Reaction Details |
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Target | cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
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Ligand | BDBM14370 |
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Substrate/Competitor | BDBM10851 |
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Meas. Tech. | PDE Activity Assay |
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pH | 8±n/a |
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Temperature | 295.15±n/a K |
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Ki | 126±43 nM |
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Citation | Whitehead, JW; Lee, GP; Gharagozloo, P; Hofer, P; Gehrig, A; Wintergerst, P; Smyth, D; McCoull, W; Hachicha, M; Patel, A; Kyle, DJ 8-Substituted analogues of 3-(3-cyclopentyloxy-4-methoxy-benzyl)-8-isopropyladenine: highly potent and selective PDE4 inhibitors. J Med Chem48:1237-43 (2005) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
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Name: | cAMP-specific 3',5'-cyclic phosphodiesterase 4A |
Synonyms: | 3',5'-cyclic phosphodiesterase | DPDE2 | PDE46 | PDE4A | PDE4A_HUMAN | Phosphodiesterase 4 (PDE4) | Phosphodiesterase 4A | Phosphodiesterase 4A (PDE4) |
Type: | Enzyme |
Mol. Mass.: | 98113.27 |
Organism: | Homo sapiens (Human) |
Description: | P27815 |
Residue: | 886 |
Sequence: | MEPPTVPSERSLSLSLPGPREGQATLKPPPQHLWRQPRTPIRIQQRGYSDSAERAERERQ
PHRPIERADAMDTSDRPGLRTTRMSWPSSFHGTGTGSGGAGGGSSRRFEAENGPTPSPGR
SPLDSQASPGLVLHAGAATSQRRESFLYRSDSDYDMSPKTMSRNSSVTSEAHAEDLIVTP
FAQVLASLRSVRSNFSLLTNVPVPSNKRSPLGGPTPVCKATLSEETCQQLARETLEELDW
CLEQLETMQTYRSVSEMASHKFKRMLNRELTHLSEMSRSGNQVSEYISTTFLDKQNEVEI
PSPTMKEREKQQAPRPRPSQPPPPPVPHLQPMSQITGLKKLMHSNSLNNSNIPRFGVKTD
QEELLAQELENLNKWGLNIFCVSDYAGGRSLTCIMYMIFQERDLLKKFRIPVDTMVTYML
TLEDHYHADVAYHNSLHAADVLQSTHVLLATPALDAVFTDLEILAALFAAAIHDVDHPGV
SNQFLINTNSELALMYNDESVLENHHLAVGFKLLQEDNCDIFQNLSKRQRQSLRKMVIDM
VLATDMSKHMTLLADLKTMVETKKVTSSGVLLLDNYSDRIQVLRNMVHCADLSNPTKPLE
LYRQWTDRIMAEFFQQGDRERERGMEISPMCDKHTASVEKSQVGFIDYIVHPLWETWADL
VHPDAQEILDTLEDNRDWYYSAIRQSPSPPPEEESRGPGHPPLPDKFQFELTLEEEEEEE
ISMAQIPCTAQEALTAQGLSGVEEALDATIAWEASPAQESLEVMAQEASLEAELEAVYLT
QQAQSTGSAPVAPDEFSSREEFVVAVSHSSPSALALQSPLLPAWRTLSVSEHAPGLPGLP
STAAEVEAQREHQAAKRACSACAGTFGEDTSALPAPGGGGSGGDPT
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BDBM14370 |
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BDBM10851 |
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Name | BDBM14370 |
Synonyms: | 8-{1-[(4-Chlorobenzyl)oxy]-1-methyl-ethyl}-3-[3-cyclopentyloxy)-4-methoxybenzyl]-3H-purin-6-amine | 8-{2-[(4-chlorophenyl)methoxy]propan-2-yl}-3-{[3-(cyclopentyloxy)-4-methoxyphenyl]methyl}-3H-purin-6-amine | V11294 Analogue 5f |
Type | Small organic molecule |
Emp. Form. | C28H32ClN5O3 |
Mol. Mass. | 522.038 |
SMILES | COc1ccc(Cn2cnc(N)c3nc(nc23)C(C)(C)OCc2ccc(Cl)cc2)cc1OC1CCCC1 |
Structure |
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