Page last updated: 2024-08-04 03:45:57

forodesine

Description

forodesine: structure in first source [MeSH]

immucillin H : no description available [CHeBI]

Cross-References

ID SourceID
PubMed CID135409409
CHEMBL ID218291
SCHEMBL ID16321929
SCHEMBL ID506383
CHEBI ID43362
MeSH IDM0292232

Synonyms (67)

Synonym
209799-67-7
immucillin-h
D06596
forodesine (usan/inn)
fodosine (tn)
IMH ,
1,4-dideoxy-4-aza-1-(s)-(9-deazahypoxanthin-9-yl)-d-ribitol
bcx-1777
fodosine
1NW4
2FF2
2FF1
1B8O
1G2O
nsc-717904
immucillin h
(1s)-1,4-dideoxy-4-imino-(9-deazahypoxanthin-9-yl)-d-ribitol
CHEBI:43362 ,
forodesine
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl)-3h-pyrrolo[3,2-d]pyrimidin-4(5h)-one
bdbm50195587
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydropyrrolo[3,2-d]pyrimidin-4-one
CHEMBL218291 ,
1-(9-deazahypoxanthin-9-yl)-1,4-dideoxy-1,4-iminoribitol
bcx 1777
nsc 717904
forodesine [usan:inn]
immh cpd
426x066elk ,
(-)-7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl)-1,5-dihydro-4h-pyrrolo(3,2-d)pyrimidin-4-one
bcx1777
unii-426x066elk
4h-pyrrolo(3,2-d)pyrimidin-4-one, 7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl)-1,5-dihydro-
forodesine [inn]
(-)-7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
forodesine [usan]
mundesine
forodesine [mi]
forodesine [who-dd]
IWKXDMQDITUYRK-KUBHLMPHSA-N
CS-3781
SCHEMBL16321929
SCHEMBL506383
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-1,5-dihydropyrrolo[2,3-e]pyrimidin-4-one
gtpl8272
fodosine (proposed trade name)
HY-16210
5(s),12(s)-dihete
(2r,3r,4s,5s)-2-(hydroxymethyl)-5-(4-hydroxy-5h-pyrrolo[3,2-d]pyrimidin-7-yl)pyrrolidine-3,4-diol
AKOS027326672
mfcd09837827
NCGC00485883-01
forodesine; immucillin h
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-3,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-hydroxymethyl-2-pyrrolidinyl]-1,5-dihydro-4h-pyrrolo-[3,2-d]-pyrimidin-4-one
Q410040
TXFGPFIDYBMMJY-KUBHLMPHSA-N
(1s)-1,4-dideoxy-1-c-(4-hydroxypyrrolo[3,2-d]pyrimidin-7-yl)-1,4-imino-d-ribitol
DB06185
AS-35282
DTXSID50943276
7-((2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl)-3,5-dihydro-4h-pyrrolo[3,2-d]pyrimidin-4-one
7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-3,5-dihydropyrrolo[3,2-d]pyrimidin-4-one
4h-pyrrolo[3,2-d]pyrimidin-4-one, 7-[(2s,3s,4r,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-
AKOS040741759
EX-A7842M

Drug Classes (2)

ClassDescription
pyrrolopyrimidine
dihydroxypyrrolidine

Protein Targets (14)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Chain A, PURINE NUCLEOSIDE PHOSPHORYLASEBos taurus (cattle)Ki0.0000AID977610
Chain A, PURINE NUCLEOSIDE PHOSPHORYLASEMycobacterium tuberculosisKi0.0000AID977610
Chain B, PURINE NUCLEOSIDE PHOSPHORYLASEMycobacterium tuberculosisKi0.0000AID977610
Chain A, IAG-nucleoside hydrolaseTrypanosoma vivaxKi0.0062AID977610
Chain A, IAG-nucleoside hydrolaseTrypanosoma vivaxKi0.0062AID977610
Purine nucleoside phosphorylaseHomo sapiens (human)IC500.0518AID272823; AID424677
Purine nucleoside phosphorylaseHomo sapiens (human)Ki0.0083AID1571176; AID1578784; AID164744; AID164928; AID164930; AID164938; AID272823; AID371442; AID409913; AID409914; AID410191
Purine nucleoside phosphorylaseMus musculus (house mouse)Ki0.0000AID164739
Purine nucleoside phosphorylase Bos taurus (cattle)Ki0.0000AID1571175; AID164739
Purine nucleoside phosphorylasePlasmodium falciparum (malaria parasite P. falciparum)Ki0.0102AID1578781; AID1578782; AID536622

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Chain A, uridine phosphorylase, putativePlasmodium falciparum 3D7Kd0.0009AID977611
Chain B, uridine phosphorylase, putativePlasmodium falciparum 3D7Kd0.0009AID977611
Chain A, Uridine phosphorylase putativePlasmodium falciparum 3D7Kd0.0009AID977611
Chain B, Uridine phosphorylase putativePlasmodium falciparum 3D7Kd0.0009AID977611
Chain A, Purine nucleoside phosphorylaseHomo sapiens (human)Kd0.0009AID977611
Purine nucleoside phosphorylaseHomo sapiens (human)Kd0.0001AID536621
Purine nucleoside phosphorylase Bos taurus (cattle)Kd0.0000AID694066

