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TargetInosine-5'-monophosphate dehydrogenase 2
LigandBDBM19282
Substrate/CompetitorBDBM19254
Meas. Tech.IMPDH2 Enzyme Inhibition and Human T-Lymphoblast (CEM) Proliferation Inhibition Assays
pH8±n/a
Temperature298.15±n/a K
IC50 12±3.2 nM
EC50 580±130 nM
Citation Watterson, SHChen, PZhao, YGu, HHDhar, TGXiao, ZBallentine, SKShen, ZFleener, CARouleau, KAObermeier, MYang, ZMcIntyre, KWShuster, DJWitmer, MDambach, DChao, SMathur, AChen, BCBarrish, JCRobl, JATownsend, RIwanowicz, EJ Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419). J Med Chem50:3730-42 (2007) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Inosine-5'-monophosphate dehydrogenase 2
Name:Inosine-5'-monophosphate dehydrogenase 2
Synonyms:IMDH2_HUMAN | IMP dehydrogenase 2 | IMPD 2 | IMPD2 | IMPDH-II | IMPDH2 | Inosine 5'-monophosphate dehydrogenase II (IMPDH II) | Inosine Monophosphate Dehydrogenase Type 2 (IMPDH2) | Inosine-5 -monophosphate dehydrogenase 2 | Inosine-5'-monophosphate dehydrogenase (IMPDH)
Type:Enzyme
Mol. Mass.:55806.87
Organism:Homo sapiens (Human)
Description:Recombinant IMPDH2 expressed in E. coli.
Residue:514
Sequence:
MADYLISGGTSYVPDDGLTAQQLFNCGDGLTYNDFLILPGYIDFTADQVDLTSALTKKIT
LKTPLVSSPMDTVTEAGMAIAMALTGGIGFIHHNCTPEFQANEVRKVKKYEQGFITDPVV
LSPKDRVRDVFEAKARHGFCGIPITDTGRMGSRLVGIISSRDIDFLKEEEHDCFLEEIMT
KREDLVVAPAGITLKEANEILQRSKKGKLPIVNEDDELVAIIARTDLKKNRDYPLASKDA
KKQLLCGAAIGTHEDDKYRLDLLAQAGVDVVVLDSSQGNSIFQINMIKYIKDKYPNLQVI
GGNVVTAAQAKNLIDAGVDALRVGMGSGSICITQEVLACGRPQATAVYKVSEYARRFGVP
VIADGGIQNVGHIAKALALGASTVMMGSLLAATTEAPGEYFFSDGIRLKKYRGMGSLDAM
DKHLSSQNRYFSEADKIKVAQGVSGAVQDKGSIHKFVPYLIAGIQHSCQDIGAKSLTQVR
AMMYSGELKFEKRTSSAQVEGGVHSLHSYEKRLF
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BDBM19282
BDBM19254
NameBDBM19282
Synonyms:2-fluoro-N-[2-(3-methanesulfonylphenyl)propan-2-yl]-9-oxo-9,10-dihydroacridine-3-carboxamide | Acridone-Based Inhibitor, 4f
TypeSmall organic molecule
Emp. Form.C24H21FN2O4S
Mol. Mass.452.498
SMILESCC(C)(NC(=O)c1cc2[nH]c3ccccc3c(=O)c2cc1F)c1cccc(c1)S(C)(=O)=O
Structure
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