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TargetPhosphodiesterase
LigandBDBM153408
Substrate/Competitorn/a
Meas. Tech.TbrPDEB1 Enzyme Assay
pH7.4±n/a
IC50 3.5e+3± 6e+2 nM
Commentsextracted
Citation Ochiana, SOBland, NDSettimo, LCampbell, RKPollastri, 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
More Info.:Get all data from this article,  Assay Method
 
Phosphodiesterase
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM153408
n/a
NameBDBM153408
Synonyms:8-Methyl-6-(1-methyl-1H-indazol-6-yl)-4-(m-tolylamino)quinoline-3-carboxamide (24e)
TypeSmall organic molecule
Emp. Form.C26H23N5O
Mol. Mass.421.4937
SMILESCc1cccc(Nc2c(cnc3c(C)cc(cc23)-c2ccc3cnn(C)c3c2)C(N)=O)c1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: