Reaction Details |
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Target | Phosphodiesterase |
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Ligand | BDBM153412 |
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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 | 3.7e+3± 5e+2 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 |
Synonyms: | Class 1 phosphodiesterase PDEB1 | Class I phosphodiesterase B1 (TbrPDEB1) | PDEB1 |
Type: | Protein |
Mol. Mass.: | 103683.20 |
Organism: | Trypanosoma brucei |
Description: | n/a |
Residue: | 930 |
Sequence: | MFMNKPFGSKRCEPFHESEHLCEAFAITEAILARYQRGKRSFTSSEKSGLAALIKRIPYD
ILVEVLDQSGFTPTSNATPPVDYLAMMEHTMTHGASITHALQYLNDLMTKCTGCPGIRTY
YHNPNDDVLADPVHDTAALIDETTAVGKSVVTKQYLNIAGAHYIPLIHGDIVVGCVEVPR
FSGNLEKLPSFPSLIRAVTCTAHKFIEEARINWNREKAEAMLQMATRLARDNLDETVLAS
SIMNTVKSLTESARCSLFLVKDDKLEAHFEDGNVVSIPKGTGIVGYVAQTGETVNIVDAY
ADDRFNREVDKATGYRTKTILCMPVMYEGTIVAVTQLINKLDLTTESGLRLPRVFGKRDE
ELFQTFSMFAGASLRNCRINDRLLKEKKKSDVILDVVTVLSNTDIRDVDGIVRHALHGAK
KLLNADRSTLFLVDKERNELCSRMADSVAGKEIRFPCGQGIAGTVAASGVGENIQDAYQD
PRFNREVDKQLGYRTQTILCEPIILNGEILAVVQLVNKLDTSGEVTVFTEDDRDTFRVFS
LFAGISINNSHLLEFAVKAGREVMELNEHRATLFNKNVPSRAVKRVTAITKVEREAVLVC
ELPSFDVTDVEFDLFRARESTDKPLDVAAAIAYRLLLGSGLPQKFGCSDEVLLNFILQCR
KKYRNVPYHNFYHVVDVCQTIHTFLYRGNVYEKLTELECFVLLITALVHDLDHMGLNNSF
YLKTESPLGILSSASGNTSVLEVHHCNLAVEILSDPESDVFDGLEGAERTLAFRSMIDCV
LATDMAKHGSALEAFLASAADQSSDEAAFHRMTMEIILKAGDISNVTKPFDISRQWAMAV
TEEFYRQGDMEKERGVEVLPMFDRSKNMELAKGQIGFIDFVAAPFFQKIVDACLQGMQWT
VDRIKSNRAQWERVLETRLSTSSGNNSSTR
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BDBM153412 |
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n/a |
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Name | BDBM153412 |
Synonyms: | 8-Ethyl-4-((3-methoxyphenyl)amino)-6-(1-methyl-1H-indazol-6-yl)quinoline-3-carboxamide (19c) |
Type | Small organic molecule |
Emp. Form. | C27H25N5O2 |
Mol. Mass. | 451.5197 |
SMILES | CCc1cc(cc2c(Nc3cccc(OC)c3)c(cnc12)C(N)=O)-c1ccc2cnn(C)c2c1 |
Structure |
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