Page last updated: 2024-12-08

aphidicolin

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Description

Aphidicolin: An antiviral antibiotic produced by Cephalosporium aphidicola and other fungi. It inhibits the growth of eukaryotic cells and certain animal viruses by selectively inhibiting the cellular replication of DNA polymerase II or the viral-induced DNA polymerases. The drug may be useful for controlling excessive cell proliferation in patients with cancer, psoriasis or other dermatitis with little or no adverse effect upon non-multiplying cells. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

aphidicolin : A tetracyclic diterpenoid that has an tetradecahydro-8,11a-methanocyclohepta[a]naphthalene skeleton with two hydroxymethyl substituents at positions 4 and 9, two methyl substituents at positions 4 and 11b and two hydroxy substituents at positions 3 and 9. An antibiotic with antiviral and antimitotical properties. Aphidicolin is a reversible inhibitor of eukaryotic nuclear DNA replication. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID457964
CHEMBL ID29711
CHEBI ID2766
SCHEMBL ID183956
MeSH IDM0025305

Synonyms (90)

Synonym
nsc-234714
CBIOL_001873
ccris 1783
8,11a-methano-11ah-cyclohepta(a)naphthalene-4,9-dimethanol, tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-, (3r-(3-alpha,4-alpha,4a-alpha,6a-beta,8-beta,9-beta,11a-beta,11b-beta))-
nsc 234714
9,15-cyclo-c,18-dinor-14,15-secoandrostane-4,17-dimethanol, 3,17-dihydroxy-4-methyl-, (3alpha,4alpha,5alpha,17alpha)-
ici-69653
brn 4689958
ACON1_000511
BCBCMAP01_000163
c20h34o4
BIO1_000159
BIO1_001137
BIO2_000638
BIO2_000158
BIO1_000648
NSC234714 ,
8,11a-methano-11ah-cyclohepta[a]naphthalene-4,9-dimethanol, tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-, (3s,4r,4ar,6as,8r,9r,11as,11bs)-
ici 69653
IDI1_033908
BSPBIO_001438
ACON0_000080
MEGXM0_000277
38966-21-1
aphidicolin
NCGC00023142-03
smr000058538
MLS000069677 ,
KBIOGR_000158
KBIO3_000316
KBIO2_000158
KBIO2_005294
KBIO2_002726
KBIOSS_000158
KBIO3_000315
SMP1_000025
NCGC00023142-04
NCGC00023142-05
(3r,4r,4ar,6as,8r,9r,11as,11bs)-4,9-bis(hydroxymethyl)-4,11b-dimethyltetradecahydro-8,11a-methanocyclohepta[a]naphthalene-3,9-diol
aphidicolin from nigrospora sphaerica, >=98% (hplc), powder
HMS1989H20
4B15B386-8738-48FE-80DB-5BA3406098DD
6,13-di(hydroxymethyl)-2,6-dimethyl-(1s,2s,5r,6r,7r,10s,12r,13r)-tetracyclo[10.3.1.01,10.02,7]hexadecane-5,13-diol(aphidicolin)
cid_457964
aphidicholin
bdbm50090910
6,13-di(hydroxymethyl)-2,6-dimethyl-(1s,2s,5r,6r,7r)-tetracyclo[10.3.1.01,10.02,7]hexadecane-5,13-diol
3alpha,16,17,18-tetrahydroxyaphidicolone
6,13-di(hydroxymethyl)-2,6-dimethyl-(1s,2s,5r,6r,7r,10s,12r,13r)-tetracyclo[10.3.1.01,10.02,7]hexadecane-5,13-diol (aphidicolin)
CHEMBL29711 ,
chebi:2766 ,
HMS1791H20
HMS1361H20
unii-192tj6pp19
192tj6pp19 ,
aphidicolin from nigrospora sphaerica
(3alpha,4alpha,5alpha,17alpha)-3,17-dihydroxy-4-methyl-9,15-cyclo-c,18-dinor-14,15-secoandrostane-4,17-dimethanol
aphidocolin
8,11|a-methano-11ah-cyclohepta[a]naphthalene-4,9-dimethanol,tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-, (3r,4r,4ar,6as,8r,9r,11as,11bs)-
CCG-208640
SCHEMBL183956
(+/-)-aphidicolin
8,11a-methano-11ah-cyclohepta(a)naphthalene-4,9-dimethanol, tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-, (3r,4r,4ar,6as,8r,9r,11as,11bs)-rel-
aphidicolin, (+/-)-
69926-98-3
unii-6b3f8qw8tu
6b3f8qw8tu ,
2ze ,
9,15-cyclo-c,18-dinor-14,15-secoandrostane-4,17-dimethanol, 3,17-dihydroxy-4-methyl-, (3.alpha.,4.alpha.,5.alpha.,17.alpha.)-
aphidicolin [mi]
(+)-aphidicolin
8,11a-methano-11ah-cyclohepta(a)naphthalene-4,9-dimethanol, tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-, (3r,4r,4ar,6as,8r,9r,11as,11bs)-
HB3690
HMS3402H20
OPERA_ID_1321
DTXSID5036711
(1s,2s,5r,6r,7r,10s,12r,13r)-6,13-bis(hydroxymethyl)-2,6-dimethyltetracyclo[10.3.1.0[1,10].0[2,7]]hexadecane-5,13-diol
aphidicolin, analytical standard
(3r,4r,4ar,6as,8r,9r,11as,11bs)-tetradecahydro-3,9-dihydroxy-4,11b-dimethyl-8,11a-methano-11ah-cyclohepta[a]naphthalene-4,9-dimethanol
AKOS027470273
NCGC00023142-06
ne-3,9-diol
(3r,4r,4ar,6as,8r,9r,11as,11bs)-4,9-bis(hydroxymethyl)-4,11b-dimethyltetradecahydro-8,11a-methanocyclohepta[a]naphthale
aphidicolin - cas 38966-21-1
HY-N6733
CS-0033151
Q27453425
rel-(3r,4r,4ar,6as,8r,9r,11as,11bs)-4,9-bis(hydroxymethyl)-4,11b-dimethyltetradecahydro-8,11a-methanocyclohepta[a]naphthalene-3,9-diol
AT25347
BA162709