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Purine nucleoside phosphorylase Bos taurus (cattle)Kieq0.0000AID694063

Bioassays (56)

Assay IDTitleYearJournalArticle
AID1578787Antimalarial activity against Plasmodium falciparum 3D7 infected in human erythrocytes assessed as reduction in [3H]ethanolamine incorporation incubated for 18 hrs followed by addition of [3H]ethanolamine and measured after 48 hrs by scintillation countin2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
ISSN: 1520-4804
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID409913Initial binding affinity to wild type human PNP2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
ISSN: 1464-3405
Immucillins in custom catalytic-site cavities.
AID272825Inhibition of DNA synthesis in CCRF-CEM cells assessed as inhibition of [3H]Thymidine incorporation upto 100 nM2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
ISSN: 0022-2623
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID536621Inhibition of human PNP2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
ISSN: 1768-3254
Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.
AID409921Ratio of relative binding Km/Ki for wild type human PNP to relative binding affinity Km/Ki for human PNP His257Gly mutant2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
ISSN: 1464-3405
Immucillins in custom catalytic-site cavities.
AID272833Antiproliferative activity against CCRF-CEM cells2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
ISSN: 0022-2623
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID462377Inhibition of calf spleen PNP assessed as inhibition of 7-methylguanosine phosphorolysis after 50 mins by spectrophotometry in presence of 50 mM inorganic phosphate2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
ISSN: 1464-3391
Structural-based design and synthesis of novel 9-deazaguanine derivatives having a phosphate mimic as multi-substrate analogue inhibitors for mammalian PNPs.
AID409920Ratio of Km for human PNP His257Gly mutant to Ki for human PNP His257Gly mutant relative to inosine2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
ISSN: 1464-3405
Immucillins in custom catalytic-site cavities.
AID523342Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum Ghana assessed as reduction in parasite growth after 3 days by fluorimetry2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523341Antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP263 intracellular amastigotes assessed as reduction in parasite growth after 3 days by fluorometrically2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523340Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 s-galactosidase strain assessed as reduction in parasite growth after 3 days by fluorometrically2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID164739Inhibitory activity of compound against bovine purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
ISSN: 0022-2623
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID164742Dissociation constant against Human Purine Nucleoside Phosphorylase was reported2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
ISSN: 0022-2623
Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase.
AID1571176Inhibition of human PNP using inosine as substrate by xanthine oxidase coupled assay2018MedChemComm, Dec-01, Volume: 9, Issue:12
ISSN: 2040-2511
The transition to magic bullets - transition state analogue drug design.
AID164938Inhibitory activity of compound against human purine nucleoside phosphorylase (PNP)2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
ISSN: 0022-2623
Targeting the polyamine pathway with transition-state analogue inhibitors of 5'-methylthioadenosine phosphorylase.
AID1571177Inhibition of bovine spleen PNP assessed as dissociation half life using inosine as substrate by xanthine oxidase coupled assay2018MedChemComm, Dec-01, Volume: 9, Issue:12
ISSN: 2040-2511
The transition to magic bullets - transition state analogue drug design.
AID409914Equilibrium binding affinity to wild type human PNP2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
ISSN: 1464-3405
Immucillins in custom catalytic-site cavities.
AID409916Ratio of Km for wild type human PNP to Ki for wild type human PNP relative to inosine2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
ISSN: 1464-3405
Immucillins in custom catalytic-site cavities.
AID272824Inhibition of human dCK activity2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
ISSN: 0022-2623
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID523326Inhibition of Trypanosoma brucei brucei Inosine guanosine nucleoside hydrolase2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523324Inhibition of Trypanosoma vivax Inosine-adenosine-guanosine-nucleoside hydrolase2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID694066Binding affinity to calf recombinant PNP expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
ISSN: 1464-3391
Trimeric purine nucleoside phosphorylase: exploring postulated one-third-of-the-sites binding in the transition state.
AID1578784Inhibition of human PNP assessed as inhibitor constant for enzyme-inhibitor-substrate complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
ISSN: 1520-4804
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID1578782Inhibition of Plasmodium falciparum His-tagged PNP assessed as inhibitor constant for enzyme-inhibitor-substrate complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
ISSN: 1520-4804
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID523328Antitrypanosomal activity against suramin sensitive Trypanosoma brucei brucei Lister 427 assessed as reduction in parasite growth after 3 days by fluorometrically2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID410191Initial binding affinity to human PNP His257Gly mutant2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
ISSN: 1464-3405
Immucillins in custom catalytic-site cavities.
AID1578783Inhibition of human PNP assessed as inhibitor constant for enzyme-inhibitor complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
ISSN: 1520-4804
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID1571178Oral bioavailability in mouse2018MedChemComm, Dec-01, Volume: 9, Issue:12
ISSN: 2040-2511
The transition to magic bullets - transition state analogue drug design.
AID164744Inhibitory activity of compound against human purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
ISSN: 0022-2623
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID272823Inhibition of human PNP activity2006Journal of medicinal chemistry, Oct-05, Volume: 49, Issue:20
