rolipram [Ligand Id: 5260] 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: CHEMBL63 (NSC-760125, Rolipram, (r,s)-rolipram, SB-95952, ZK 62 711, ZK-62711, ZK-62771) |
|---|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
|---|---|---|---|---|---|---|---|---|
| A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
| ChEMBL | Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1990) 33: 2240-2254 [PMID:2374150] |
| Class 1 phosphodiesterase PDEB1 in Trypanosoma brucei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010636] [UniProtKB: Q8WQX9] | ||||||||
| ChEMBL | Inhibition of Trypanosoma brucei recombinant TbrPDEB1 expressed in Sf21 insect cells assessed as reduction of [3H]-cAMP hydrolysis by scintillation proximity assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2012) 55: 8745-8756 [PMID:22963052] |
| epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913] | ||||||||
| ChEMBL | Inhibition of recombinant human sEH using MNPC as substrate by fluorescence-based assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2018) 61: 3541-3550 [PMID:29614224] |
| phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
| ChEMBL | Inhibition of PDE10 | B | 4.8 | pIC50 | >16000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| phosphodiesterase 11A/Phosphodiesterase 11A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9] | ||||||||
| ChEMBL | Inhibition of PDE11 | B | 4.8 | pIC50 | >16000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| phosphodiesterase 1A/Phosphodiesterase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750] | ||||||||
| ChEMBL | Inhibition of PDE1A | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1297-1303 [PMID:18243697] |
| phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 2 (PDE2) from porcine platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| ChEMBL | Inhibition of guinea pig cardiac ventricle Phosphodiesterase 2 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1088-1099 [PMID:10090791] |
| ChEMBL | Inhibition of PDE2 | B | 4.8 | pIC50 | >16000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of Phosphodiesterase 2 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1829-1833 [PMID:15780616] |
| 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 in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3061] [UniProtKB: Q9XSW7] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 3 (PDE3) from porcine platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815] | ||||||||
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4AL (PDE4AL) in baculovirus expression system | B | 5.1 | pKi | 7940 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged PDE4A4 (2 to 886 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay | B | 5.71 | pIC50 | 1950 | nM | IC50 | Eur J Med Chem (2018) 145: 673-690 [PMID:29353721] |
| ChEMBL | Inhibitory activity against Phosphodiesterase 4A (PDE4A) from human source expressed in Saccharomyces cerevisiae | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
| ChEMBL | Inhibition of phosphodiesterase (PDE) 4A | B | 5.9 | pIC50 | 5.9 | nM | Log IC50 | Bioorg Med Chem Lett (1998) 8: 3229-3234 [PMID:9873708] |
| ChEMBL | Inhibition of full-length PDE4A4 using cAMP as substrate by two-step radiochemical assay | B | 6.08 | pIC50 | 830 | nM | IC50 | J Med Chem (2011) 54: 3331-3347 [PMID:21456625] |
| ChEMBL | Inhibition of full length human PDE4A4 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay | B | 6.41 | pIC50 | 386 | nM | IC50 | Eur J Med Chem (2016) 124: 372-379 [PMID:27597413] |
| ChEMBL | Inhibition of PDE4A4 expressed in yeast | B | 6.62 | pIC50 | 241 | nM | IC50 | J Med Chem (2010) 53: 6912-6922 [PMID:20825218] |
| ChEMBL | Inhibition of human recombinant PDE4A | B | 6.79 | pIC50 | 162 | nM | IC50 | J Med Chem (2012) 55: 7525-7545 [PMID:22891752] |
| ChEMBL | Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells | B | 7.02 | pIC50 | 95 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 4308-4314 [PMID:23806553] |
| ChEMBL | Inhibition of PDE4A | B | 7.08 | pIC50 | 84 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1297-1303 [PMID:18243697] |
