forodesine: structure in first source [MeSH]
immucillin H : no description available [CHeBI]
ID Source | ID |
---|---|
PubMed CID | 135409409 |
CHEMBL ID | 218291 |
SCHEMBL ID | 16321929 |
SCHEMBL ID | 506383 |
CHEBI ID | 43362 |
MeSH ID | M0292232 |
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 |
Class | Description |
---|---|
pyrrolopyrimidine | |
dihydroxypyrrolidine |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Chain A, PURINE NUCLEOSIDE PHOSPHORYLASE | Bos taurus (cattle) | Ki | 0.0000 | AID977610 |
Chain A, PURINE NUCLEOSIDE PHOSPHORYLASE | Mycobacterium tuberculosis | Ki | 0.0000 | AID977610 |
Chain B, PURINE NUCLEOSIDE PHOSPHORYLASE | Mycobacterium tuberculosis | Ki | 0.0000 | AID977610 |
Chain A, IAG-nucleoside hydrolase | Trypanosoma vivax | Ki | 0.0062 | AID977610 |
Chain A, IAG-nucleoside hydrolase | Trypanosoma vivax | Ki | 0.0062 | AID977610 |
Purine nucleoside phosphorylase | Homo sapiens (human) | IC50 | 0.0518 | AID272823; AID424677 |
Purine nucleoside phosphorylase | Homo sapiens (human) | Ki | 0.0083 | AID1571176; AID1578784; AID164744; AID164928; AID164930; AID164938; AID272823; AID371442; AID409913; AID409914; AID410191 |
Purine nucleoside phosphorylase | Mus musculus (house mouse) | Ki | 0.0000 | AID164739 |
Purine nucleoside phosphorylase | Bos taurus (cattle) | Ki | 0.0000 | AID1571175; AID164739 |
Purine nucleoside phosphorylase | Plasmodium falciparum (malaria parasite P. falciparum) | Ki | 0.0102 | AID1578781; AID1578782; AID536622 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Chain A, uridine phosphorylase, putative | Plasmodium falciparum 3D7 | Kd | 0.0009 | AID977611 |
Chain B, uridine phosphorylase, putative | Plasmodium falciparum 3D7 | Kd | 0.0009 | AID977611 |
Chain A, Uridine phosphorylase putative | Plasmodium falciparum 3D7 | Kd | 0.0009 | AID977611 |
Chain B, Uridine phosphorylase putative | Plasmodium falciparum 3D7 | Kd | 0.0009 | AID977611 |
Chain A, Purine nucleoside phosphorylase | Homo sapiens (human) | Kd | 0.0009 | AID977611 |
Purine nucleoside phosphorylase | Homo sapiens (human) | Kd | 0.0001 | AID536621 |
Purine nucleoside phosphorylase | Bos taurus (cattle) | Kd | 0.0000 | AID694066 |
Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
---|---|---|---|---|
Purine nucleoside phosphorylase | Bos taurus (cattle) | Kieq | 0.0000 | AID694063 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1578787 | Antimalarial 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 countin | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 ISSN: 1520-4804 | Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues. |
AID409913 | Initial binding affinity to wild type human PNP | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405 | Immucillins in custom catalytic-site cavities. |
AID272825 | Inhibition of DNA synthesis in CCRF-CEM cells assessed as inhibition of [3H]Thymidine incorporation upto 100 nM | 2006 | Journal 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. |
AID536621 | Inhibition of human PNP | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 ISSN: 1768-3254 | Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase. |
AID409921 | Ratio of relative binding Km/Ki for wild type human PNP to relative binding affinity Km/Ki for human PNP His257Gly mutant | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405 | Immucillins in custom catalytic-site cavities. |
AID272833 | Antiproliferative activity against CCRF-CEM cells | 2006 | Journal 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. |
AID462377 | Inhibition of calf spleen PNP assessed as inhibition of 7-methylguanosine phosphorolysis after 50 mins by spectrophotometry in presence of 50 mM inorganic phosphate | 2010 | Bioorganic & 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. |
AID409920 | Ratio of Km for human PNP His257Gly mutant to Ki for human PNP His257Gly mutant relative to inosine | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405 | Immucillins in custom catalytic-site cavities. |
