tadalafil [Ligand Id: 7299] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL779 (Adcirca, Cialis, IC-351, IC351, LY-450190, LY450190, NSC-750236, NSC-759172, Tadalafil, Tadalafil mylan, Tadliq, Trans-tadalafil) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| acetylcholinesterase (Yt 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] |
| TLX/Nuclear receptor subfamily 2 group E member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1961788] [GtoPdb: 615] [UniProtKB: Q9Y466] | ||||||||
| ChEMBL | Agonist activity at in human TLX LBD expressed in human HEK293T cells coexpressing Gal4-VP 16 assessed as increase in reporter activity measured after 14 hrs by luciferase reporter gene assay relative to control | B | 5.3 | pEC50 | 5000 | nM | EC50 | J Med Chem (2021) 64: 8727-8738 [PMID:34115934] |
| 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 PDE5A (unknown origin) | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127097-127097 [PMID:32171616] |
| 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] |
| ChEMBL | Inhibition of PDE5A in HEK293 cells stably transfected with cGMP biosensor assessed as increase in SNP-induced intracellular cGMP level measured after 90 mins by luminescence assay | B | 5.24 | pEC50 | 5810 | nM | EC50 | J Med Chem (2021) 64: 4462-4477 [PMID:33793216] |
| 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 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]
