ChEMBL ligand: CHEMBL193240 (Arq-151, B-9302-107, B9302-107, BY-217, BY217, BYK-20869, BYK20869, Daliresp, Daxas, Roflumilast, Zoryve)
Class 1 phosphodiesterase PDEB1 in Trypanosoma brucei [ChEMBL: CHEMBL2010636] [UniProtKB: Q8WQX9] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 3A/Phosphodiesterase 3A in Human [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4A/Phosphodiesterase 4A in Human [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4B/Phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4C/Phosphodiesterase 4C in Human [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4D/Phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] 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
Class 1 phosphodiesterase PDEB1 in Trypanosoma brucei (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010636] [UniProtKB: Q8WQX9]
ChEMBL	Inhibition of full length Trypanosoma brucei PDEB1 expressed in Sf21 insect cells using cAMP as substrate by scintillation proximity assay	B	5.5	pKi	3162.28	nM	Ki	J Med Chem (2018) 61: 3870-3888 [PMID:29672041]
phosphodiesterase 3A/Phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432]
ChEMBL	Inhibition of core catalytic domains PDE3A (unknown origin)	B	4	pIC50	>100000	nM	IC50	Bioorg Med Chem Lett (2013) 23: 5311-5316 [PMID:23988356]
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815]
ChEMBL	Inhibition of human recombinant PDE4A	B	9.15	pIC50	0.7	nM	IC50	J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
ChEMBL	Inhibition of human PDE4A4 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assay	B	9.23	pIC50	0.59	nM	IC50	Eur J Med Chem (2011) 46: 4946-4956 [PMID:21871695]
ChEMBL	Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells	B	9.46	pIC50	0.35	nM	IC50	Bioorg Med Chem Lett (2013) 23: 4308-4314 [PMID:23806553]
ChEMBL	Inhibition of human recombinant PDE4A using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 15 mins by SPA bead based scintillation counting analysis	B	9.68	pIC50	0.21	nM	IC50	Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478]
phosphodiesterase 4B/Phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
ChEMBL	Inhibition of human PDE4B2 catalytic domain and UCR2 (92 to 521) expressed in Escherichia coli BL21 using [3H]-cAMP/[3H]-cGMP after 15 mins by liquid scintillation counting	B	6.17	pIC50	670	nM	IC50	Bioorg Med Chem Lett (2012) 22: 3261-3264 [PMID:22483586]
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	7.08	pIC50	84	nM	IC50	J Med Chem (2016) 59: 7029-7065 [PMID:26908025]
ChEMBL	Inhibition of PDE4B (unknown origin)	B	8.89	pIC50	1.3	nM	IC50	Eur J Med Chem (2019) 174: 198-215 [PMID:31035240]
ChEMBL	Inhibition of core catalytic domains PDE4B (unknown origin)	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem Lett (2013) 23: 5311-5316 [PMID:23988356]
ChEMBL	Inhibition of human recombinant PDE4B2 assessed as inhibition of cAMP hydrolysis by colorimetric assay	B	9	pIC50	1	nM	IC50	Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734]
ChEMBL	Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assay	B	9	pIC50	1	nM	IC50	Bioorg Med Chem Lett (2012) 22: 1523-1526 [PMID:22297114]
ChEMBL	Inhibition of human PDE4B by ELISA	B	9.05	pIC50	0.9	nM	IC50	Eur J Med Chem (2018) 148: 477-486 [PMID:29477888]