AID523342 | Antiparasitic activity against chloroquine-sensitive Plasmodium falciparum Ghana assessed as reduction in parasite growth after 3 days by fluorimetry | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID523341 | Antileishmanial activity against Leishmania infantum MHOM/MA/67/ITMAP263 intracellular amastigotes assessed as reduction in parasite growth after 3 days by fluorometrically | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID523340 | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen CL2 s-galactosidase strain assessed as reduction in parasite growth after 3 days by fluorometrically | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID164739 | Inhibitory activity of compound against bovine purine nucleoside phosphorylase (PNP) | 2003 | Journal 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. |
AID164742 | Dissociation constant against Human Purine Nucleoside Phosphorylase was reported | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 ISSN: 0022-2623 | Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase. |
AID1571176 | Inhibition of human PNP using inosine as substrate by xanthine oxidase coupled assay | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 ISSN: 2040-2511 | The transition to magic bullets - transition state analogue drug design. |
AID164938 | Inhibitory activity of compound against human purine nucleoside phosphorylase (PNP) | 2004 | Journal 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. |
AID1571177 | Inhibition of bovine spleen PNP assessed as dissociation half life using inosine as substrate by xanthine oxidase coupled assay | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 ISSN: 2040-2511 | The transition to magic bullets - transition state analogue drug design. |
AID409914 | Equilibrium binding affinity to wild type human PNP | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405 | Immucillins in custom catalytic-site cavities. |
AID409916 | Ratio of Km for wild type human PNP to Ki for wild type human PNP relative to inosine | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405 | Immucillins in custom catalytic-site cavities. |
AID272824 | Inhibition of human dCK activity | 2006 | Journal 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. |
AID523326 | Inhibition of Trypanosoma brucei brucei Inosine guanosine nucleoside hydrolase | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID523324 | Inhibition of Trypanosoma vivax Inosine-adenosine-guanosine-nucleoside hydrolase | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID694066 | Binding affinity to calf recombinant PNP expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry | 2012 | Bioorganic & 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. |
AID1578784 | Inhibition of human PNP assessed as inhibitor constant for enzyme-inhibitor-substrate complex formation | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 ISSN: 1520-4804 | Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues. |
AID1578782 | Inhibition of Plasmodium falciparum His-tagged PNP assessed as inhibitor constant for enzyme-inhibitor-substrate complex formation | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 ISSN: 1520-4804 | Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues. |
AID523328 | Antitrypanosomal activity against suramin sensitive Trypanosoma brucei brucei Lister 427 assessed as reduction in parasite growth after 3 days by fluorometrically | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID410191 | Initial binding affinity to human PNP His257Gly mutant | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405 | Immucillins in custom catalytic-site cavities. |
AID1578783 | Inhibition of human PNP assessed as inhibitor constant for enzyme-inhibitor complex formation | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 ISSN: 1520-4804 | Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues. |
AID1571178 | Oral bioavailability in mouse | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 ISSN: 2040-2511 | The transition to magic bullets - transition state analogue drug design. |
AID164744 | Inhibitory activity of compound against human purine nucleoside phosphorylase (PNP) | 2003 | Journal 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. |
