL: CHEMBL3478] [UniProtKB: Q28156]
  • phosphodiesterase 5A/Phosphodiesterase 5A in Rat [ChEMBL: CHEMBL4567] [GtoPdb: 1304] [UniProtKB: O54735]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 6C/Phosphodiesterase 6C in Human [ChEMBL: CHEMBL3977] [GtoPdb: 1314] [UniProtKB: P51160]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 7A/Phosphodiesterase 7A in Human [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
There should be some charts here, you may need to enable JavaScript!
  • phosphodiesterase 8A/Phosphodiesterase 8A in Human [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658]
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!
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
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3199] [GtoPdb: 2465] [UniProtKB: P37136]
ChEMBL Inhibition of AChE from rat cortex by Ellman's method B 4.58 pIC50 26159 nM IC50 Eur J Med Chem (2019) 176: 228-247 [PMID:31103902]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG channel in HEK293 cells by voltage-clamp method B 4 pIC50 100000 nM IC50 Eur. J. Med. Chem. (2008) 43: 2479-2488 [PMID:18262683]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay F 4 pIC50 100000 nM IC50 J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753]
ChEMBL Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG 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/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
ChEMBL Inhibitory concentration against human phosphodiesterase 10 B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2365-2369 [PMID:15837326]
ChEMBL Inhibition of PDE10 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay B 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2013) 60: 285-294 [PMID:23313637]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged PDE10A1 (2 to 789 residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
phosphodiesterase 11A/Phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
ChEMBL Inhibitory concentration against phosphodiesterase-11 B 4.22 pIC50 60000 nM IC50 J. Med. Chem. (2005) 48: 3449-3462 [PMID:15887951]
GtoPdb - - 6.52 pIC50 300 nM IC50 J Med Chem (2011) 54: 495-509 [PMID:21189023]
ChEMBL Inhibition of human recombinant PDE11A-mediated hydrolysis of cAMP after 30 mins by fluorescence polarization assay B 6.52 pIC50 300 nM IC50 J. Med. Chem. (2011) 54: 495-509 [PMID:21189023]
ChEMBL Inhibition of human recombinant PDE11 B 6.54 pIC50 290 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 6279-6282 [PMID:18976905]
ChEMBL Inhibition of human recombinant PDE11 B 6.54 pIC50 290 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 383-386 [PMID:19906530]
ChEMBL Inhibition of human recombinant PDE11A-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assay B 7.3 pIC50 50 nM IC50 J. Med. Chem. (2011) 54: 495-509 [PMID:21189023]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged PDE11A4 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 7.33 pIC50 47 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
ChEMBL Inhibitory activity against phosphodiesterase 11 (PDE11) obtained from recombinant Sf9 expression B 7.43 pIC50 37 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1425-1428 [PMID:12668004]
ChEMBL Inhibition of human phosphodiesterase 11 B 7.48 pIC50 33 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2365-2369 [PMID:15837326]
ChEMBL Inhibition of PDE11 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay B 8 pIC50 10 nM IC50 Eur. J. Med. Chem. (2013) 60: 285-294 [PMID:23313637]
phosphodiesterase 1A/Phosphodiesterase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged PDE1A expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
ChEMBL Inhibition of Human recombinant PDE2 (Phosphodiesterase 2) B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2003) 46: 4533-4542 [PMID:14521415]
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 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2013) 60: 285-294 [PMID:23313637]
ChEMBL Inhibition of recombinant human N-terminal FLAG-tagged PDE2A (2 to 941 residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
phosphodiesterase 3B/Phosphodiesterase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370]
ChEMBL Inhibition of human recombinant PDE3B-mediated hydrolysis of cAMP after 30 mins by fluorescence polarization assay B 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2011) 54: 495-509 [PMID:21189023]
ChEMBL Inhibition of human recombinant PDE3B-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assay B 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2011) 54: 495-509 [PMID:21189023]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged PDE3B (592 to end residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
Phosphodiesterase 3B in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5129] [UniProtKB: E1BN64]
ChEMBL Inhibition of bovine aorta PDE3 (Phosphodiesterase 3) B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2003) 46: 4533-4542 [PMID:14521415]
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged PDE4A1A expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL Inhibition of human recombinant PDE4B-mediated hydrolysis of cAMP after 30 mins by fluorescence polarization assay B 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2011) 54: 495-509 [PMID:21189023]
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
ChEMBL Inhibition of human phosphodiesterase 5 B 8 pKi 10 nM Ki J. Med. Chem. (2005) 48: 3449-3462 [PMID:15887951]
ChEMBL Inhibition of PDE5 (unknown origin) B 8.28 pKi 5.2 nM Ki Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
ChEMBL Inhibition of recombinant human PDE5A B 8.03 pIC50 9.4 nM IC50 J Med Chem (2016) 59: 8967-9004 [PMID:27606546]
ChEMBL Inhibition of PDE5A (unknown origin) B 8.03 pIC50 9.4 nM IC50 Eur J Med Chem (2018) 150: 506-524 [PMID:29549837]