| ChEMBL | Inhibition of PDE4A (unknown origin) | B | 7.17 | pIC50 | 67 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
| ChEMBL | Inhibition of PDE4A | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase type 4A (PDE4A). | B | 7.97 | pIC50 | 10.7 | nM | IC50 | J Med Chem (1998) 41: 266-270 [PMID:9464356] |
| ChEMBL | Inhibition of recombinant human PDE4A expressed in Sf9 cells | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2000) 43: 3820-3823 [PMID:11052785] |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268] |
| ChEMBL | Inhibition of PDE4A4 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay | B | 5.58 | pEC50 | 2620 | nM | EC50 | Medchemcomm (2012) 3: 667-672 |
| ChEMBL | Induction of SQSTM1-dependent intracellular redistribution of GFP-tagged PDE4A4 assessed as maximal accretion of enzyme into foci | B | 6.3 | pEC50 | 500 | nM | EC50 | J Med Chem (2011) 54: 3331-3347 [PMID:21456625] |
| Phosphodiesterase 4A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3333] [UniProtKB: O77823] | ||||||||
| ChEMBL | Inhibition of phosphodiesterase 4 (PDE4) from porcine liver | B | 5.44 | pIC50 | 3630 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] | ||||||||
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4BL (PDE4BL) in baculovirus expression system | B | 5.83 | pKi | 1470 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| ChEMBL | Inhibition of cAMP hydrolysis by the human phosphodiesterase 4B enzyme | B | 6.65 | pKi | 223.87 | nM | Ki | J Med Chem (1995) 38: 1505-1510 [PMID:7739009] |
| ChEMBL | Inhibition of human Phosphodiesterase 4B | B | 6.66 | pKi | 221 | nM | Ki | J Med Chem (1995) 38: 4848-4854 [PMID:7490734] |
| ChEMBL | Ability to inhibit the catalytic activity of human Phosphodiesterase 4B (PDE IVB) | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 1977-1982 |
| ChEMBL | Binding affinity to human recombinant full length PDE4B | B | 8.3 | pKi | 5 | nM | Ki | Eur J Med Chem (2021) 212: 113123-113123 [PMID:33412421] |
| ChEMBL | Inhibition of PDE4B in human PBMC assessed as reduction in LPS-induced TNFalpha release preincubated for 30 mins followed by LPS stimulation and measured after 18 hrs by TR-FRET assay | B | 4.72 | pIC50 | 18900 | nM | IC50 | Eur J Med Chem (2020) 207: 112795-112795 [PMID:33002845] |
| ChEMBL | Inhibition of PDE4B | B | 4.8 | pIC50 | 16000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1297-1303 [PMID:18243697] |
| ChEMBL | Inhibition of PDE4B in human PBMC assessed as inhibition in LPS-induced TNFalpha production preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET analysis | B | 4.94 | pIC50 | 11370 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126720-126720 [PMID:31610942] |
| ChEMBL | Inhibition of human PDE4B2 | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Nat Prod (2013) 76: 382-387 [PMID:23301853] |
| ChEMBL | Inhibition of human U-937 cells derived PDE4B using [3H] cAMP as substrate measured after 30 mins | B | 5.7 | pIC50 | 2000 | nM | IC50 | Eur J Med Chem (2020) 207: 112795-112795 [PMID:33002845] |
| ChEMBL | Inhibition of PDE4B | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 2032-2037 [PMID:18304812] |
| ChEMBL | Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 mins | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3271-3275 [PMID:30131242] |
| ChEMBL | Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate measured after 30 mins | B | 5.72 | pIC50 | 1900 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3276-3280 [PMID:30131240] |
| ChEMBL | Inhibition of PDE4B in human U937 cells using [3H] cAMP as substrate incubated for 30 mins | B | 5.74 | pIC50 | 1820 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126720-126720 [PMID:31610942] |
| ChEMBL | Inhibition of human U937 cells-derived PDE4B using [3H]cAMP as substrate after 30 mins | B | 5.74 | pIC50 | 1800 | nM | IC50 | Bioorg Med Chem (2017) 25: 1852-1859 [PMID:28196708] |
| ChEMBL | Inhibition of PDE4B derived from human monocytes using [3H]-cAMP as substrate after 30 mins | B | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3632-3635 [PMID:27289320] |