ISSN: 0022-2623
Simplified analogues of immucillin-G retain potent human purine nucleoside phosphorylase inhibitory activity.
AID92759Inhibitory activity of compound against inosine-uridine nucleoside hydrolase (IU-NH) from crithidia fasciculata2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
ISSN: 0022-2623
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID92758Inhibitory activity of compound against perine-specific inosine-adenosine-guanosine nucleoside hydrolase (IAG-NH) from Trypanosoma brucei2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
ISSN: 0022-2623
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID164604Rate constant of compound was determined for interaction with bovine purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
ISSN: 0022-2623
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID1571175Inhibition of bovine spleen PNP using inosine as substrate by xanthine oxidase coupled assay2018MedChemComm, Dec-01, Volume: 9, Issue:12
ISSN: 2040-2511
The transition to magic bullets - transition state analogue drug design.
AID164930Equilibrium dissociation constant determined against human purine nucleoside phosphorylase (PNP) after slow-onset inhibition2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
ISSN: 0022-2623
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase.
AID409918Equilibrium binding affinity to human PNP His257Gly mutant2008Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22
ISSN: 1464-3405
Immucillins in custom catalytic-site cavities.
AID694063Inhibition of bovine PNP using 7-methylguanosine as substrate by spectrophotometric based coupled assay2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
ISSN: 1464-3391
Trimeric purine nucleoside phosphorylase: exploring postulated one-third-of-the-sites binding in the transition state.
AID523327Inhibition of human purine nucleoside phosphorylase2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523329Cytotoxicity against human MRC5 SV2 cells after 48 hrs2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID523325Inhibition of Trypanosoma brucei brucei inosine-adenosine-guanosine nucleoside hydrolase (IAG-NH)2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
ISSN: 1098-6596
Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis.
AID1578781Inhibition of Plasmodium falciparum His-tagged PNP assessed as inhibitor constant for enzyme-inhibitor complex formation2019Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18
ISSN: 1520-4804
Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues.
AID164928Inhibition of human purine nucleoside phosphorylase; Initial rate.2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
ISSN: 0022-2623
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase.
AID536622Inhibition of Plasmodium falciparum PNP expressed in Escherichia coli BL21(DE3) cells by spectrophotometry2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
ISSN: 1768-3254
Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.
AID164740Rate constant of compound was determined for interaction with human purine nucleoside phosphorylase (PNP)2003Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
ISSN: 0022-2623
8-Aza-immucillins as transition-state analogue inhibitors of purine nucleoside phosphorylase and nucleoside hydrolases.
AID164741Binding affinity towards Human Purine Nucleoside Phosphorylase was reported2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
ISSN: 0022-2623
Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase.
AID371442Inhibition of human PNP by xanthine-oxidase coupled assay2009Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
ISSN: 1520-4804
Third-generation immucillins: syntheses and bioactivities of acyclic immucillin inhibitors of human purine nucleoside phosphorylase.
AID424677Inhibition of human purine nucleoside phosphorylase2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
ISSN: 1464-3405
Synthesis of analogs of forodesine HCl, a human purine nucleoside phosphorylase inhibitor-Part II.
AID1811Experimentally measured binding affinity data derived from PDB2006Journal of molecular biology, Jun-02, Volume: 359, Issue:2
ISSN: 0022-2836
Transition-state complex of the purine-specific nucleoside hydrolase of T. vivax: enzyme conformational changes and implications for catalysis.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2006Journal of molecular biology, Jun-02, Volume: 359, Issue:2
ISSN: 0022-2836
Transition-state complex of the purine-specific nucleoside hydrolase of T. vivax: enzyme conformational changes and implications for catalysis.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
ISSN: 2472-5560
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
ISSN: 1521-0111
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
ISSN: 1091-6490
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346173Human purine nucleoside phosphorylase (Nucleoside synthesis and metabolism)1998Biochemistry, Jun-16, Volume: 37, Issue:24
ISSN: 0006-2960
One-third-the-sites transition-state inhibitors for purine nucleoside phosphorylase.
AID1811Experimentally measured binding affinity data derived from PDB2001Biochemistry, Jul-27, Volume: 40, Issue:28
ISSN: 0006-2960
Structures of purine nucleoside phosphorylase from Mycobacterium tuberculosis in complexes with immucillin-H and its pieces.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2001Biochemistry, Jul-27, Volume: 40, Issue:28
ISSN: 0006-2960
Structures of purine nucleoside phosphorylase from Mycobacterium tuberculosis in complexes with immucillin-H and its pieces.
AID977610Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB2001Biochemistry, Jan-30, Volume: 40, Issue:4
ISSN: 0006-2960
Transition state structure of purine nucleoside phosphorylase and principles of atomic motion in enzymatic catalysis.
AID1811Experimentally measured binding affinity data derived from PDB2001Biochemistry, Jan-30, Volume: 40, Issue:4
ISSN: 0006-2960
Transition state structure of purine nucleoside phosphorylase and principles of atomic motion in enzymatic catalysis.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2004The Journal of biological chemistry, Apr-30, Volume: 279, Issue:18
ISSN: 0021-9258
Plasmodium falciparum purine nucleoside phosphorylase: crystal structures, immucillin inhibitors, and dual catalytic function.
AID1811Experimentally measured binding affinity data derived from PDB2004The Journal of biological chemistry, Apr-30, Volume: 279, Issue:18
ISSN: 0021-9258
Plasmodium falciparum purine nucleoside phosphorylase: crystal structures, immucillin inhibitors, and dual catalytic function.

