sildenafil [Ligand Id: 4743] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL192 (Aphrodil, HIP-0908, HIP0908, Nipatra, Patrex, Revatio, Sildenafil, Sildenafil actavis, Sildenafilo, Sildenafil ratiopharm, Sildenafil teva, UK-92480, Viagra, Vizarsin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 6.06 | pKi | 871 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) | B | 5.83 | pIC50 | 1493 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Displacement of [3H]ZM241385 from human AA2AR expressed in HEK293T cells after 2 hrs by liquid scintillation counter | B | 6.7 | pKi | 199.53 | nM | Ki | J Med Chem (2012) 55: 5311-5325 [PMID:22563707] |
| ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 6.85 | pKi | 142 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA) | B | 6.6 | pIC50 | 253 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.09 | pKi | 806 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.84 | pIC50 | 1457 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG in MCF7 cells | B | 4 | pIC50 | 100000 | nM | IC50 | Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341] |
| ChEMBL | K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 | F | 4 | pIC50 | 100000 | nM | IC50 | J Med Chem (2002) 45: 3844-3853 [PMID:12190308] |
| 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 | pIC50 | 100000 | 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 | Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique | B | 5.48 | pIC50 | 3311.31 | nM | IC50 | Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342] |
| ChEMBL | Inhibition of human ERG | B | 5.48 | pIC50 | 3311.31 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| ChEMBL | Inhibitory concentration against potassium channel HERG | B | 5.48 | pIC50 | 3311.31 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273] |
| ChEMBL | Inhibition of human Potassium channel HERG expressed in mammalian cells | B | 5.48 | pIC50 | 3311.31 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512] |
| ChEMBL | Inhibition of human ERG channel | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
| ChEMBL | Inhibition of human ERG channel | B | 5.48 | pIC50 | 3300 | nM | IC50 | J Med Chem (2009) 52: 4266-4276 [PMID:19534531] |
| indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075294] [GtoPdb: 2829] [UniProtKB: P28776] | ||||||||
| ChEMBL | Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7641-7646 [PMID:23122865] |
| indoleamine 2,3-dioxygenase 2/Indoleamine 2,3-dioxygenase 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189159] [GtoPdb: 3019] [UniProtKB: Q8R0V5] | ||||||||
| ChEMBL | Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis | B | 5.35 | pIC50 | 4500 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7641-7646 [PMID:23122865] |
| ABCC4/Multidrug resistance-associated protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743128] [GtoPdb: 782] [UniProtKB: O15439] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP4-expressing HEK293 cells | F | 4.7 | pIC50 | 20000 | nM | IC50 | Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538] |
| ABCC5/Multidrug resistance-associated protein 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2046258] [GtoPdb: 783] [UniProtKB: O15440] | ||||||||
| GtoPdb | - | - | 5.92 | pKi | 1200 | nM | Ki | J Med Chem (2012) 55: 3049-57 [PMID:22380603] |
| ChEMBL | Inhibition of ABCC5 in human erythrocytes assessed as inhibition of ATP-mediated [3H]cGMP uptake in inside-out vesicles after 60 mins by liquid scintillation counting | B | 5.92 | pKi | 1200 | nM | Ki | J Med Chem (2012) 55: 3049-3057 [PMID:22380603] |
| ChEMBL | TP_TRANSPORTER: inhibition of 9-(2-phosphonomethoxyethyl)adenine(PMEA) efflux (PMEA: 1 uM) in MRP5-expressing HEK293 cells | F | 4.1 | pIC50 | 80000 | nM | IC50 | Mol Pharmacol (2003) 63: 1094-1103 [PMID:12695538] |
| phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
| ChEMBL | Inhibition of human recombinant PDE10A2 at 1 uM by [3H]cGMP based tritium scintillation proximity assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 10540-10550 [PMID:23137303] |