| ChEMBL | Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4610-4614 [PMID:26320621] |
| ChEMBL | Inhibition of recombinant full length human N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay | B | 5.9 | pIC50 | 1270 | nM | IC50 | Eur J Med Chem (2018) 145: 673-690 [PMID:29353721] |
| ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay | B | 5.9 | pIC50 | 1270 | nM | IC50 | Eur J Med Chem (2018) 145: 673-690 [PMID:29353721] |
| ChEMBL | Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 mins | B | 5.91 | pIC50 | 1220 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1188-1193 [PMID:29545101] |
| ChEMBL | Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP incubated for 30 mins | B | 5.91 | pIC50 | 1220 | nM | IC50 | Bioorg Med Chem (2017) 25: 5709-5717 [PMID:28888661] |
| ChEMBL | Inhibition of human recombinant PDE4B using cAMP as substrate incubated for 20 mins measured by Kinase Glo reagent based microplate reader assay | B | 5.95 | pIC50 | 1120 | nM | IC50 | Eur J Med Chem (2021) 209: 112854-112854 [PMID:33022582] |
| ChEMBL | Inhibition of recombinant human PDE4B using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Eur J Med Chem (2018) 158: 517-533 [PMID:30245393] |
| ChEMBL | Inhibition of human GST-tagged PDE4B expressed in baculovirus infected Sf9 insect cells using cAMP as substrate after 10 mins by PDE-Glo Phosphodiesterase Assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Eur J Med Chem (2018) 146: 381-394 [PMID:29407965] |
| ChEMBL | Inhibition of PDE4B (unknown origin) using [3H]cAMP as substrate incubated for 1 hr by PDElight HTS cAMP phosphodiesterase assay | B | 5.98 | pIC50 | 1040 | nM | IC50 | Eur J Med Chem (2022) 238: 114497-114497 [PMID:35660249] |
| ChEMBL | Inhibition of recombinant human PDE4B expressed in baculovirus infected Sf9 cells using [3H] cAMP as substrate after 30 min by scintillation proximity assay | B | 5.99 | pIC50 | 1030 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127112-127112 [PMID:32209292] |
| ChEMBL | Inhibition of recombinant His-tagged PDE4B (unknown origin) expressed in Sf9 cells using cAMP as substrate incubated for 15 mins prior to substrate addition measured after 1 hr by luminescence-based assay | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2013) 62: 395-404 [PMID:23380174] |
| ChEMBL | Inhibition of PDE4B1 (unknown origin) expressed in sf9 cells using cAMP as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay | B | 6.03 | pIC50 | 941 | nM | IC50 | Bioorg Med Chem (2013) 21: 1952-1963 [PMID:23415088] |
| ChEMBL | Inhibition of recombinant His-tagged human PDE4B expressed in Sf9 cells using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry | B | 6.03 | pIC50 | 940 | nM | IC50 | Eur J Med Chem (2019) 174: 198-215 [PMID:31035240] |
| ChEMBL | Inhibition of His-tagged recombinant human PDE4B1 expressed in baculovirus infected sf9 cells using cAMP as substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by luminescence assay | B | 6.03 | pIC50 | 940 | nM | IC50 | Medchemcomm (2012) 3: 667-672 |
| ChEMBL | Inhibition of PDE4B (unknown origin) using [3H]cAMP as substrate incubated for 30 mins by scintillation proximity assay | B | 6.03 | pIC50 | 940 | nM | IC50 | Eur J Med Chem (2021) 221: 113514-113514 [PMID:33992926] |
| ChEMBL | Inhibition of PDE4B1 | B | 6.05 | pIC50 | 901 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3686-3692 [PMID:19464886] |
| ChEMBL | Inhibitory activity against recombinant phosphodiesterase 4B (PDE4B) of human mononuclear lymphocytes | B | 6.13 | pIC50 | 741 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 653-658 [PMID:11844693] |
| ChEMBL | Inhibition of release of TNF alpha in human whole blood | F | 6.2 | pIC50 | 625 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of human PDE4B catalytic domain (152 to 528 residues) | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| 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 | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| ChEMBL | Inhibition of PDE4B2 | B | 6.27 | pIC50 | 534 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3686-3692 [PMID:19464886] |