Research

Studies (108)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (2.78)18.2507
2000's65 (60.19)29.6817
2010's33 (30.56)24.3611
2020's7 (6.48)2.80

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (6.42%)5.53%
Reviews25 (22.94%)6.00%
Case Studies2 (1.83%)4.05%
Observational1 (0.92%)0.25%
Other74 (67.89%)84.16%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
1,5-diazabicyclo(4.3.0)non-5-enepyrrolopyrimidine00low000000
antalarminpyrrolopyrimidine;
tertiary amino compound
corticotropin-releasing factor receptor antagonist00low000000
2-(1,3-dimethyl-2,4,6-trioxo-5,7-dihydropyrrolo[2,3-d]pyrimidin-5-yl)-N-(2-methoxyphenyl)acetamidepyrrolopyrimidine00low000000
2-[[2-(2-ethyl-1-piperidinyl)-2-oxoethyl]thio]-3-methyl-5H-pyrimido[5,4-b]indol-4-onepyrimido-indole;
pyrrolopyrimidine
00low000000
b 43aromatic amine;
aromatic ether;
cyclopentanes;
primary amino compound;
pyrrolopyrimidine
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
geroprotector
00low000000
tofacitinibN-acylpiperidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound
antirheumatic drug;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
00low000000
batzelladine aalkaloid;
carboxylic ester;
guanidines;
organic heterotricyclic compound;
pyrrolopyrimidine;
triazaacenaphthylene
anti-HIV-1 agent;
metabolite
00low000000
pevonedistatcyclopentanols;
indanes;
pyrrolopyrimidine;
secondary amino compound;
sulfamidate
antineoplastic agent;
apoptosis inducer
00low000000
3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1-pyrazolyl]propanenitrilepyrrolopyrimidine00low000000
incb-018424nitrile;
pyrazoles;
pyrrolopyrimidine
antineoplastic agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
00low000000
3-[(2-fluorophenyl)methyl]-5-methyl-4-thieno[3,4]pyrrolo[1,3-d]pyrimidinonepyrrolopyrimidine00low000000
baricitinibazetidines;
nitrile;
pyrazoles;
pyrrolopyrimidine;
sulfonamide
anti-inflammatory agent;
antirheumatic drug;
antiviral agent;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor;
immunosuppressive agent
00low000000
3-[(4-fluorophenyl)methyl]-5-methyl-4-thieno[3,4]pyrrolo[1,3-d]pyrimidinonepyrrolopyrimidine00low000000
delgocitinibazaspiro compound;
N-acylazetidine;
nitrile;
pyrrolopyrimidine;
tertiary amino compound;
tertiary carboxamide
anti-inflammatory drug;
antipsoriatic;
antiseborrheic;
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
00low000000
pf 956980N-acylpiperidine;
N-acylpyrrolidine;
pyrrolopyrimidine;
tertiary amino compound
EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor00low000000
gsk2656157biaryl;
indoles;
methylpyridines;
organofluorine compound;
pyrrolopyrimidine;
tertiary carboxamide
antineoplastic agent;
EC 3.1.3.48 (protein-tyrosine-phosphatase) inhibitor;
PERK inhibitor
00low000000
queuinepyrrolopyrimidineEscherichia coli metabolite00low000000
pemetrexedN-acyl-L-glutamic acid;
pyrrolopyrimidine
antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor;
EC 2.1.1.45 (thymidylate synthase) inhibitor;
EC 2.1.2.2 (phosphoribosylglycinamide formyltransferase) inhibitor
00low000000
7-deaza-2'-deoxyguanosinepyrrolopyrimidine00low000000
immucillin gdihydroxypyrrolidine;
pyrrolopyrimidine
00low000000
mirodenafilaromatic ether;
N-alkylpiperazine;
primary alcohol;
pyrrolopyrimidine;
sulfonamide
EC 3.1.4.35 (3',5'-cyclic-GMP phosphodiesterase) inhibitor;
vasodilator agent
00low000000
2,5-dihydroxymethyl-3,4-dihydroxypyrrolidinedihydroxypyrrolidine00low000000
adenosine diphosphate (hydroxymethyl)pyrrolidinedioldihydroxypyrrolidine;
purine ribonucleoside 5'-diphosphate
00low000000
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
chloroquineaminoquinoline;
organochlorine compound;
secondary amino compound;
tertiary amino compound
anticoronaviral agent;
antimalarial;
antirheumatic drug;
autophagy inhibitor;
dermatologic drug
2010201014.0low000100
tubercidinantibiotic antifungal agent;
N-glycosylpyrrolopyrimidine;
ribonucleoside
antimetabolite;
antineoplastic agent;
bacterial metabolite
201920195.0low000010
2-chloroadenosinepurine nucleoside201920195.0low000010
nsc 65346nucleoside analogueprotein kinase inhibitor201920195.0low000010
coformycincoformycinsEC 3.5.4.4 (adenosine deaminase) inhibitor201920195.0low000010
adefovir6-aminopurines;
ether;
phosphonic acids
antiviral drug;
DNA synthesis inhibitor;
drug metabolite;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent
201920195.0low000010
adefovir dipivoxil6-aminopurines;
carbonate ester;
ether;
organic phosphonate
antiviral drug;
DNA synthesis inhibitor;
HIV-1 reverse transcriptase inhibitor;
nephrotoxic agent;
prodrug
201920195.0low000010
adenosineadenosines;
purines D-ribonucleoside
analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
201920195.0low000010
psicofuraninepsicose derivative;
purine nucleoside
201920195.0low000010
4-nitrobenzylthioinosinepurine nucleoside201920195.0low000010
9-(s)-(3-hydroxy-2-(phosphonomethoxy)propyl)adenine201920195.0low000010