AID272823 | Inhibition of human PNP activity | 2006 | Journal 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. |
AID92759 | Inhibitory activity of compound against inosine-uridine nucleoside hydrolase (IU-NH) from crithidia fasciculata | 2003 | Journal 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. |
AID92758 | Inhibitory activity of compound against perine-specific inosine-adenosine-guanosine nucleoside hydrolase (IAG-NH) from Trypanosoma brucei | 2003 | Journal 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. |
AID164604 | Rate constant of compound was determined for interaction with bovine purine nucleoside phosphorylase (PNP) | 2003 | Journal 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. |
AID1571175 | Inhibition of bovine spleen PNP using inosine as substrate by xanthine oxidase coupled assay | 2018 | MedChemComm, Dec-01, Volume: 9, Issue:12 ISSN: 2040-2511 | The transition to magic bullets - transition state analogue drug design. |
AID164930 | Equilibrium dissociation constant determined against human purine nucleoside phosphorylase (PNP) after slow-onset inhibition | 2003 | Journal 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. |
AID409918 | Equilibrium binding affinity to human PNP His257Gly mutant | 2008 | Bioorganic & medicinal chemistry letters, Nov-15, Volume: 18, Issue:22 ISSN: 1464-3405 | Immucillins in custom catalytic-site cavities. |
AID694063 | Inhibition of bovine PNP using 7-methylguanosine as substrate by spectrophotometric based coupled assay | 2012 | Bioorganic & 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. |
AID523327 | Inhibition of human purine nucleoside phosphorylase | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID523329 | Cytotoxicity against human MRC5 SV2 cells after 48 hrs | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID523325 | Inhibition of Trypanosoma brucei brucei inosine-adenosine-guanosine nucleoside hydrolase (IAG-NH) | 2010 | Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5 ISSN: 1098-6596 | Evaluation of nucleoside hydrolase inhibitors for treatment of African trypanosomiasis. |
AID1578781 | Inhibition of Plasmodium falciparum His-tagged PNP assessed as inhibitor constant for enzyme-inhibitor complex formation | 2019 | Journal of medicinal chemistry, 09-26, Volume: 62, Issue:18 ISSN: 1520-4804 | Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues. |
AID164928 | Inhibition of human purine nucleoside phosphorylase; Initial rate. | 2003 | Journal 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. |
AID536622 | Inhibition of Plasmodium falciparum PNP expressed in Escherichia coli BL21(DE3) cells by spectrophotometry | 2010 | European journal of medicinal chemistry, Nov, Volume: 45, Issue:11 ISSN: 1768-3254 | Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase. |
AID164740 | Rate constant of compound was determined for interaction with human purine nucleoside phosphorylase (PNP) | 2003 | Journal 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. |
AID164741 | Binding affinity towards Human Purine Nucleoside Phosphorylase was reported | 2003 | Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24 ISSN: 0022-2623 | Synthesis of second-generation transition state analogues of human purine nucleoside phosphorylase. |
AID371442 | Inhibition of human PNP by xanthine-oxidase coupled assay | 2009 | Journal 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. |
AID424677 | Inhibition of human purine nucleoside phosphorylase | 2009 | Bioorganic & 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. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2006 | Journal 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. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2006 | Journal 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. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS 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. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