| ChEMBL | Inhibition of PDE4B1 expressed in yeast | B | 6.3 | pIC50 | 498 | nM | IC50 | J Med Chem (2010) 53: 6912-6922 [PMID:20825218] |
| ChEMBL | Inhibition of recombinant human PDE4B using 5'-cGMP as substrate measured after 90 mins by colorimetric assay | B | 6.49 | pIC50 | 320 | nM | IC50 | Eur J Med Chem (2021) 212: 113125-113125 [PMID:33422981] |
| ChEMBL | Inhibition of human recombinant PDE4B | B | 6.64 | pIC50 | 231 | nM | IC50 | J Med Chem (2012) 55: 7525-7545 [PMID:22891752] |
| ChEMBL | Inhibition of PDE4B (unknown origin) | B | 6.66 | pIC50 | 220 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
| ChEMBL | Inhibition of human PDE4B2 in particular fraction of lung | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate incubated for 1 hr by fluorescence polarization assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2019) 168: 221-231 [PMID:30822711] |
| ChEMBL | Inhibition of recombinant human C-terminal His-tagged N-terminal GST-tagged PDE4B2 expressed in baculovirus infected Sf9 cells by radioligand binding assay | B | 6.96 | pIC50 | 110 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1848-1854 [PMID:33062163] |
| ChEMBL | Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis | B | 6.98 | pIC50 | 105 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1530-1533 [PMID:18222088] |
| ChEMBL | Inhibition of human PDE4B3 in particular fraction of lung | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human recombinant PDE4B2 assessed after 60 mins by IMAP fluorescence polarization assay | B | 7.01 | pIC50 | 97.9 | nM | IC50 | J Med Chem (2014) 57: 8590-8607 [PMID:25264825] |
| ChEMBL | Inhibition of human full-length PDE4B1 using AM-Cyclic-3',5'-AMP after 60 mins by fluorescence polarization assay | B | 7.07 | pIC50 | 86 | nM | IC50 | Bioorg Med Chem (2015) 23: 7332-7339 [PMID:26526739] |
| ChEMBL | Inhibition of full length human PDE4B1 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay | B | 7.07 | pIC50 | 86 | nM | IC50 | Eur J Med Chem (2016) 124: 372-379 [PMID:27597413] |
| ChEMBL | Inhibition of human PDE4B1 in cytosolic fraction of lung | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human recombinant PDE4B1 activity assessed as residual cAMP concentration by HTRF assay | B | 7.28 | pIC50 | 52 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4594-4597 [PMID:25149511] |
| ChEMBL | Inhibition of human PDE4B1 in particular fraction of lung | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human PDE4B3 in cytosolic fraction of lung | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of recombinant human Phosphodiesterase 4B | B | 7.45 | pIC50 | 35.7 | nM | IC50 | J Med Chem (1998) 41: 266-270 [PMID:9464356] |
| ChEMBL | Inhibition of PDE4B | B | 7.47 | pIC50 | 34 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of human PDE4B2 in cytosolic fraction of lung | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| GtoPdb | - | - | 9 | pIC50 | 1 | nM | IC50 | Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268] |
| ChEMBL | Inhibition of PDE4B expressed in HEK293 cells assessed as fold reduction in forskolin-stimulated cAMP production pretreated for 30 mins measured 4 hrs after forskolin challenge by luciferase reporter gene assay | F | 6.66 | pEC50 | 220 | nM | EC50 | Bioorg Med Chem (2012) 20: 2199-2207 [PMID:22386978] |
| ChEMBL | Inhibition of PDE4B1 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay | B | 6.8 | pEC50 | 160 | nM | EC50 | Medchemcomm (2012) 3: 667-672 |
| phosphodiesterase 4B/Phosphodiesterase 4B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3382] [GtoPdb: 1301] [UniProtKB: P14646] | ||||||||
| ChEMBL | Inhibitory activity against Phosphodiesterase 4B (PDE4B) from rat source expressed in Saccharomyces cerevisiae | B | 5.57 | pIC50 | 2700 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
| ChEMBL | Inhibition of phosphodiesterase (PDE) 4B | B | 5.7 | pIC50 | 5.7 | nM | Log IC50 | Bioorg Med Chem Lett (1998) 8: 3229-3234 [PMID:9873708] |
| phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493] | ||||||||