ChEMBL Inhibitory activity against phosphodiesterase 5 (PDE5) obtained from human corpus cavernosum tissue B 8.17 pIC50 6.7 nM IC50 Bioorg. Med. Chem. Lett. (2003) 13: 1425-1428 [PMID:12668004]
ChEMBL Inhibition of PDE5 B 8.3 pIC50 5.01 nM IC50 Bioorg. Med. Chem. (2008) 16: 7599-7606 [PMID:18656371]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-GMP as substrate after 1 hr by fluorescence polarization assay B 8.33 pIC50 4.67 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
ChEMBL Inhibition of human recombinant PDE5 after 1.5 hrs by fluorescent polarization assay B 8.4 pIC50 4 nM IC50 Eur. J. Med. Chem. (2010) 45: 1278-1286 [PMID:20206015]
ChEMBL Inhibition of human phosphodiesterase 5 B 8.4 pIC50 4 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2365-2369 [PMID:15837326]
ChEMBL Inhibition of PDE5A1 (unknown origin) by immobilized metal ion affinity-based fluorescence polarization B 8.4 pIC50 4 nM IC50 Eur J Med Chem (2019) 176: 228-247 [PMID:31103902]
ChEMBL Inhibition of PDE5 (unknown origin) B 8.5 pIC50 3.16 nM IC50 J Med Chem (2018) 61: 6421-6467 [PMID:29620890]
GtoPdb - - 8.52 pIC50 3 nM IC50 J Med Chem (2011) 54: 495-509 [PMID:21189023]
ChEMBL Inhibition of human recombinant PDE5A-mediated hydrolysis of cGMP after 30 mins by fluorescence polarization assay B 8.52 pIC50 3 nM IC50 J. Med. Chem. (2011) 54: 495-509 [PMID:21189023]
ChEMBL Inhibition of N-terminal GST-tagged human PDE5A1 expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay B 8.63 pIC50 2.35 nM IC50 J Med Chem (2019) 62: 4979-4990 [PMID:31021628]
ChEMBL Inhibition of Phosphodiesterase 5 from human platelets B 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (2003) 46: 457-460 [PMID:12570368]
ChEMBL Inhibition of PDE5A (unknown origin) B 8.92 pIC50 1.2 nM IC50 J Med Chem (2018) 61: 5467-5483 [PMID:29363967]
ChEMBL Inhibition of PDE5 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay B 8.92 pIC50 1.2 nM IC50 Eur. J. Med. Chem. (2013) 60: 285-294 [PMID:23313637]
Phosphodiesterase 5A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3478] [UniProtKB: Q28156]
ChEMBL Inhibition of bovine PDE5 B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 6279-6282 [PMID:18976905]
ChEMBL Inhibition of bovine platelet PDE5 B 7.92 pIC50 12 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 383-386 [PMID:19906530]
ChEMBL In vitro inhibitory activity against bovine phosphodiesterase 5 B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2003) 46: 4533-4542 [PMID:14521415]
ChEMBL In vitro inhibitory activity against bovine phosphodiesterase 5 B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2003) 46: 4533-4542 [PMID:14521415]
ChEMBL Inhibition of bovine PDE5 after 24 hrs by time-resolved fluorescence resonance energy transfer assay B 8.3 pIC50 5 nM IC50 J. Med. Chem. (2012) 55: 1274-1286 [PMID:22204607]
ChEMBL Inhibition of bovine PDE5 after 24 hrs by HTRF B 8.48 pIC50 3.3 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 789-792 [PMID:17107795]
phosphodiesterase 5A/Phosphodiesterase 5A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4567] [GtoPdb: 1304] [UniProtKB: O54735]
ChEMBL Inhibition of phosphodiesterase 5 in rat fetal lung fibroblast (RFL-6) cells B 8.3 pKi 5 nM Ki J. Med. Chem. (2005) 48: 2126-2133 [PMID:15771456]
ChEMBL Inhibition of PDE5 in Wistar rat mesentric arteries assessed as inhibition of phenylephrine-induced contraction by measuring increase in acetylcholine-induced vasorelaxation by pressure myographic method B 7.11 pEC50 78 nM EC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
Phosphodiesterase 6A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3741] [UniProtKB: P11541]
ChEMBL Inhibition of bovine retina PDE6 B 5.52 pIC50 3000 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 383-386 [PMID:19906530]
phosphodiesterase 6C/Phosphodiesterase 6C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3977] [GtoPdb: 1314] [UniProtKB: P51160]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged PDE6C expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
phosphodiesterase 7A/Phosphodiesterase 7A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946]
ChEMBL Inhibition of recombinant human N-terminal GST-tagged PDE7A (122 to end residues) expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
phosphodiesterase 8A/Phosphodiesterase 8A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged PDE8A1 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
phosphodiesterase 9A/Phosphodiesterase 9A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
ChEMBL Inhibition of Phosphodiesterase 9 B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2005) 15: 2365-2369 [PMID:15837326]
ChEMBL Inhibition of PDE9 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay B 5 pIC50 >10000 nM IC50 Eur. J. Med. Chem. (2013) 60: 285-294 [PMID:23313637]
ChEMBL Inhibition of full length recombinant human N-terminal GST-tagged PDE9A2 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-AMP as substrate after 1 hr by fluorescence polarization assay B 5 pIC50 >10000 nM IC50 Eur J Med Chem (2018) 158: 767-780 [PMID:30245400]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against chloroquine-susceptible Plasmodium falciparum GHA strain infected in human erythrocytes after 72 hrs by spectrophotometry F 4.19 pIC50 >64000 nM IC50 J. Med. Chem. (2011) 54: 3222-3240 [PMID:21504142]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum GHA infected in human erythrocytes after 72 hrs using malstat staining by spectrophotometry F 4.19 pIC50 >64000 nM IC50 J. Med. Chem. (2012) 55: 1274-1286 [PMID:22204607]
ChEMBL DNDI: Malaria in Vitro, 72 hour F 4.89 pIC50 >12840 nM IC50 Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning

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, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]