| Reaction Details |
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 | Report a problem with these data |
| Target | Phosphodiesterase |
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| Ligand | BDBM153393 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | TbrPDEB1 Enzyme Assay |
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| pH | 7.4±n/a |
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| IC50 | 1.6e+4± 1.7e+3 nM |
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| Comments | extracted |
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| Citation |  Ochiana, SO; Bland, ND; Settimo, L; Campbell, RK; Pollastri, MP Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei. Chem Biol Drug Des85:549-64 (2015) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Phosphodiesterase |
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| Name: | Phosphodiesterase |
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| Synonyms: | Class 1 phosphodiesterase PDEB1 | Class I phosphodiesterase B1 (TbrPDEB1) | PDEB1 |
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| Type: | Protein |
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| Mol. Mass.: | 103683.20 |
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| Organism: | Trypanosoma brucei |
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| Description: | n/a |
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| Residue: | 930 |
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| Sequence: | MFMNKPFGSKRCEPFHESEHLCEAFAITEAILARYQRGKRSFTSSEKSGLAALIKRIPYD
ILVEVLDQSGFTPTSNATPPVDYLAMMEHTMTHGASITHALQYLNDLMTKCTGCPGIRTY
YHNPNDDVLADPVHDTAALIDETTAVGKSVVTKQYLNIAGAHYIPLIHGDIVVGCVEVPR
FSGNLEKLPSFPSLIRAVTCTAHKFIEEARINWNREKAEAMLQMATRLARDNLDETVLAS
SIMNTVKSLTESARCSLFLVKDDKLEAHFEDGNVVSIPKGTGIVGYVAQTGETVNIVDAY
ADDRFNREVDKATGYRTKTILCMPVMYEGTIVAVTQLINKLDLTTESGLRLPRVFGKRDE
ELFQTFSMFAGASLRNCRINDRLLKEKKKSDVILDVVTVLSNTDIRDVDGIVRHALHGAK
KLLNADRSTLFLVDKERNELCSRMADSVAGKEIRFPCGQGIAGTVAASGVGENIQDAYQD
PRFNREVDKQLGYRTQTILCEPIILNGEILAVVQLVNKLDTSGEVTVFTEDDRDTFRVFS
LFAGISINNSHLLEFAVKAGREVMELNEHRATLFNKNVPSRAVKRVTAITKVEREAVLVC
ELPSFDVTDVEFDLFRARESTDKPLDVAAAIAYRLLLGSGLPQKFGCSDEVLLNFILQCR
KKYRNVPYHNFYHVVDVCQTIHTFLYRGNVYEKLTELECFVLLITALVHDLDHMGLNNSF
YLKTESPLGILSSASGNTSVLEVHHCNLAVEILSDPESDVFDGLEGAERTLAFRSMIDCV
LATDMAKHGSALEAFLASAADQSSDEAAFHRMTMEIILKAGDISNVTKPFDISRQWAMAV
TEEFYRQGDMEKERGVEVLPMFDRSKNMELAKGQIGFIDFVAAPFFQKIVDACLQGMQWT
VDRIKSNRAQWERVLETRLSTSSGNNSSTR
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| BDBM153393 |
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| n/a |
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| Name | BDBM153393 |
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| Synonyms: | Methyl 3-(3-carbamoyl-4-(3-methoxyphenylamino)-8-methylquinolin-6-ylamino)benzoate (13) |
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| Type | Small organic molecule |
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| Emp. Form. | C26H24N4O4 |
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| Mol. Mass. | 456.4932 |
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| SMILES | COC(=O)c1cccc(Nc2cc(C)c3ncc(C(N)=O)c(Nc4cccc(OC)c4)c3c2)c1 |
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| Structure | 
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