| ChEMBL | Inhibition of PDE4 CAT (unknown origin) at 1 uM relative to control | B | 4.23 | pIC50 | 59000 | nM | IC50 | Eur J Med Chem (2021) 224: 113700-113700 [PMID:34311158] |
| ChEMBL | Inhibitory activity against Phosphodiesterase 4C (PDE4C) from human source expressed in Saccharomyces cerevisiae | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
| ChEMBL | Inhibition of human recombinant PDE4C | B | 5.43 | pIC50 | 3690 | nM | IC50 | J Med Chem (2012) 55: 7525-7545 [PMID:22891752] |
| ChEMBL | Inhibition of PDE4C | B | 5.47 | pIC50 | 3410 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Evaluated in vitro for its inhibitory activity on unpurified recombinant Phosphodiesterase 4C | B | 5.58 | pIC50 | 2630 | nM | IC50 | J Med Chem (1998) 41: 266-270 [PMID:9464356] |
| ChEMBL | Inhibition of recombinant human full length N-terminal GST-tagged PDE4C1 expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by LANCE TR-FRET assay | B | 5.77 | pIC50 | 1680 | nM | IC50 | Eur J Med Chem (2018) 145: 673-690 [PMID:29353721] |
| ChEMBL | Inhibition of PDE4C (unknown origin) | B | 5.9 | pIC50 | 1258 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
| ChEMBL | Inhibition of PDE4 CAT (unknown origin) | B | 6.19 | pIC50 | 640 | nM | IC50 | Eur J Med Chem (2021) 224: 113700-113700 [PMID:34311158] |
| GtoPdb | - | - | 6.5 | pIC50 | 316 | nM | IC50 | Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268] |
| ChEMBL | Inhibition of full length human PDE4C1 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay | B | 6.93 | pIC50 | 118 | nM | IC50 | Eur J Med Chem (2016) 124: 372-379 [PMID:27597413] |
| phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4DE (PDE4DE) in baculovirus expression system | B | 5.07 | pKi | 8460 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| ChEMBL | Inhibition of human recombinant PDE4D2 expressed in baculovirus system by radiometric assay | B | 6.03 | pKi | 930 | nM | Ki | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of human recombinant PDE4D1 expressed in baculovirus system by radiometric assay | B | 6.31 | pKi | 490 | nM | Ki | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4D3 (PDE4D3) in baculovirus expression system | B | 6.42 | pKi | 382 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| ChEMBL | Inhibition of [3H]cAMP binding to recombinant human Phosphodiesterase 4D5 (PDE4D5) in baculovirus expression system | B | 6.43 | pKi | 375 | nM | Ki | J Med Chem (2005) 48: 1237-1243 [PMID:15715490] |
| ChEMBL | Inhibition of human recombinant PDE4D3 expressed in baculovirus system by radiometric assay | B | 6.52 | pKi | 300 | nM | Ki | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of human recombinant PDE4D3 | B | 7.23 | pKi | 58.9 | nM | Ki | J Med Chem (2009) 52: 1530-1539 [PMID:19256502] |
| ChEMBL | Inhibition of C5a mediated human eosinophil chemotaxis | F | 4.77 | pIC50 | 17000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of Eotaxin mediated by human eosinophil chemotaxis | F | 4.89 | pIC50 | 13000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of LTB4 mediated human eosinophil chemotaxis | F | 5.19 | pIC50 | 6500 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of PAF mediated human eosinophil chemotaxis | F | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate after 30 mins | B | 5.55 | pIC50 | 2800 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3271-3275 [PMID:30131242] |
| ChEMBL | Inhibition of human U-937 cells derived PDE4D using [3H] cAMP as substrate measured after 30 mins | B | 5.55 | pIC50 | 2800 | nM | IC50 | Eur J Med Chem (2020) 207: 112795-112795 [PMID:33002845] |
| ChEMBL | Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate measured after 30 mins | B | 5.6 | pIC50 | 2500 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3276-3280 [PMID:30131240] |
| ChEMBL | Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate after 30 mins | B | 5.84 | pIC50 | 1430 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 1188-1193 [PMID:29545101] |
