[3H]rolipram [Ligand Id: 5313] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL63 (NSC-760125, Rolipram, (r,s)-rolipram, SB-95952, ZK 62 711, ZK-62711, ZK-62771) |
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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 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] |
| 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 | 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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 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] |
| 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] |
| 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 | |||||