Research Excerpts

Overview

Aphidicolin is a potent antitumor and apoptotic agent against human cervical carcinoma. Its effects are mediated via chromatin condensation and mitochondrial membrane potential loss. Aphidicol inhibits both the DNA polymerase and 3'-5'-exonuclease activities of delta.

ExcerptReferenceRelevance
"Aphidicolin is a potent antitumor and apoptotic agent against human cervical carcinoma and its effects are mediated via chromatin condensation and mitochondrial membrane potential loss."( Inhibitory effect of Aphidicolin - a tetracyclic diterpene - on the proliferation and apoptotic induction in human cervical cancer (HeLa) cells.
Wang, DS; Yu, EY; Zhao, RY,
)
1.89
"Aphidicolin, considered to be a specific inhibitor of DNA polymerase alpha, inhibits both the DNA polymerase and 3'-5'-exonuclease activities of delta."( DNA polymerase delta: one polypeptide, two activities.
Byrnes, JJ; Goscin, LP, 1982
)
0.99
"Aphidicolin is a potent inhibitor of both host cell DNA polymerase alpha and herpes simplex virus (HSV)-induced DNA polymerase but has no effect on DNA polymerases beta and gamma of host cells. "( Involvement of DNA polymerase alpha in host cell reactivation of UV-irradiated herpes simplex virus.
Maeno, K; Nishiyama, Y; Yoshida, S, 1984
)
1.71
"Aphidicolin is a selective inhibitor of eukaryotic DNA polymerase alpha (Ikegami et al."( Specific inhibitors of eukaryotic DNA synthesis and DNA polymerase alpha, 3-deoxyaphidicolin and aphidicolin-17-monoacetate.
Haraguchi, T; Ichihara, A; Nagano, H; Oguro, M; Sakamura, S, 1983
)
1.21
"Aphidicolin is a more useful reagent than hydroxyurea and thymidine because it does not affect cell viability or "S" phase duration and does not interfere with the synthesis of dNTPs or DNA polymerases."( Synchronization of HeLa cell cultures by inhibition of DNA polymerase alpha with aphidicolin.
Koch, G; Kruppa, J; Miller, AO; Miller-Faurès, A; Pedrali-Noy, G; Spadari, S, 1980
)
1.21
"Aphidicolin is a specific inhibitor of DNA polymerase alpha. "( Aphidicolin: an inhibitor of DNA repair in human fibroblasts.
Waters, R, 1981
)
3.15
"Aphidicolin is a specific inhibitor of DNA polymerase alpha and blocks DNA synthesis in vivo. "( Isolation and characterization of a UV-sensitive hypermutable aphidicolin-resistant Chinese hamster cell line.
Boezi, JA; Chang, CC; Glatzer, L; Liu, PK; Sabourin, CL; Trosko, JE; Warren, ST, 1981
)
1.95
"Aphidicolin is a selective inhibitor of DNA polymerase alpha. "( Aphidicolin inhibits DNA synthesis by DNA polymerase alpha and isolated nuclei by a similar mechanism.
Krokan, H; Krokan, RH; Wist, E, 1981
)
3.15