| ChEMBL | Inhibition of human recombinant PDE4D2 expressed in baculovirus system by radiometric assay | B | 5.93 | pIC50 | 1170 | nM | IC50 | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of human PDE4D2 | B | 6 | pIC50 | 1000 | nM | IC50 | J Nat Prod (2014) 77: 1928-1936 [PMID:25075977] |
| ChEMBL | Inhibition of human recombinant PDE4D1 expressed in baculovirus system by radiometric assay | B | 6.04 | pIC50 | 910 | nM | IC50 | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of human PDE4D2 using cAMP substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by luminescence assay | B | 6.06 | pIC50 | 880 | nM | IC50 | Medchemcomm (2012) 3: 667-672 |
| ChEMBL | Inhibition of recombinant human PDE4D2 catalytic domain (86 to 413 residues) expressed in Escherichia coli BL21 codonplus cells using [3H]cAMP as substrate preincubated for 15 mins followed by substrate addition by liquid scintillation counting method | B | 6.17 | pIC50 | 671 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 2150-2152 [PMID:31281020] |
| ChEMBL | Inhibition of human recombinant PDE4D | B | 6.21 | pIC50 | 622 | nM | IC50 | J Med Chem (2012) 55: 7525-7545 [PMID:22891752] |
| ChEMBL | Inhibition of human PDE4D2 (86 to 413 residues) catalytic domain using [3H]-cAMP as substrate after 15 mins by liquid scintillation counting method | B | 6.21 | pIC50 | 621 | nM | IC50 | Eur J Med Chem (2019) 163: 512-526 [PMID:30553143] |
| ChEMBL | Inhibition of human PDE4D2 catalytic domain (86 to 413 residues) expressed in Escherichia coli strain BL21 using [3H]cAMP as substrate after 15 mins by liquid scintillation counter analysis | B | 6.21 | pIC50 | 620 | nM | IC50 | Eur J Med Chem (2018) 144: 758-766 [PMID:29291443] |
| ChEMBL | Inhibition of human PDE4D using 3H-cAMP as substrate after 15 mins by liquid scintillation counting analysis | B | 6.21 | pIC50 | 610 | nM | IC50 | J Med Chem (2015) 58: 8616-8637 [PMID:26473791] |
| ChEMBL | Inhibition of human PDE4D2 catalytic domain (86 to 413 amino acids) expressed in Escherichia coli strain BL21 after 15 mins using [3H]-cAMP by liquid scintillation counting | B | 6.22 | pIC50 | 600 | nM | IC50 | J Nat Prod (2014) 77: 1928-1936 [PMID:25075977] |
| ChEMBL | Inhibition of PDE4D2 (unknown origin) | B | 6.23 | pIC50 | 590 | nM | IC50 | Eur J Med Chem (2022) 242: 114631-114631 [PMID:35985255] |
| ChEMBL | Inhibition of PDE4D2 (86-413) (unknown origin) expressed in Escherichia coli BL21 assessed as using [3H]-cAMP as substrate measured for 15 mins by liquid scintillation counting analysis | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2021) 64: 13736-13751 [PMID:34520193] |
| ChEMBL | Inhibition of human PDE4D5 in particular fraction of lung | B | 6.23 | pIC50 | 590 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of recombinant PDE4D2 (86 to 413 residues) (unknown origin) expressed in Escherichia coli BL21 using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation method | B | 6.23 | pIC50 | 590 | nM | IC50 | Eur J Med Chem (2022) 242: 114631-114631 [PMID:35985255] |
| ChEMBL | Inhibition of human PDE4D2 catalytic domain (86 to 413aa) expressed in Escherichia coli strain BL21 after 15 mins by liquid scintillation counting in presence of [3H]-cAMP | B | 6.23 | pIC50 | 590 | nM | IC50 | J Nat Prod (2014) 77: 955-962 [PMID:24597921] |
| ChEMBL | Inhibition of human His-tagged PDE4D 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 | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| ChEMBL | Inhibition of full length human PDE4D2 expressed in Escherichia coli BL21 by liquid scintillation counting | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2008) 51: 7673-7688 [PMID:19049349] |
| ChEMBL | Inhibition of human recombinant PDE4D3 expressed in baculovirus system by radiometric assay | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of human PDE4D | B | 6.26 | pIC50 | 550 | nM | IC50 | Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577] |
| ChEMBL | Inhibition of human PDE4D2 catalytic domain (79 to 438 residues) Escherichia coli BL21-CodonPlus(DE3) cells | B | 6.26 | pIC50 | 550 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
