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TargetMethylthioadenosine Phosphorylase (MTAP)
LigandBDBM22113
Substrate/CompetitorBDBM22111
Meas. Tech.MTAP/MTAN Inhibition Assay
pH7±n/a
Temperature295.15±n/a K
Ki 1.7±0.2 nM
Km5000±n/a nM
CommentsKi is the dissociation constant for the first step in the two-step binding characteristic of slow-onset tight-binding inhibition.
Citation Evans GBFurneaux RHGreatrex BMurkin ASSchramm VLTyler PC Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases. J Med Chem 51:948-56 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Methylthioadenosine Phosphorylase (MTAP)
Name:Methylthioadenosine Phosphorylase (MTAP)
Synonyms:5'-Methylthioadenosine phosphorylase (MTAP) | MTA phosphorylase | MTAPase | S-methyl-5 -thioadenosine phosphorylase
Type:Enzyme
Mol. Mass.:31239.23
Organism:Homo sapiens (Human)
Description:n/a
Residue:283
Sequence:
MASGTTTTAVKIGIIGGTGLDDPEILEGRTEKYVDTPFGKPSDALILGKIKNVDCVLLAR
HGRQHTIMPSKVNYQANIWALKEEGCTHVIVTTACGSLREEIQPGDIVIIDQFIDRTTMR
PQSFYDGSHSCARGVCHIPMAEPFCPKTREVLIETAKKLGLRCHSKGTMVTIEGPRFSSR
AESFMFRTWGADVINMTTVPEVVLAKEAGICYASIAMATDYDCWKEHEEAVSVDRVLKTL
KENANKAKSLLLTTIPQIGSTEWSETLHNLKNMAQFSVLLPRH
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  Blast E-value cutoff:
BDBM22113
BDBM22111
NameBDBM22113
Synonyms:(3R,4S)-1-({4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl}methyl)-4-[(methylsulfanyl)methyl]pyrrolidin-3-ol | (3R,4S)-1-[(4-amino-5H-pyrrolo[3,2-d]pyrimidin-7-yl)methyl]-4-[(methylsulfanyl)methyl]pyrrolidin-3-ol | (3R,4S)-1-[(9-Deazaadenin-9-yl)methyl]-3-hydroxy-4-methylthiomethylpyrrolidine, 7 | DADMe-ImmA-Me | MT-DADMe-ImmA
Typen/a
Emp. Form.C13H19N5OS
Mol. Mass.293.388
SMILESCSC[C@H]1CN(Cc2c[nH]c3c(N)ncnc23)C[C@@H]1O |r|
Structure
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