9-(3-hydroxy-2-phosphonomethoxypropyl)-2,6-diaminopurine201920195.0medium000010
6-(4-nitrobenzylthio)guanosine201920195.0low000010
5-iodotubercidinorganoiodine compound201920195.0low000010
angustmycin a6-aminopurines201920195.0low000010
n(6)-methyl-2'-deoxyadenosinepurine 2'-deoxyribonucleoside201920195.0medium000010
pentostatincoformycinsantimetabolite;
antineoplastic agent;
Aspergillus metabolite;
bacterial metabolite;
EC 3.5.4.4 (adenosine deaminase) inhibitor
201920195.0low000010
1,4-dideoxy-1,4-iminoarabinitol, (2r-(2alpha,3beta,4beta))-isomerpyrrolidines2010201810.0high000110
galidesivir201820186.0low000010
acyclovir2-aminopurines;
oxopurine
antimetabolite;
antiviral drug
201820186.0low000010
guanine2-aminopurines;
oxopurine;
purine nucleobase
algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
2012201212.0low000010
hypoxanthinenucleobase analogue;
oxopurine;
purine nucleobase
fundamental metabolite201220198.5low000020
inosineinosines;
purines D-ribonucleoside
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
200820199.0low000120
8-amino-9-(2-thienylmethyl)guanine201820186.0medium000010
8-amino-9-benzylguanine201820186.0medium000010
peldesine201820186.0low000010
acyclovir monophosphate201820186.0high000010
immucillin gdihydroxypyrrolidine;
pyrrolopyrimidine
2003201914.8high000420
ulodesine2003201912.6high000320
9-deazaguanine2012201212.0low000010
9-deazahypoxanthine2001200123.0medium000100
9-deaza-9-(3-thienylmethyl)guanine201820186.0low000010
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
adenine6-aminopurines;
purine nucleobase
Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
2004202111.4low000221
arsenic acidarsenic oxoacidEscherichia coli metabolite2004200420.0low000100
glycinealpha-amino acid;
amino acid zwitterion;
proteinogenic amino acid;
serine family amino acid
EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor;
fundamental metabolite;
hepatoprotective agent;
micronutrient;
neurotransmitter;
NMDA receptor agonist;
nutraceutical
2008200816.0low000100
hydrogenelemental hydrogen;
elemental molecule;
gas molecular entity
antioxidant;
electron donor;
food packaging gas;
fuel;
human metabolite
2005200519.0low000100
melatoninacetamides;
tryptamines
anticonvulsant;
central nervous system depressant;
geroprotector;
hormone;
human metabolite;
immunological adjuvant;
mouse metabolite;
radical scavenger
2003200321.0low000100
purinepurine2005200519.0low000100
pyruvic acid2-oxo monocarboxylic acidcofactor;
fundamental metabolite
2004200420.0low000100
mercaptoethanolalkanethiol;
primary alcohol
geroprotector2009200915.0low000100
mechlorethaminenitrogen mustard;
organochlorine compound
alkylating agent2007200717.0low000100
vorinostatdicarboxylic acid diamide;
hydroxamic acid
antineoplastic agent;
apoptosis inducer;
EC 3.5.1.98 (histone deacetylase) inhibitor
2007201214.5low100110
thalidomidephthalimides;
piperidones
2010201213.3low100210
prednisone11-oxo steroid;
17alpha-hydroxy steroid;
20-oxo steroid;
21-hydroxy steroid;
3-oxo-Delta(1),Delta(4)-steroid;
C21-steroid;
glucocorticoid;
primary alpha-hydroxy ketone;
tertiary alpha-hydroxy ketone
adrenergic agent;
anti-inflammatory drug;
antineoplastic agent;
immunosuppressive agent;
prodrug
2008200816.0low000100
aspartic acidaspartate family amino acid;
aspartic acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
mouse metabolite;
neurotransmitter
2005200519.0low000100
tubercidinantibiotic antifungal agent;
N-glycosylpyrrolopyrimidine;
ribonucleoside
antimetabolite;
antineoplastic agent;
bacterial metabolite
2010201014.0low000100
asparagineamino acid zwitterion;
asparagine;
aspartate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
2002200222.0low000100
histidineamino acid zwitterion;
histidine;
L-alpha-amino acid;
polar amino acid zwitterion;
proteinogenic amino acid
algal metabolite;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
Saccharomyces cerevisiae metabolite
2008200816.0low000100
tryptophanerythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid zwitterion;
L-alpha-amino acid;
proteinogenic amino acid;
tryptophan zwitterion;
tryptophan
antidepressant;
Escherichia coli metabolite;
human metabolite;
micronutrient;
mouse metabolite;
nutraceutical;
plant metabolite;
Saccharomyces cerevisiae metabolite
2009200915.0low000100
xylitol2004200420.0low000100
phosphoribosyl pyrophosphate5-O-phosphono-D-ribofuranosyl diphosphateEscherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite
1999199925.0low001000
pyrrolespyrrole;
secondary amine
1998201520.4medium1043720
piperidineazacycloalkane;
piperidines;
saturated organic heteromonocyclic parent;
secondary amine
base;
catalyst;
human metabolite;
non-polar solvent;
plant metabolite;
protic solvent;
reagent
202120213.0low000001
pyrazinesdiazine;
pyrazines
Daphnia magna metabolite2010201213.0low100110
methylthioinosinepurine ribonucleoside;
thiopurine
2004200420.0low000100
