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ChEMBL ligand: CHEMBL193240 (Arq-151, B-9302-107, B9302-107, BY217, BY-217, BYK20869, BYK-20869, Daliresp, Daxas, Roflumilast, Zoryve) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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 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 PDE4B2 | B | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734] |
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 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 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 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 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 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 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 (null) |
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 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 PDE4D2 (unknown origin) | B | 9.4 | pIC50 | 0.4 | nM | IC50 | J Med Chem (2020) 63: 3370-3380 [PMID:32115956] |
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 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 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]