"Aphidicolin is a highly specific inhibitor of DNA polymerase alpha and has been most useful for assessing the role of this enzyme in various replication processes (J. "( Resistance of adenoviral DNA replication to aphidicolin is dependent on the 72-kilodalton DNA-binding protein.
Foster, DA; Hantzopoulos, P; Zubay, G, 1982
)
1.97
"Aphidicolin is a tetracyclic diterpene antibiotic which kills human neuroblastoma cells (NB) in vitro while it has no significant effect on the viability of different human cell types including normal embryonal cells. "( Increased efficacy of aphidicolin killing of human neuroblastoma cells in vitro by encapsulation in liposomes.
Cinatl, J; Doerr, HW; Gümbel, HO; Hernáiz Driever, P; Kornhuber, B; Rabenau, H; Rückert, DG, 1997
)
2.05
"Aphidicolin is a fungal derived tetracyclic diterpene antibiotic. "( Aphidicolin glycinate inhibits human neuroblastoma cell growth in vivo.
Bertels, S; Bindseil, K; Cinatl, J; Doerr, HW; Driever, PH; Jas, G; Kotchetkov, R; Pouckova, P; Rabenau, HF; Schwabe, D; Siems, K,
)
3.02
"Aphidicolin is an inhibitor of cellular DNA polymerase alpha, and it halts progression of the cell cycle at the G1/S border or early S phase."( Antisense oligonucleotide complementary to the BamHI-H gene family of Marek's disease virus induced growth arrest of MDCC-MSB1 cells in the S-phase.
Akaike, H; Arai, S; Hayashi, M; Kawamura, T; Okui, T, 1999
)
1.02
"Aphidicolin is a tetracyclic diterpene antibiotic which is known to inhibit the growth of eucaryotic cells by reversible binding to DNA polymerase alpha without significant effect on cell viability in most common human cell lines. "( Aphidicolin selectively kills neuroblastoma cells in vitro.
Cinatl, J; Doerr, HW; Kornhuber, B; Mainke, M; Rabenau, H; Steigmann, G; Weissflog, A, 1992
)
3.17
"Aphidicolin is a specific inhibitor of DNA polymerase-alpha and -delta from eukaryotic cells. "( Aphidicolin hypersensitive mutant of Chinese hamster V79 fibroblasts that underproduces DNA polymerase-alpha antigen.
Goudreau, B; Hsu, GS; Liu, PK, 1989
)
3.16
"Aphidicolin is a specific inhibitor of DNA polymerase alpha, the enzyme responsible for the replicative synthesis of DNA."( Prevention of dacarbazine damage of human neoplastic cell DNA by aphidicolin.
Lohn, S; Lönn, U, 1987
)
1.23
"Aphidicolin was shown to be a more potent inhibitor of DNA replication than of DNA polymerase alpha or delta activity."( Identification of DNA polymerase delta in CV-1 cells: studies implicating both DNA polymerase delta and DNA polymerase alpha in DNA replication.
Byrnes, JJ; Hammond, RA; Miller, MR, 1987
)
0.99
"Aphidicolin is an inhibitor of DNA polymerase alpha and blocks nuclear DNA replication without interfering with mitochondrial DNA synthesis. "( Kinetics of DNA replication in C3H 10T1/2 cells synchronized by aphidicolin.
Cordeiro-Stone, M; Kaufman, DG, 1985
)
1.95