deoxycytidinepyrimidine 2'-deoxyribonucleosideEscherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
2008200816.0low000100
d-alpha tocopherolalpha-tocopherolalgal metabolite;
antiatherogenic agent;
anticoagulant;
antioxidant;
antiviral agent;
EC 2.7.11.13 (protein kinase C) inhibitor;
immunomodulator;
micronutrient;
nutraceutical;
plant metabolite
202020204.0low000010
stavudinedihydrofuran;
nucleoside analogue;
organic molecular entity
antimetabolite;
antiviral agent;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
2003200321.0low000100
dithiothreitol1,4-dimercaptobutane-2,3-diol;
butanediols;
dithiol;
glycol;
thiol
chelator;
human metabolite;
reducing agent
2003200918.7low000300
vidarabinebeta-D-arabinoside;
purine nucleoside
antineoplastic agent;
bacterial metabolite;
nucleoside antibiotic
2009201014.5low100200
deuteriumdihydrogen2001200521.0low000200
glutamic acidglutamic acid;
glutamine family amino acid;
L-alpha-amino acid;
proteinogenic amino acid
Escherichia coli metabolite;
ferroptosis inducer;
micronutrient;
mouse metabolite;
neurotransmitter;
nutraceutical
2002200222.0low000100
gemcitabineorganofluorine compound;
pyrimidine 2'-deoxyribonucleoside
antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
2008200816.0low000100
lamivudinemonothioacetal;
nucleoside analogue;
oxacycle;
primary alcohol
allergen;
anti-HBV agent;
antiviral drug;
EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor;
HIV-1 reverse transcriptase inhibitor;
prodrug
2003200321.0low000100
adenosineadenosines;
purines D-ribonucleoside
analgesic;
anti-arrhythmia drug;
fundamental metabolite;
human metabolite;
vasodilator agent
200820218.2low000131
neplanocin a202020204.0low000010
bendamustine hydrochloride2008201214.3low100210
clofarabineadenosines;
organofluorine compound
antimetabolite;
antineoplastic agent
2007201613.5low000220
magnesium pyrophosphate1999199925.0low001000
10-propargyl-10-deazaaminopterinN-acyl-L-glutamic acid;
pteridines;
terminal acetylenic compound
antimetabolite;
antineoplastic agent;
EC 1.5.1.3 (dihydrofolate reductase) inhibitor
2010201014.0low000100
aminopterindicarboxylic acidEC 1.5.1.3 (dihydrofolate reductase) inhibitor;
mutagen
2010201014.0low000100
enzastaurinindoles;
maleimides
2008201214.0low100110
lenalidomidearomatic amine;
dicarboximide;
isoindoles;
piperidones
angiogenesis inhibitor;
antineoplastic agent;
immunomodulator
2010201213.3low100210
bortezomibamino acid amide;
L-phenylalanine derivative;
pyrazines
antineoplastic agent;
antiprotozoal drug;
protease inhibitor;
proteasome inhibitor
2010201213.0low100110
5'-methylthioadenosinethioadenosinealgal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
2005200519.0low000100
n-acetylneuraminic acidN-acetylneuraminic acidsantioxidant;
bacterial metabolite;
EC 3.2.1.18 (exo-alpha-sialidase) inhibitor;
human metabolite;
mouse metabolite
2010201014.0low000100
hexacyanoferrate iii2004200420.0low000100
sodium arsenitearsenic molecular entity;
inorganic sodium salt
antibacterial agent;
antifungal agent;
antineoplastic agent;
carcinogenic agent;
herbicide;
insecticide;
rodenticide
2009200915.0low000100
acetyl coenzyme aacyl-CoAacyl donor;
coenzyme;
effector;
fundamental metabolite
2009200915.0low000100
pyrophosphatediphosphate ion1999199925.0low001000
fludarabinepurine nucleoside2009201014.5low100200
unithiol2009200915.0low000100
succimerdicarboxylic acid;
dithiol;
sulfur-containing carboxylic acid
chelator2009200915.0low000100
nadp2004200420.0low000100
nelarabinebeta-D-arabinoside;
monosaccharide derivative;
purine nucleoside
antineoplastic agent;
DNA synthesis inhibitor;
prodrug
2006201414.7low000430
sirolimusantibiotic antifungal drug;
cyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
organic heterotricyclic compound;
secondary alcohol
antibacterial drug;
anticoronaviral agent;
antineoplastic agent;
bacterial metabolite;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
2008201214.0low100110
antimonymetalloid atom;
pnictogen
2003200321.0low000100
arsenicmetalloid atom;
pnictogen
micronutrient2003200321.0low000100
involucrin2003200321.0low000100
everolimuscyclic acetal;
cyclic ketone;
ether;
macrolide lactam;
primary alcohol;
secondary alcohol
anticoronaviral agent;
antineoplastic agent;
geroprotector;
immunosuppressive agent;
mTOR inhibitor
2012201212.0low100010
galidesivir200820219.2low000121
piperidines2003202112.0low000101
cyclosporine2002200222.0low000100
acyclovir2-aminopurines;
oxopurine
antimetabolite;
antiviral drug
2005200519.0low000100
deoxyguanosinepurine 2'-deoxyribonucleoside;
purines 2'-deoxy-D-ribonucleoside
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
2003200818.4low000500
deoxyguanosine triphosphatedeoxyguanosine phosphate;
guanyl deoxyribonucleotide;
purine 2'-deoxyribonucleoside 5'-triphosphate
Arabidopsis thaliana metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
plant metabolite;
Saccharomyces cerevisiae metabolite
2001202015.8low200530
guanosine monophosphateguanosine 5'-phosphate;