| ChEMBL | Inhibition of PDE10 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay | B | 5.17 | pIC50 | 6800 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibition of PDE10A1 (unknown origin) using fluorescently labeled cAMP substrate by fluorescence polarization assay | B | 5.27 | pIC50 | 5400 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| ChEMBL | Inhibitory concentration against human phosphodiesterase 10 | B | 5.51 | pIC50 | 3100 | 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 GST-tagged recombinant human PDE11A4 | B | 5.11 | pIC50 | 7800 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| ChEMBL | Inhibition of PDE11 (unknown origin) using FAM-cGMP and FAM-cAMP as substrate after 60 mins by fluorescence assay | B | 5.21 | pIC50 | 6100 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibition of human recombinant PDE11A4 at 1 uM by [3H]cGMP based tritium scintillation proximity assay | B | 5.38 | pIC50 | 4210 | nM | IC50 | J Med Chem (2012) 55: 10540-10550 [PMID:23137303] |
| ChEMBL | Inhibition of human recombinant PDE11 | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6279-6282 [PMID:18976905] |
| ChEMBL | Inhibition of human recombinant PDE11 | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 383-386 [PMID:19906530] |
| ChEMBL | Inhibition of human phosphodiesterase 11 | B | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| phosphodiesterase 1A/Phosphodiesterase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750] | ||||||||
| ChEMBL | Inhibition of PDE1A1 (unknown origin) using fluorescently labeled cAMP substrate by fluorescence polarization assay | B | 6.22 | pIC50 | 600 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition of PDE2A1 (unknown origin) using fluorescently labeled cAMP substrate by fluorescence polarization assay | B | 4.2 | pIC50 | 63000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| 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 recombinant PDE2 (phosphodiesterase 2) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 4525-4532 [PMID:14521414] |
| ChEMBL | Inhibition of Phosphodiesterase 2 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1829-1833 [PMID:15780616] |
| 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] |
| Phosphodiesterase 2A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3477] [UniProtKB: P14099] | ||||||||
| ChEMBL | Inhibitory activity against phosphodiesterase-2 (PDE2) isolated from bovine adrenal gland | B | 4.37 | pIC50 | 43000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2341-2345 [PMID:12824030] |
| ChEMBL | Inhibition of bovine adrenal gland Phosphodiesterase 2 (PDE2) | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2001) 44: 2204-2218 [PMID:11405657] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4650] [GtoPdb: 1297] [UniProtKB: Q01062] | ||||||||
| ChEMBL | Inhibitory concentration against phosphodiesterase 2 from rat kidney | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2955-2958 [PMID:15125967] |
| phosphodiesterase 3A/Phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432] | ||||||||
| ChEMBL | Inhibition of PDE3A (unknown origin) using fluorescently labeled cAMP substrate by fluorescence polarization assay | B | 4.59 | pIC50 | 26000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| Phosphodiesterase 3B in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5129] [UniProtKB: E1BN64] | ||||||||
| ChEMBL | Inhibition of bovine aorta PDE3 (Phosphodiesterase 3) | B | 5.04 | pIC50 | 9200 | nM | IC50 | J Med Chem (2003) 46: 4533-4542 [PMID:14521415] |
| ChEMBL | Inhibition of bovine aorta PDE3 (phosphodiesterase 3) | B | 5.04 | pIC50 | 9200 | nM | IC50 | J Med Chem (2003) 46: 4525-4532 [PMID:14521414] |
| phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815] | ||||||||
| ChEMBL | Inhibition of PDE4A1 (unknown origin) using fluorescently labeled cAMP substrate by fluorescence polarization assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