| ChEMBL | Inhibition of full length human PDE4D2 expressed in Escherichia coli BL21 by liquid scintillation counting | B | 6.26 | pIC50 | 549.54 | nM | IC50 | J Med Chem (2008) 51: 7673-7688 [PMID:19049349] |
| ChEMBL | Inhibition of human PDE4D2 (86 to 413 residues) expressed in Escherichia coli BL21 codon-plus cells using [3H]cAMP as substrate incubated for 15 mins by liquid scintillation counting method | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2020) 63: 3370-3380 [PMID:32115956] |
| ChEMBL | Inhibition of human PDE4D2 catalytic domain (86 to 413 residues) expressed in Escherichia coli strain BL21 using [3H]cAMP as substrate after 15 mins by liquid scintillation counter analysis | B | 6.3 | pIC50 | 500 | nM | IC50 | J Nat Prod (2019) 82: 1820-1830 [PMID:31244143] |
| ChEMBL | Inhibition of PDE4D2 | B | 6.39 | pIC50 | 403 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3686-3692 [PMID:19464886] |
| ChEMBL | Inhibition of human recombinant PDE4D3 expressed in baculovirus system by IMAP assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of phosphodiesterase (PDE) 4D | B | 6.4 | pIC50 | 6.4 | nM | Log IC50 | Bioorg Med Chem Lett (1998) 8: 3229-3234 [PMID:9873708] |
| ChEMBL | Inhibitory activity against Phosphodiesterase 4D (PDE4D) from human source expressed in Saccharomyces cerevisiae | B | 6.41 | pIC50 | 390 | nM | IC50 | J Med Chem (2000) 43: 675-682 [PMID:10691693] |
| ChEMBL | Inhibition of human PDE4D3 in particular fraction of lung | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of PDE4D (unknown origin) using cAMP as substrate | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2019) 62: 5579-5593 [PMID:31099559] |
| ChEMBL | Inhibition of PDE4D2 (unknown origin) by preincubated for 30 mins before substrate addition and measured after 60 mins by IMAP TR-FRET phosphodiesterase evaluation assay | B | 6.7 | pIC50 | 200 | nM | IC50 | J Nat Prod (2019) 82: 1820-1830 [PMID:31244143] |
| ChEMBL | Inhibition of full length human PDE4D7 using FAM-3',5'-cAMP as substrate after 1 hr by fluorescence polarization assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Eur J Med Chem (2016) 124: 372-379 [PMID:27597413] |
| ChEMBL | Inhibition of human full-length PDE4D7 using AM-Cyclic-3',5'-AMP after 60 mins by fluorescence polarization assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Bioorg Med Chem (2015) 23: 7332-7339 [PMID:26526739] |
| ChEMBL | Inhibition of human PDE4D3 in cytosolic fraction of lung | B | 6.85 | pIC50 | 140 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human recombinant PDE4D2 activity assessed as residual cAMP concentration by HTRF assay | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4594-4597 [PMID:25149511] |
| ChEMBL | Inhibition of PDE4D7 (unknown origin) | B | 6.89 | pIC50 | 130 | nM | IC50 | Eur J Med Chem (2022) 238: 114503-114503 [PMID:35689855] |
| ChEMBL | Inhibition of recombinant human N-terminal GST-tagged PDE4D3 expressed in baculovirus infected Sf9 cells by radioligand binding assay | B | 6.96 | pIC50 | 110 | nM | IC50 | ACS Med Chem Lett (2020) 11: 1848-1854 [PMID:33062163] |
| ChEMBL | Inhibition of human recombinant PDE4D expressed in Sf9 cells | B | 7.04 | pIC50 | 92 | nM | IC50 | J Med Chem (2009) 52: 6546-6557 [PMID:19827751] |
| ChEMBL | Inhibition of recombinant human PDE4D3 expressed in baculoviral system | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2014) 57: 7061-7072 [PMID:25126889] |
| ChEMBL | Inhibition of human recombinant PDE4D3 assessed after 60 mins by IMAP fluorescence polarization assay | B | 7.08 | pIC50 | 82.5 | nM | IC50 | J Med Chem (2014) 57: 8590-8607 [PMID:25264825] |
| ChEMBL | Inhibition of PDE4D | B | 7.09 | pIC50 | 82 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1297-1303 [PMID:18243697] |
| ChEMBL | Inhibition of human PDE4D5 in cytosolic fraction of lung | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of PDE4D (unknown origin) | B | 7.1 | pIC50 | 79 | nM | IC50 | Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478] |
| ChEMBL | Inhibition of PDE4D3 expressed in yeast | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2010) 53: 6912-6922 [PMID:20825218] |