purine ribonucleoside 5'-monophosphate
biomarker;
Escherichia coli metabolite;
metabolite;
mouse metabolite
1999200323.0low001100
guanosine triphosphateguanosine 5'-phosphate;
purine ribonucleoside 5'-triphosphate
Escherichia coli metabolite;
mouse metabolite;
uncoupling protein inhibitor
2001200123.0low000100
guanine2-aminopurines;
oxopurine;
purine nucleobase
algal metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
2003200520.0low000200
guanosineguanosines;
purines D-ribonucleoside
fundamental metabolite2003200520.0low000200
hypoxanthinenucleobase analogue;
oxopurine;
purine nucleobase
fundamental metabolite1999201220.2low001310
inosinic acidinosine phosphate;
purine ribonucleoside 5'-monophosphate
Escherichia coli metabolite;
human metabolite;
mouse metabolite
1999199925.0low001000
inosineinosines;
purines D-ribonucleoside
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
2001200919.4low000900
azaguaninenucleobase analogue;
triazolopyrimidines
antimetabolite;
antineoplastic agent;
EC 2.4.2.1 (purine-nucleoside phosphorylase) inhibitor
2005200519.0low000100
peldesine2003200321.0low000100
immucillin gdihydroxypyrrolidine;
pyrrolopyrimidine
1998201519.5high002620
ulodesine2006201016.0medium000300
9-arabinofuranosylguaninebeta-D-arabinoside;
purine nucleoside
antineoplastic agent;
DNA synthesis inhibitor
2011201113.0low000010
5'-deoxy-5'-methylthioinosine5'-deoxyribonucleoside;
inosines
2004200420.0medium000100
pyrimidinones1998202216.3high70470193
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Acute Disease02013201311.0low100010
Acute Lymphoid Leukemia02007201612.5low000110
Acute Myelogenous Leukemia02011201113.0low000010
Adverse Drug Event0201520159.0low000010
African Sleeping Sickness02010201014.0low000100
Anaplastic Large-Cell Lymphoma02012201212.0low100010
ATLL02003201017.7low000300
B-Cell Chronic Lymphocytic Leukemia02006202013.7low100510
B-Cell Leukemia02007200717.0low000100
B-Cell Lymphoma02012201411.0low100020
B-Cell Prolymphocytic Leukemia02011201113.0low000010
Benign Neoplasms02006201016.0low000200
Black Fever0201520159.0low000020
Brill-Symmers Disease02008200816.0low000100
Cancer of Skin02007201712.6low200230
Congenital Zika Syndrome0202020204.0low000010
Cutaneous T-Cell Lymphoma02007201712.0low000110
Diffuse Large B-Cell Lymphoma02008200816.0low000100
Disease Models, Animal0201520206.5low000020
Drug-Related Side Effects and Adverse Reactions0201520159.0low000010
Erythroderma, Sezary02007201414.7low100210
Exanthem02012201212.0low100010
Exanthema02012201212.0low100010
Experimental Leukemia02006200618.0low000100
Germinoblastoma02006201215.0low100110
Graft vs Host Disease02002200222.0low000100
Graft-Versus-Host Disease02002200222.0low000100
Hematologic Malignancies02008201114.5low000110
Hematologic Neoplasms02008201114.5low000110
Infections, Plasmodium02004201912.5low000110
Leishmaniasis, American0201520159.0low000010
Leishmaniasis, Cutaneous0201520159.0low000010
Leishmaniasis, Visceral0201520159.0low000020
Leucocythaemia02006200618.0low000100
Leukemia12006200618.0low000100
Leukemia-Lymphoma, Adult T-Cell02003201017.7low000300
Leukemia, Lymphoblastic, Acute, T Cell02007201413.3low000120
Leukemia, Lymphocytic02005200519.0low100100
Leukemia, Lymphocytic, Chronic, B-Cell12006202013.7low100510
Leukemia, Lymphocytic, T Cell02002200818.3low000300
Leukemia, Lymphoid02005200519.0low100100
Leukemia, Myeloid, Acute02011201113.0low000010
Leukemia, Pre-B-Cell02013201311.0low100010
Leukemia, Prolymphocytic, B-Cell02011201113.0low000010
Leukemia, T-Cell02002200818.3low000300
Local Neoplasm Recurrence02007200717.0low000100
Lymphocytopenia02012201212.0low100010
Lymphoma12006201215.0low100110
Lymphoma, B-Cell02012201411.0low100020
Lymphoma, Follicular02008200816.0low000100
Lymphoma, Large B-Cell, Diffuse02008200816.0low000100
Lymphoma, Large-Cell, Anaplastic02012201212.0low100010
Lymphoma, T Cell, Peripheral0200820228.5low200222
Lymphoma, T-Cell02006201215.0low100110
Lymphoma, T-Cell, Cutaneous12007201712.0low000110
Lymphoma, T-Cell, Peripheral0200820228.5low200222
Lymphopenia02012201212.0low100010
Malaria02004201912.5low000110
Malaria, Falciparum02011201113.0low000010
Malignant Melanoma02011201113.0low000010
Melanoma02011201113.0low000010
Mycosis Fungoides02007201413.0low200120
Neoplasms02006201016.0low000200
Parodontosis02013201311.0low000010
Periodontal Diseases02013201311.0low000010
Plasmodium falciparum Malaria02011201113.0low000010
Precursor B-Cell Lymphoblastic Leukemia-Lymphoma02013201311.0low100010
Precursor Cell Lymphoblastic Leukemia-Lymphoma02007201612.5low000110
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma02007201413.3low000120
Recrudescence0201220198.3low200030
Sensitivity and Specificity02011201113.0low000010
Sezary Syndrome02007201414.7low100210
Skin Neoplasms02007201712.6low200230
T-Cell Lymphoma02006201215.0low100110
Trypanosomiasis, African02010201014.0low000100
Zika Virus Infection0202020204.0low000010