| ChEMBL | Inhibition of human His-tagged PDE4B catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method | B | 4.7 | pIC50 | 20000 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
| ChEMBL | Inhibition of human PDE4D | B | 4.7 | pIC50 | 20000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577] |
| 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 | Inhibitory activity against Phosphodiesterase 5 (PDE5) was evaluated | B | 8.72 | pKi | 1.91 | nM | Ki | J Med Chem (2003) 46: 441-444 [PMID:12540243] |
| ChEMBL | Inhibitory activity against human Phosphodiesterase 5 | B | 8.72 | pKi | 1.91 | nM | Ki | J Med Chem (2004) 47: 656-662 [PMID:14736245] |
| ChEMBL | Phosphodiesterase 5 activity of human corpus cavernosum | B | 8.73 | pKi | 1.87 | nM | Ki | J Med Chem (2002) 45: 4094-4096 [PMID:12213052] |
| ChEMBL | Inhibitory activity against PDE5 from human corpus cavernosum | B | 8.73 | pKi | 1.87 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 761-765 [PMID:12639576] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 8.8 | pKi | 1.6 | nM | Ki | Eur J Med Chem (2018) 158: 767-780 [PMID:30245400] |
| ChEMBL | Inhibition of human PDE5A preincubated for 30 mins followed by TMB substrate addition by spectrophotometry | B | 4.9 | pIC50 | 12590 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4180-4184 [PMID:28751142] |
| ChEMBL | Inhibition of human recombinant PDE5A1 expressed in COS7 cells | B | 7.12 | pIC50 | 75 | nM | IC50 | J Nat Prod (2008) 71: 1513-1517 [PMID:18778098] |
| ChEMBL | Inhibition of PDE5 in human platelets after 5 mins by LC-MS/MS analysis | B | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2008) 51: 2807-2815 [PMID:18393409] |
| ChEMBL | Inhibition of PDE5 | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2006) 49: 5363-5371 [PMID:16913726] |
| ChEMBL | Inhibition of human Phosphodiesterase 5 (n=2-3) | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2381-2384 [PMID:15837329] |
| ChEMBL | Inhibitory concentration against phosphodiesterase 5 (PDE5) from human platelet | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2955-2958 [PMID:15125967] |
| ChEMBL | Inhibition of recombinant human PDE5A | B | 8.07 | pIC50 | 8.5 | nM | IC50 | J Med Chem (2016) 59: 8967-9004 [PMID:27606546] |
| ChEMBL | Inhibition of PDE5A (unknown origin) | B | 8.07 | pIC50 | 8.5 | nM | IC50 | Eur J Med Chem (2018) 150: 506-524 [PMID:29549837] |
| ChEMBL | Inhibition of PDE5 | B | 8.18 | pIC50 | 6.61 | nM | IC50 | Bioorg Med Chem (2008) 16: 7599-7606 [PMID:18656371] |
| ChEMBL | Inhibition of phosphodiesterase 5 | B | 8.18 | pIC50 | 6.6 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3900-3907 [PMID:15993055] |
| ChEMBL | Inhibition of Phosphodiesterase 5 | B | 8.18 | pIC50 | 6.6 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 865-868 [PMID:11958981] |
| ChEMBL | Inhibition of human PDE5A1 expressed in baculovirus in sf9 cells by PDE Glo phosphodiesterase assay | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| ChEMBL | Inhibition of PDE5A1 (unknown origin) | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 8.28 | pIC50 | 5.22 | nM | IC50 | RSC Med Chem (2022) 13: 1300-1321 [PMID:36439976] |
| ChEMBL | Inhibition of human PDE5A1 catalytic domain (535 to 860 residues) expressed in Escherichia coli BL21 using 3H-cGMP as substrate after 15 mins by liquid scintillation counting | B | 8.29 | pIC50 | 5.1 | nM | IC50 | J Med Chem (2018) 61: 8468-8473 [PMID:30148362] |
| ChEMBL | Inhibition of human PDE5A1 (535-860 residues) expressed in Escherichia coli BL21 incubated for 15 mins using [3H]-cGMP as substrate by liquid scintillation counting method | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2020) 63: 9828-9837 [PMID:32794708] |
| ChEMBL | Inhibition of human PDE5A1 catalytic domain (Glu535 to Gln860 residues) expressed in Escherichia coli BL21 using [3H]-cGMP as substrate preincubated for 15 mins followed by snake venom 5'-nucleotidase and further incubated for 10 mins by scintillation counting method | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (2021) 64: 4462-4477 [PMID:33793216] |