| GtoPdb | - | - | 7.2 | pIC50 | 63.1 | nM | IC50 | Biochem Biophys Res Commun (1997) 234: 320-4 [PMID:9177268] |
| ChEMBL | Inhibition of human PDE4D4 in cytosolic fraction of lung | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human PDE4D1 in cytosolic fraction of lung | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human PDE4D4 in particular fraction of lung | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of human PDE4D2 in cytosolic fraction of lung | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2008) 51: 5471-5489 [PMID:18686943] |
| ChEMBL | Inhibition of release of LTE4 in human whole blood | F | 7.39 | pIC50 | 41 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of PDE4D | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | In vitro inhibitory activity on unpurified recombinant Phosphodiesterase 4D | B | 7.5 | pIC50 | 31.6 | nM | IC50 | J Med Chem (1998) 41: 266-270 [PMID:9464356] |
| ChEMBL | cAMP elevation in U937 cells | F | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibition of PDE4D3 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay | B | 6.17 | pEC50 | 670 | nM | EC50 | Medchemcomm (2012) 3: 667-672 |
| phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
| ChEMBL | 50% inhibitory concentration against phosphodiesterase 5 (PDE5) from porcine platelets | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2000) 43: 2523-2529 [PMID:10891111] |
| ChEMBL | Inhibition of Phosphodiesterase 5 of guinea pig lung | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1999) 42: 1088-1099 [PMID:10090791] |
| ChEMBL | Inhibition of PDE5 | B | 4.8 | pIC50 | >16000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| ChEMBL | Inhibitory concentration against phosphodiesterase 5 (PDE5) from human platelet | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 2955-2958 [PMID:15125967] |
| ChEMBL | Inhibitory activity against cGMP-phosphodiesterase from porcine aorta | B | 6.14 | pIC50 | 720 | nM | IC50 | J Med Chem (1994) 37: 2106-2111 [PMID:8027992] |
| Phosphodiesterase 5A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3478] [UniProtKB: Q28156] | ||||||||
| ChEMBL | Inhibition of bovine arterial Phosphodiesterase 5 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1996) 39: 297-303 [PMID:8568820] |
| ChEMBL | Inhibition of bovine platelet PDE5 | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3983-3987 [PMID:22607677] |
| phosphodiesterase 8A/Phosphodiesterase 8A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658] | ||||||||
| ChEMBL | Inhibition of PDE8A | B | 4.8 | pIC50 | >16000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| phosphodiesterase 8B/Phosphodiesterase 8B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4408] [GtoPdb: 1308] [UniProtKB: O95263] | ||||||||
| ChEMBL | Inhibition of PDE8B | B | 4.8 | pIC50 | >16000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| phosphodiesterase 9A/Phosphodiesterase 9A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083] | ||||||||
| ChEMBL | Inhibition of PDE9 | B | 4.8 | pIC50 | >16000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 718-721 [PMID:16263279] |
| TNF-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1825] [UniProtKB: P01375] | ||||||||
| ChEMBL | TNF-alpha production in PBMC by ELISA method | F | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (1996) 39: 2-9 [PMID:8568809] |
| ChEMBL | Inhibition of LPS-induced TNF-alpha production in human PBMC preincubated for 30 mins followed by LPS addition measured after 5 hrs by ELISA | B | 6.3 | pIC50 | 500 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 24-30 [PMID:29173945] |
| ChEMBL | Inhibition of TNFalpha in LPS-stimulated human mononuclear cell line by radioimmunoassay | B | 6.3 | pIC50 | 500 | nM | IC50 | Eur J Med Chem (2021) 226: 113867-113867 [PMID:34607244] |
| ChEMBL | Inhibition of LPS-induced TNF-alpha production in human MNC suspension after 20 hrs by radioimmunoassay | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 24-30 [PMID:29173945] |
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]