ChEMBL	Inhibition of human U937 cells-derived PDE4B using [3H]-cAMP as substrate after 30 mins	B	9.05	pIC50	0.89	nM	IC50	Bioorg Med Chem Lett (2018) 28: 1188-1193 [PMID:29545101]
ChEMBL	Inhibition of human PDE4B by scintillation counting method	B	9.08	pIC50	0.84	nM	IC50	J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
ChEMBL	Inhibition of human PDE4B	B	9.08	pIC50	0.84	nM	IC50	Bioorg Med Chem (2010) 18: 2204-2218 [PMID:20188577]
ChEMBL	Inhibition of human recombinant PDE4B by liquid scintillation counter method	B	9.08	pIC50	0.84	nM	IC50	Eur J Med Chem (2021) 226: 113877-113877 [PMID:34624823]
ChEMBL	Inhibition of the human PDE4B catalytic domain after 30 mins in presence of [3H]cAMP/[3H]cGMP by scintillation counting	B	9.08	pIC50	0.84	nM	IC50	J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
ChEMBL	Inhibition of human recombinant PDE4B2 assessed as decrease in cAMP hydrolysis preincubated with substrate prior to enzyme addition measured after 30 mins by colorimetric assay method	B	9.1	pIC50	0.8	nM	IC50	Bioorg Med Chem Lett (2013) 23: 1548-1552 [PMID:23375225]
ChEMBL	Inhibition of human PDE4B2	B	9.1	pIC50	0.8	nM	IC50	Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734]
ChEMBL	Inhibition of human recombinant PDE4B	B	9.15	pIC50	0.7	nM	IC50	J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
ChEMBL	Inhibition of recombinant human PDE4B1 using [3H]-cAMP as substrate preincubated for 15 mins followed substrate addition measured after 60 mins by scintillation proximity assay	B	9.15	pIC50	0.7	nM	IC50	J Med Chem (2018) 61: 2472-2489 [PMID:29502405]
ChEMBL	Inhibition of recombinant human PDE4B1 expressed in African green monkey COS7 cells using cAMP as substrate	B	9.15	pIC50	0.7	nM	IC50	J Med Chem (2018) 61: 2472-2489 [PMID:29502405]
ChEMBL	Inhibition of human PDE4B1 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assay	B	9.16	pIC50	0.69	nM	IC50	Eur J Med Chem (2011) 46: 4946-4956 [PMID:21871695]
ChEMBL	Inhibition of human recombinant PDE4B1 assessed as reduction in [3H]cAMP hydrolysis to [3H]AMP incubated for 60 mins by PDE-SPA assay	B	9.16	pIC50	0.69	nM	IC50	J Med Chem (2016) 59: 10479-10497 [PMID:27933955]
ChEMBL	Inhibition of recombinant human PDE4B using cAMP as substrate after 30 mins	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem (2013) 21: 7025-7037 [PMID:24094436]
ChEMBL	Inhibition of human recombinant PDE4B (152 to 564 amino acids) using cAMP as substrate after 30 mins by plate reader analysis	B	9.31	pIC50	0.49	nM	IC50	Bioorg Med Chem Lett (2013) 23: 3325-3328 [PMID:23602400]
ChEMBL	Inhibition of human recombinant PDE4B1 activity assessed as residual cAMP concentration by HTRF assay	B	9.4	pIC50	0.4	nM	IC50	Bioorg Med Chem Lett (2014) 24: 4594-4597 [PMID:25149511]
GtoPdb	-	-	9.4	pIC50	-	-	-	Bioorg Med Chem Lett (2009) 19: 1380-5 [PMID:19195882]
ChEMBL	Inhibition of human recombinant PDE4B by scintillation proximity assay	B	9.4	pIC50	0.4	nM	IC50	Bioorg Med Chem Lett (2009) 19: 1380-1385 [PMID:19195882]
ChEMBL	Inhibition of human recombinant PDE4B by scintillation proximity assay	B	9.4	pIC50	0.4	nM	IC50	Bioorg Med Chem Lett (2009) 19: 5261-5265 [PMID:19656678]
ChEMBL	Inhibition of human PDE4B using [3H]cAMP as substrate incubated for 5 mins followed by substrate addition and measured after 10 mins by scintillation proximity assay	B	9.7	pIC50	0.2	nM	IC50	Bioorg Med Chem (2016) 24: 5702-5716 [PMID:27713015]