| ChEMBL | Inhibition of PDE-5A (unknown origin) | B | 8.33 | pIC50 | 4.66 | nM | IC50 | Eur J Med Chem (2020) 186: 111852-111852 [PMID:31759729] |
| ChEMBL | DRUGMATRIX: Phosphodiesterase PDE5 enzyme inhibition (substrate: [3H]cGMP + cGMP) | B | 8.34 | pIC50 | 4.58 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 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 | 8.37 | pIC50 | 4.31 | nM | IC50 | J Med Chem (2019) 62: 4979-4990 [PMID:31021628] |
| ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in baculovirus infected Sf9 cells using cGMP as substrate after 30 mins by HTRF assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2016) 59: 8967-9004 [PMID:27606546] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 8.4 | pIC50 | 3.98 | nM | IC50 | J Med Chem (2018) 61: 6421-6467 [PMID:29620890] |
| ChEMBL | Inhibition of human recombinant PDE5A by [3H]cGMP based tritium scintillation proximity assay | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (2012) 55: 10540-10550 [PMID:23137303] |
| ChEMBL | Inhibition of N-terminal GST-tagged full length recombinant human PDE5A1 catalytic domain expressed in Baculovirus infected Sf9 insect cells using FAM-cGMP as substrate after 1 hr by fluorescence polarization assay | B | 8.44 | pIC50 | 3.65 | nM | IC50 | Eur J Med Chem (2018) 150: 30-38 [PMID:29505934] |
| ChEMBL | Inhibition of PDE5 | B | 8.44 | pIC50 | 3.63 | nM | IC50 | Bioorg Med Chem (2008) 16: 7599-7606 [PMID:18656371] |
| ChEMBL | Inhibition of human corpus cavernosum PDE5 | B | 8.44 | pIC50 | 3.6 | nM | IC50 | J Med Chem (2020) 63: 15153-15186 [PMID:33314936] |
| ChEMBL | Inhibition of Phosphodiesterase 5 from rabbit platelets | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1819-1824 |
| ChEMBL | Inhibition of PDE5 | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3125-3128 [PMID:20400309] |
| ChEMBL | Inhibitory concentration against human phosphodiesterase 5 (PDE5) enzyme | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1291-1294 [PMID:14980684] |
| ChEMBL | Inhibition of human phosphodiesterase 5 | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| ChEMBL | Inhibition of human corpus cavernosum PDE5 | B | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2006) 49: 3581-3594 [PMID:16759100] |
| ChEMBL | Inhibition of human corpus cavernosum PDE5 by scintillation proximity assay | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6033-6036 [PMID:18951784] |
| ChEMBL | Concentration required to inhibit phosphodiesterase type 5 (PDE5) isolated from corpus cavernosum by 50% was determined | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 3149-3152 [PMID:12372521] |
| ChEMBL | Inhibition of phosphodiesterase 5 isolated from human platelets | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2790-2794 [PMID:15878277] |
| ChEMBL | Inhibition of Phosphodiesterase 5 from human corpus cavernosum | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1819-1824 |
| ChEMBL | Inhibition of human full length His-tagged PDE5A1 expressed in baculovirus infected Sf9 insect cells using [3H]-cGMP as substrate preincubated for 15 mins followed by snake venom 5'-nucleotidase and further incubated for 10 mins by scintillation counting method | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 4462-4477 [PMID:33793216] |
| ChEMBL | Inhibition of recombinant full length GST-tagged PDE5A1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using TAMRA-cGMP as substrate incubated for 1.5 hrs by IMAP-FP assay | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2021) 64: 4462-4477 [PMID:33793216] |
| ChEMBL | Inhibition of human His-tagged PDE5A catalytic domain expressed in Escherichia coli BL21-CodonPlus(DE3) cells using [3H]cAMP or [3H]cGMP as substrate incubated for 30 mins by scintillation counting method | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| ChEMBL | Inhibition of recombinant human full length PDE5A1 catalytic domain expressed in Escherichia coli BL21 using [3H]cGMP as substrate after 15 mins by liquid scintillation counting | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2018) 61: 5467-5483 [PMID:29363967] |
