ChEMBL ligand: CHEMBL514800 (Apremilast, Apremilast accord, CC-10004, CC10004, Otezla)
phosphodiesterase 4B/3`,5`-cyclic-AMP phosphodiesterase 4B in Human [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4D/3`,5`-cyclic-AMP phosphodiesterase 4D in Human [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4A in Human [GtoPdb: 1300] [UniProtKB: P27815] There should be some charts here, you may need to enable JavaScript!
phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493] 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
phosphodiesterase 4B/3`,5`-cyclic-AMP phosphodiesterase 4B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL275] [GtoPdb: 1301] [UniProtKB: Q07343]
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	7.13	pIC50	74	nM	IC50	Bioorg Med Chem (2016) 24: 5702-5716 [PMID:27713015]
ChEMBL	Inhibition of recombinant human PDE4B2 expressed in African green monkey COS7 cells using cAMP as substrate	B	7.52	pIC50	30	nM	IC50	J Med Chem (2018) 61: 2472-2489 [PMID:29502405]
ChEMBL	Inhibition of PDE4B (unknown origin)	B	7.57	pIC50	27	nM	IC50	Eur J Med Chem (2019) 174: 198-215 [PMID:31035240]
GtoPdb	Potency against recombinant human PDE4B1 and B2 isoforms in a TR-FRET assay.	-	7.57	pIC50	27	nM	IC50	Cell Signal (2014) 26: 2016-29 [PMID:24882690]
ChEMBL	Inhibitory Effect on the Enzyme In Vitro Assay: The enzyme activity was indicated by measuring the AMP/GMP expression and tracing AMP/GMP antibody binding based on fluorescence polarization in the biological assay.Reagents:Experimental Buffer Solution:10 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 0.01% Brij 35, 1 mM DTT and 1% DMSO.Enzyme:Recombinant human PDE4B (Gen accession number: NM_002600; amino acid 305 end) was expressed by baculovirus in Sf9 insect cells using an N-terminal GST tag. MW=78 kDa.Enzyme Substrate:1 μM cAMPDetection:Transcreener® AMP2/GMP2 antibody and AMP2/GMP2 AlexaFluor633 tracerOperation Procedures:i) Recombinant human PDE4B and the enzyme substrate (1 μM cAMP) were dissolved in the newly-prepared buffer solution, respectively.ii) The PDE4B buffer solution defined as above was transferred into the reaction wells.iii) The compound which was dissolved in 100% DMSO was added to the reaction wells of the PDE4B buffer solution by ultrasonic oscillator (echo 550; nanoliter range) and incubated at room temperature for 10 minutes.iv) The enzymatic buffer solution was then added to the reaction wells defined as above to initiate the reaction.v) The reaction was incubated at room temperature for 1 hour.vi) The reaction was terminated by adding detecting mixture (Transcreener AMP2/GMP2 antibody and AMP2/GMP2 AlexaFluor633 tracer) and incubated for 90 minutes with slowly mixing. The measurement range of fluorescence polarization is Ex/Em=620/688.	B	7.78	pIC50	16.5	nM	IC50	US-10662189-B2. PDE4 inhibitor (2020)
phosphodiesterase 4D/3`,5`-cyclic-AMP phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499]
ChEMBL	Inhibition of PDE4D2 (unknown origin)	B	6.27	pIC50	540	nM	IC50	J Med Chem (2020) 63: 3370-3380 [PMID:32115956]
ChEMBL	Inhibition of PDE4D2 (unknown origin)	B	6.3	pIC50	500	nM	IC50	Eur J Med Chem (2022) 242: 114631-114631 [PMID:35985255]
ChEMBL	Inhibition of PDE4D (unknown origin) using cAMP as substrate	B	7.13	pIC50	74	nM	IC50	J Med Chem (2019) 62: 5579-5593 [PMID:31099559]
ChEMBL	Inhibition of human PDE4D catalytic domain (86 to 413 residues) expressed in Escherichia coli BL21 (DE3) cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	B	7.32	pIC50	47.6	nM	IC50	J Nat Prod (2020) 83: 1229-1237 [PMID:32100544]
GtoPdb	Potency against recombinant human PDE4D2 isoform in a TR-FRET assay.	-	7.48	pIC50	33	nM	IC50	Cell Signal (2014) 26: 2016-29 [PMID:24882690]
ChEMBL	Inhibition of PDE4D (unknown origin)	B	7.48	pIC50	33	nM	IC50	Eur J Med Chem (2019) 174: 198-215 [PMID:31035240]
ChEMBL	Inhibition of his-tagged recombinant human PDE4D catalytic domain (T86 to S413 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cAMP as substrate incubated for 10 mins by SPA assay	B	7.49	pIC50	32.44	nM	IC50	Eur J Med Chem (2023) 262: 115893-115893 [PMID:37918035]
ChEMBL	Inhibition of human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 insect cells using FAM-cyclic-3',5'-AMP as substrate measured after 1 hr by fluorescence polarization assay	B	8	pIC50	10	nM	IC50	Eur J Med Chem (2024) 275: 116576-116576 [PMID:38861808]
phosphodiesterase 4A in Human [GtoPdb: 1300] [UniProtKB: P27815]
GtoPdb	Potency against recombinant human PDE4A1A isoform in a TR-FRET assay.	-	7.85	pIC50	14	nM	IC50	Cell Signal (2014) 26: 2016-29 [PMID:24882690]
phosphodiesterase 4C in Human [GtoPdb: 1302] [UniProtKB: Q08493]
GtoPdb	Potency against recombinant human PDE4C1 isoform in a TR-FRET assay.	-	6.93	pIC50	118	nM	IC50	Cell Signal (2014) 26: 2016-29 [PMID:24882690]

ChEMBL data shown on this page come from version 36:

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]