ChEMBL	Inhibition of human recombinant PDE4B using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 15 mins by SPA bead based scintillation counting analysis	B	9.82	pIC50	0.15	nM	IC50	Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478]
phosphodiesterase 4C/Phosphodiesterase 4C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL291] [GtoPdb: 1302] [UniProtKB: Q08493]
ChEMBL	Inhibition of human recombinant PDE4C	B	8.52	pIC50	3	nM	IC50	J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
ChEMBL	Inhibition of human recombinant PDE4C using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 15 mins by SPA bead based scintillation counting analysis	B	8.77	pIC50	1.7	nM	IC50	Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478]
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
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	6.32	pIC50	480	nM	IC50	Eur J Med Chem (2019) 163: 512-526 [PMID:30553143]
ChEMBL	Inhibition of human PDE4D2 catalytic domain (86 to 413) expressed in Escherichia coli BL21 using [3H]-cAMP/[3H]-cGMP after 15 mins by liquid scintillation counting	B	6.34	pIC50	460	nM	IC50	Bioorg Med Chem Lett (2012) 22: 3261-3264 [PMID:22483586]
ChEMBL	Inhibition of human U937 cells-derived PDE4D using [3H]-cAMP as substrate after 30 mins	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem Lett (2018) 28: 1188-1193 [PMID:29545101]
ChEMBL	Inhibition of human recombinant PDE4D2 activity assessed as residual cAMP concentration by HTRF assay	B	9.15	pIC50	0.7	nM	IC50	Bioorg Med Chem Lett (2014) 24: 4594-4597 [PMID:25149511]
ChEMBL	Inhibition of human PDE4D by scintillation counting method	B	9.17	pIC50	0.68	nM	IC50	J Med Chem (2020) 63: 10594-10617 [PMID:32255344]
ChEMBL	Inhibition of human PDE4D catalytic domain using [3H]-cAMP or [3H]-cGMP incubated for 30 mins by scintillation counting method	B	9.17	pIC50	0.68	nM	IC50	EP-2674161-A1. FMO3 inhibitors for treating pain (2013)
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	9.17	pIC50	0.68	nM	IC50	J Med Chem (2016) 59: 7029-7065 [PMID:26908025]
ChEMBL	Inhibition of PDE4D (unknown origin)	B	9.4	pIC50	0.4	nM	IC50	J Med Chem (2022) 65: 4238-4254 [PMID:35188767]
ChEMBL	Inhibition of PDE4D (unknown origin) using cAMP as substrate	B	9.4	pIC50	0.4	nM	IC50	J Med Chem (2019) 62: 5579-5593 [PMID:31099559]
ChEMBL	Inhibition of PDE4D2 (unknown origin)	B	9.4	pIC50	0.4	nM	IC50	J Med Chem (2020) 63: 3370-3380 [PMID:32115956]
ChEMBL	Inhibition of human recombinant PDE4D	B	9.52	pIC50	0.3	nM	IC50	J Med Chem (2021) 64: 1786-1815 [PMID:33569941]
ChEMBL	Inhibition of human PDE4D3 assessed as inhibition of [3H]cAMP hydrolysis to [3H]AMP after 15 mins by scintillation proximity assay	B	9.57	pIC50	0.27	nM	IC50	Eur J Med Chem (2011) 46: 4946-4956 [PMID:21871695]
ChEMBL	Inhibition of PDE4D (unknown origin)	B	9.7	pIC50	0.2	nM	IC50	Eur J Med Chem (2019) 174: 198-215 [PMID:31035240]
ChEMBL	Inhibition of human recombinant PDE4D using [3H]cAMP as substrate preincubated with enzyme for 10 mins followed by substrate addition and measured after 15 mins by SPA bead based scintillation counting analysis	B	9.89	pIC50	0.13	nM	IC50	Eur J Med Chem (2020) 204: 112492-112492 [PMID:32717478]

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]