AID1346173 | Human purine nucleoside phosphorylase (Nucleoside synthesis and metabolism) | 1998 | Biochemistry, Jun-16, Volume: 37, Issue:24 ISSN: 0006-2960 | One-third-the-sites transition-state inhibitors for purine nucleoside phosphorylase. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2001 | Biochemistry, 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. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2001 | Biochemistry, 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. |
AID977610 | Experimentally measured binding affinity data (Ki) for protein-ligand complexes derived from PDB | 2001 | Biochemistry, Jan-30, Volume: 40, Issue:4 ISSN: 0006-2960 | Transition state structure of purine nucleoside phosphorylase and principles of atomic motion in enzymatic catalysis. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2001 | Biochemistry, Jan-30, Volume: 40, Issue:4 ISSN: 0006-2960 | Transition state structure of purine nucleoside phosphorylase and principles of atomic motion in enzymatic catalysis. |
AID977611 | Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB | 2004 | The 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. |
AID1811 | Experimentally measured binding affinity data derived from PDB | 2004 | The 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. |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 3 (2.78) | 18.2507 |
2000's | 65 (60.19) | 29.6817 |
2010's | 33 (30.56) | 24.3611 |
2020's | 7 (6.48) | 2.80 |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 7 (6.42%) | 5.53% |
Reviews | 25 (22.94%) | 6.00% |
Case Studies | 2 (1.83%) | 4.05% |
Observational | 1 (0.92%) | 0.25% |
Other | 74 (67.89%) | 84.16% |
Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
---|---|---|---|---|---|---|---|---|---|---|---|---|
Acute Disease | 0 | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Acute Lymphoid Leukemia | 0 | 2007 | 2016 | 12.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Acute Myelogenous Leukemia | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Adverse Drug Event | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
African Sleeping Sickness | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Anaplastic Large-Cell Lymphoma | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
ATLL | 0 | 2003 | 2010 | 17.7 | low | 0 | 0 | 0 | 3 | 0 | 0 | |
B-Cell Chronic Lymphocytic Leukemia | 0 | 2006 | 2020 | 13.7 | low | 1 | 0 | 0 | 5 | 1 | 0 | |
B-Cell Leukemia | 0 | 2007 | 2007 | 17.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
B-Cell Lymphoma | 0 | 2012 | 2014 | 11.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
B-Cell Prolymphocytic Leukemia | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Benign Neoplasms | 0 | 2006 | 2010 | 16.0 | low | 0 | 0 | 0 | 2 | 0 | 0 | |
Black Fever | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
Brill-Symmers Disease | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Cancer of Skin | 0 | 2007 | 2017 | 12.6 | low | 2 | 0 | 0 | 2 | 3 | 0 | |
Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Cutaneous T-Cell Lymphoma | 0 | 2007 | 2017 | 12.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Diffuse Large B-Cell Lymphoma | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Disease Models, Animal | 0 | 2015 | 2020 | 6.5 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
Drug-Related Side Effects and Adverse Reactions | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Erythroderma, Sezary | 0 | 2007 | 2014 | 14.7 | low | 1 | 0 | 0 | 2 | 1 | 0 | |
Exanthem | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Exanthema | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Experimental Leukemia | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Germinoblastoma | 0 | 2006 | 2012 | 15.0 | low | 1 | 0 | 0 | 1 | 1 | 0 | |
Graft vs Host Disease | 0 | 2002 | 2002 | 22.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Graft-Versus-Host Disease | 0 | 2002 | 2002 | 22.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Hematologic Malignancies | 0 | 2008 | 2011 | 14.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Hematologic Neoplasms | 0 | 2008 | 2011 | 14.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Infections, Plasmodium | 0 | 2004 | 2019 | 12.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Leishmaniasis, American | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Leishmaniasis, Cutaneous | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Leishmaniasis, Visceral | 0 | 2015 | 2015 | 9.0 | low | 0 | 0 | 0 | 0 | 2 | 0 | |
