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, 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 PDE5A (unknown origin) | B | 8.07 | pIC50 | 8.5 | nM | IC50 | Eur J Med Chem (2018) 150: 506-524 [PMID:29549837] |
| 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 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 (2002) 12: 865-868 [PMID:11958981] |
| 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 PDE5A1 (unknown origin) | B | 8.25 | pIC50 | 5.6 | nM | IC50 | Bioorg Med Chem (2015) 23: 2121-2128 [PMID:25801159] |
| 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 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 | 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 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 | Inhibition of human phosphodiesterase 5 | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 2365-2369 [PMID:15837326] |
| 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 | 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 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 | 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 Phosphodiesterase 5 from human corpus cavernosum | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 1819-1824 |
| 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 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 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 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 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 human PDE5A | B | 8.66 | pIC50 | 2.2 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| 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 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 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 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 PDE5 of human platelets | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2001) 44: 1025-1027 [PMID:11297448] |
| 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 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 from human platelets | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2461-2464 [PMID:11549447] |
| ChEMBL | Inhibition of PDE5 (unknown origin) | B | 8.8 | pIC50 | 1.6 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5175-5180 [PMID:25442307] |
| 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 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]