Pharmacokinetics (2)

ArticleYear
Phase 2 and pharmacodynamic study of oral forodesine in patients with advanced, fludarabine-treated chronic lymphocytic leukemia.
Blood, , Aug-12, Volume: 116, Issue:6
2010
A proof-of-principle pharmacokinetic, pharmacodynamic, and clinical study with purine nucleoside phosphorylase inhibitor immucillin-H (BCX-1777, forodesine).
Blood, , Dec-15, Volume: 106, Issue:13
2005

Bioavailability (4)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, , Volume: 96, Issue:5
2019
Preclinical and clinical evaluation of forodesine in pediatric and adult B-cell acute lymphoblastic leukemia.
Clinical lymphoma, myeloma & leukemia, , Volume: 13, Issue:4
2013
Intravenous and oral pharmacokinetic study of BCX-1777, a novel purine nucleoside phosphorylase transition-state inhibitor. In vivo effects on blood 2'-deoxyguanosine in primates.
International immunopharmacology, , Volume: 3, Issue:4
2003
Purine nucleoside phosphorylase inhibitor BCX-1777 (Immucillin-H)--a novel potent and orally active immunosuppressive agent.
International immunopharmacology, , Volume: 1, Issue:6
2001

Dosage (3)

ArticleYear
Forodesine in the treatment of cutaneous T-cell lymphoma.
Expert opinion on investigational drugs, , Volume: 26, Issue:6
2017
Phase 2 and pharmacodynamic study of oral forodesine in patients with advanced, fludarabine-treated chronic lymphocytic leukemia.
Blood, , Aug-12, Volume: 116, Issue:6
2010
Intravenous and oral pharmacokinetic study of BCX-1777, a novel purine nucleoside phosphorylase transition-state inhibitor. In vivo effects on blood 2'-deoxyguanosine in primates.
International immunopharmacology, , Volume: 3, Issue:4
2003