| ChEMBL | Inhibition of recombinant human PDE5A1 catalytic domain (535 to 860 residues) expressed in baculovirus infected sf9 cells using [3H]cGMP as substrate incubated for 15 mins by liquid scintillation counting method | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| ChEMBL | Inhibition of PDE5 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibition of human PDE5A | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| ChEMBL | Inhibition of phosphodiesterase 5 of rabbit platelets | B | 8.75 | pIC50 | 1.78 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2099-2103 [PMID:15080987] |
| ChEMBL | Inhibition of PDE5 from human platelets | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2461-2464 [PMID:11549447] |
| ChEMBL | Inhibition of phosphodiesterase type 5 (PDE5) of human platelets | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2000) 43: 1257-1263 [PMID:10753463] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5175-5180 [PMID:25442307] |
| ChEMBL | In vitro inhibitory concentration against human platelet Phosphodiesterase 5 was determined | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2000) 43: 5037-5043 [PMID:11150175] |
| ChEMBL | Inhibition of phosphodiesterase 5 from human platelets | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1577-1580 [PMID:15006407] |
| ChEMBL | Inhibition of Phosphodiesterase 5 from human platelets | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2003) 46: 457-460 [PMID:12570368] |
| ChEMBL | Inhibition of PDE5 of human platelets | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2001) 44: 1025-1027 [PMID:11297448] |
| ChEMBL | Inhibition of human PDE5 using [3H]cGMP as substrate incubated for 10 mins by liquid scintillation counter analysis | B | 8.85 | pIC50 | 1.4 | nM | IC50 | Bioorg Med Chem (2022) 76: 117092-117092 [PMID:36450167] |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 |
Mol Pharmacol (1999) 56: 124-30 [PMID:10385692]; J Med Chem (2012) 55: 10540-50 [PMID:23137303] |
| ChEMBL | Inhibition of human platelets PDE5 | B | 9 | pIC50 | 1 | nM | IC50 | Eur J Med Chem (2019) 177: 269-290 [PMID:31158744] |
| ChEMBL | Inhibition of PDE5 in human platelets incubated for 30 mins using cGMP as substrate by HPLC analysis relative to sildenafil | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 127337-127337 [PMID:32631538] |
| ChEMBL | Relaxant effect on rabbit corpus cavernosal tissue strips | F | 7.38 | pEC50 | 42 | nM | EC50 | J Med Chem (2001) 44: 1025-1027 [PMID:11297448] |
| ChEMBL | Relaxant effect on isolated rabbit corpus cavernosum | F | 8.06 | pEC50 | 8.7 | nM | EC50 | J Med Chem (2001) 44: 2204-2218 [PMID:11405657] |
| Phosphodiesterase 5A in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304402] [UniProtKB: O77746] | ||||||||
| ChEMBL | Inhibitory activity against canine lung Phosphodiesterase 5 (PDE5) | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (2001) 44: 2204-2218 [PMID:11405657] |
| ChEMBL | Inhibitory activity against phosphodiesterase 5 (PDE5) isolated from canine lung | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2341-2345 [PMID:12824030] |
| Phosphodiesterase 5A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3478] [UniProtKB: Q28156] | ||||||||
| ChEMBL | Inhibition of bovine aortic smooth muscle PDE5 using cGMP as substrate incubated for 30 mins in presence of EGTA and [3H]cGMP by liquid scintillation counting method | B | 5.48 | pIC50 | 3300 | nM | IC50 | Eur J Med Chem (2019) 177: 269-290 [PMID:31158744] |
| ChEMBL | Inhibition of bovine PDE5 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6279-6282 [PMID:18976905] |
| ChEMBL | Inhibition of bovine platelet PDE5 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 383-386 [PMID:19906530] |