Leucocythaemia | 0 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Leukemia | 1 | 2006 | 2006 | 18.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Leukemia-Lymphoma, Adult T-Cell | 0 | 2003 | 2010 | 17.7 | low | 0 | 0 | 0 | 3 | 0 | 0 | |
Leukemia, Lymphoblastic, Acute, T Cell | 0 | 2007 | 2014 | 13.3 | low | 0 | 0 | 0 | 1 | 2 | 0 | |
Leukemia, Lymphocytic | 0 | 2005 | 2005 | 19.0 | low | 1 | 0 | 0 | 1 | 0 | 0 | |
Leukemia, Lymphocytic, Chronic, B-Cell | 1 | 2006 | 2020 | 13.7 | low | 1 | 0 | 0 | 5 | 1 | 0 | |
Leukemia, Lymphocytic, T Cell | 0 | 2002 | 2008 | 18.3 | low | 0 | 0 | 0 | 3 | 0 | 0 | |
Leukemia, Lymphoid | 0 | 2005 | 2005 | 19.0 | low | 1 | 0 | 0 | 1 | 0 | 0 | |
Leukemia, Myeloid, Acute | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Leukemia, Pre-B-Cell | 0 | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Leukemia, Prolymphocytic, B-Cell | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Leukemia, T-Cell | 0 | 2002 | 2008 | 18.3 | low | 0 | 0 | 0 | 3 | 0 | 0 | |
Local Neoplasm Recurrence | 0 | 2007 | 2007 | 17.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Lymphocytopenia | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Lymphoma | 1 | 2006 | 2012 | 15.0 | low | 1 | 0 | 0 | 1 | 1 | 0 | |
Lymphoma, B-Cell | 0 | 2012 | 2014 | 11.0 | low | 1 | 0 | 0 | 0 | 2 | 0 | |
Lymphoma, Follicular | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Lymphoma, Large B-Cell, Diffuse | 0 | 2008 | 2008 | 16.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Lymphoma, Large-Cell, Anaplastic | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Lymphoma, T Cell, Peripheral | 0 | 2008 | 2022 | 8.5 | low | 2 | 0 | 0 | 2 | 2 | 2 | |
Lymphoma, T-Cell | 0 | 2006 | 2012 | 15.0 | low | 1 | 0 | 0 | 1 | 1 | 0 | |
Lymphoma, T-Cell, Cutaneous | 1 | 2007 | 2017 | 12.0 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Lymphoma, T-Cell, Peripheral | 0 | 2008 | 2022 | 8.5 | low | 2 | 0 | 0 | 2 | 2 | 2 | |
Lymphopenia | 0 | 2012 | 2012 | 12.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Malaria | 0 | 2004 | 2019 | 12.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Malaria, Falciparum | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Malignant Melanoma | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Melanoma | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Mycosis Fungoides | 0 | 2007 | 2014 | 13.0 | low | 2 | 0 | 0 | 1 | 2 | 0 | |
Neoplasms | 0 | 2006 | 2010 | 16.0 | low | 0 | 0 | 0 | 2 | 0 | 0 | |
Parodontosis | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Periodontal Diseases | 0 | 2013 | 2013 | 11.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Plasmodium falciparum Malaria | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Precursor B-Cell Lymphoblastic Leukemia-Lymphoma | 0 | 2013 | 2013 | 11.0 | low | 1 | 0 | 0 | 0 | 1 | 0 | |
Precursor Cell Lymphoblastic Leukemia-Lymphoma | 0 | 2007 | 2016 | 12.5 | low | 0 | 0 | 0 | 1 | 1 | 0 | |
Precursor T-Cell Lymphoblastic Leukemia-Lymphoma | 0 | 2007 | 2014 | 13.3 | low | 0 | 0 | 0 | 1 | 2 | 0 | |
Recrudescence | 0 | 2012 | 2019 | 8.3 | low | 2 | 0 | 0 | 0 | 3 | 0 | |
Sensitivity and Specificity | 0 | 2011 | 2011 | 13.0 | low | 0 | 0 | 0 | 0 | 1 | 0 | |
Sezary Syndrome | 0 | 2007 | 2014 | 14.7 | low | 1 | 0 | 0 | 2 | 1 | 0 | |
Skin Neoplasms | 0 | 2007 | 2017 | 12.6 | low | 2 | 0 | 0 | 2 | 3 | 0 | |
T-Cell Lymphoma | 0 | 2006 | 2012 | 15.0 | low | 1 | 0 | 0 | 1 | 1 | 0 | |
Trypanosomiasis, African | 0 | 2010 | 2010 | 14.0 | low | 0 | 0 | 0 | 1 | 0 | 0 | |
Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | low | 0 | 0 | 0 | 0 | 1 | 0 |
Article | Year |
---|---|
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 |
Article | Year |
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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 |
Article | Year |
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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 |