rolipram [Ligand Id: 5260] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL63 (Rolipram, SB-95952, ZK-62711, ZK-62771, ZK 62 711)
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • Class 1 phosphodiesterase PDEB1 in Trypanosoma brucei [ChEMBL: CHEMBL2010636] [UniProtKB: Q8WQX9]
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  • epoxide hydrolase 2/Epoxide hydratase in Human [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913]
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  • phosphodiesterase 10A/Phosphodiesterase 10A in Human [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233]
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  • phosphodiesterase 11A/Phosphodiesterase 11A in Human [ChEMBL: CHEMBL2717] [GtoPdb: 1311] [UniProtKB: Q9HCR9]
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  • phosphodiesterase 1A/Phosphodiesterase 1A in Human [ChEMBL: CHEMBL3421] [GtoPdb: 1294] [UniProtKB: P54750]
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  • phosphodiesterase 2A/Phosphodiesterase 2A in Human [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408]
  • phosphodiesterase 2A/Phosphodiesterase 2A in Rat [ChEMBL: CHEMBL4650] [GtoPdb: 1297] [UniProtKB: Q01062]
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  • phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
  • Phosphodiesterase 4A in Pig [ChEMBL: CHEMBL3333] [UniProtKB: O77823]
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  • phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
  • phosphodiesterase 4B/Phosphodiesterase 4B in Rat [ChEMBL: CHEMBL3382] [GtoPdb: 1301] [UniProtKB: P14646]
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  • phosphodiesterase 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
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  • phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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  • phosphodiesterase 5A/Phosphodiesterase 5A in Human [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074]
  • Phosphodiesterase 5A in Bovine [ChEMBL: CHEMBL3478] [UniProtKB: Q28156]
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  • phosphodiesterase 8A/Phosphodiesterase 8A in Human [ChEMBL: CHEMBL4640] [GtoPdb: 1307] [UniProtKB: O60658]
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  • phosphodiesterase 8B/Phosphodiesterase 8B in Human [ChEMBL: CHEMBL4408] [GtoPdb: 1308] [UniProtKB: O95263]
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  • phosphodiesterase 9A/Phosphodiesterase 9A in Human [ChEMBL: CHEMBL3535] [GtoPdb: 1309] [UniProtKB: O76083]
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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 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 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 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 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 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 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 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 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 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 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 human recombinant PDE4B B 6.64 pIC50 231 nM IC50 J. Med. Chem. (2012) 55: 7525-7545 [PMID:22891752]
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 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 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 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 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 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]
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 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. (20