| ChEMBL | Inhibition of bovine platelet PDE5 | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3983-3987 [PMID:22607677] |
| ChEMBL | Inhibition of bovine aorta PDE5 (Phosphodiesterase 5) | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2003) 46: 4533-4542 [PMID:14521415] |
| ChEMBL | Inhibitory activity against bovine PDE5 (phosphodiesterase-5). | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2003) 46: 4525-4532 [PMID:14521414] |
| 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 | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2005) 48: 2126-2133 [PMID:15771456] |
| ChEMBL | Inhibition of rat lung PDE5 using [3H]cGMP as substrate measured after 10 mins by scintillation counting method | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 267-270 [PMID:30509781] |
| ChEMBL | Inhibition of Phosphodiesterase 5 from rat diaphragm | B | 9.52 | pIC50 | 0.3 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 2313-2316 [PMID:12161123] |
| Phosphodiesterase 6A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3741] [UniProtKB: P11541] | ||||||||
| ChEMBL | Inhibition of bovine retina PDE6 | B | 6.85 | pIC50 | 140 | 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 human PDE6C | B | 6.8 | pIC50 | 160 | nM | IC50 | J Nat Prod (2008) 71: 1513-1517 [PMID:18778098] |
| ChEMBL | Inhibition of human recombinant PDE6C at 1 uM by [3H]cGMP based tritium scintillation proximity assay | B | 7.41 | pIC50 | 39.2 | nM | IC50 | J Med Chem (2012) 55: 10540-10550 [PMID:23137303] |
| GtoPdb | - | - | 7.41 | pIC50 | 39.2 | nM | IC50 | J Med Chem (2012) 55: 10540-50 [PMID:23137303] |
| ChEMBL | Inhibition of PDE6C (unknown origin) | B | 7.62 | pIC50 | 24 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| Phosphodiesterase 6C in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3479] [UniProtKB: P16586] | ||||||||
| ChEMBL | Inhibition of bovine cone PDE6 | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2006) 49: 3581-3594 [PMID:16759100] |
| phosphodiesterase 7A/Phosphodiesterase 7A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3012] [GtoPdb: 1305] [UniProtKB: Q13946] | ||||||||
| ChEMBL | Inhibition of GST-tagged recombinant human PDE7A1 | B | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| ChEMBL | Inhibition of human recombinant PDE7A1 at 1 uM by [3H]cGMP based tritium scintillation proximity assay | B | 5.33 | pIC50 | 4690 | nM | IC50 | J Med Chem (2012) 55: 10540-10550 [PMID:23137303] |
| phosphodiesterase 8A/Phosphodiesterase 8A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658] | ||||||||
| ChEMBL | Inhibition of GST-tagged recombinant human PDE8A1 | B | 4 | pIC50 | 100000 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| ChEMBL | Inhibition of human recombinant PDE8A1 at 1 uM by [3H]cGMP based tritium scintillation proximity assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 10540-10550 [PMID:23137303] |
| phosphodiesterase 9A/Phosphodiesterase 9A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083] | ||||||||
| ChEMBL | Inhibition of human recombinant PDE9A2 at 1 uM by [3H]cGMP based tritium scintillation proximity assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 10540-10550 [PMID:23137303] |
| ChEMBL | Inhibition of PDE9 (unknown origin) using FAM-cGMP as substrate after 60 mins by fluorescence assay | B | 5.25 | pIC50 | 5600 | nM | IC50 | Eur J Med Chem (2013) 60: 285-294 [PMID:23313637] |
| ChEMBL | Inhibition of GST-tagged recombinant human PDE9A2 | B | 5.44 | pIC50 | 3600 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| ChEMBL | Inhibition of Phosphodiesterase 9 | B | 5.47 | pIC50 | 3400 | 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 | pIC50 | 100000 | nM | IC50 | J Pharmacol Toxicol Methods (2014) 70: 246-254 [PMID:25087753] |
| OATP1B3 in Human [GtoPdb: 1221] [UniProtKB: Q9NPD5] | ||||||||
| GtoPdb | - | - | 6.1 | pIC50 | 800 | nM | IC50 | Drug Metab Dispos (2007) 35: 1400-7 [PMID:17496208] |
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]