Effects

Aphidicolin has no effect on actin-microfilaments. serum deprivation induces the terminal pattern of filaments in many early cells.

ExcerptReferenceRelevance
"Aphidicolin has no effect on actin-microfilaments whereas serum deprivation induces the terminal pattern of filaments in many early cells."( Cell morphology, cell filaments and cell death during in vitro ageing: aphidicolin and serum deprivation effects on mouse diploid fibroblasts (a correlated scanning electron microscope and immunocytochemical study).
De Vos, L; Van Gansen, P, 1982
)
1.22
"Aphidicolin has thus proved extremely useful in elucidating the functional role of DNA polymerase alpha in nuclear DNA replication, of DNA polymerase gamma in mitochondrial DNA synthesis and both DNA polymerases beta and alpha in DNA repair synthesis."( Control of cell division by aphidicolin without adverse effects upon resting cells.
Ciarrocchi, G; Falaschi, A; Focher, F; Koch, G; Pedrali-Noy, G; Sala, F; Spadari, S, 1985
)
1.28

Actions

Aphidicolin might increase the occurrence of breakage events at FRA6E by prolonging the time interval separating the replication of early and late replication domains. When aphidicol was used to inhibit repair mediated by DNA polymerase alpha, both normal control and Fanconi anemia fibroblasts showed significantly more chromosome breakage.

ExcerptReferenceRelevance
"Aphidicolin might increase the occurrence of breakage events at FRA6E by prolonging the time interval separating the replication of early and late replication domains."( Replication dynamics at common fragile site FRA6E.
Bensimon, A; Matricardi, L; Palumbo, E; Russo, A; Tosoni, E, 2010
)
1.08
"Aphidicolin did not inhibit exonuclease activity on single-stranded DNA; however, activity on double-stranded DNA was partially inhibited."( DNA polymerase epsilon: aphidicolin inhibition and the relationship between polymerase and exonuclease activity.
Cheng, CH; Kuchta, RD, 1993
)
1.31
"Aphidicolin can inhibit this DNA repair."( Aphidicolin markedly increases the in vitro sensitivity to ara-C of blast cells from patients with AML.
Elgie, AW; Sargent, JM; Taylor, CG; Williamson, CJ, 1999
)
2.47
"Aphidicolin, known to inhibit both the DNA synthesis and 3' to 5' exonuclease activities of polymerases delta and epsilon, reduced appearance of 3' to 5' excision tracts roughly 4-fold at 90 microm but had no effect on 5' to 3' excision."( Mismatch repair in human nuclear extracts. Time courses and ATP requirements for kinetically distinguishable steps leading to tightly controlled 5' to 3' and aphidicolin-sensitive 3' to 5' mispair-provoked excision.
Hays, JB; Wang, H, 2002
)
1.23
"When aphidicolin was used to inhibit repair mediated by DNA polymerase alpha, both normal control and Fanconi anemia fibroblasts showed significantly more chromosome breakage than was produced by bleomycin alone, but there was no increase in the amount of breakage seen in the N syndrome fibroblasts over that seen with bleomycin alone."( DNA polymerase alpha defect in the N syndrome.
Floy, KM; Hess, RO; Meisner, LF, 1990
)
0.73
"Aphidicolin could inhibit EBV DNA polymerase competitively with respect to dATP and dCTP and noncompetitively with respect to dGTP and dTTP; whereas 5'-GMP was a noncompetitive inhibitor with respect to all four dNTPs."( Interaction of Epstein-Barr virus DNA polymerase with aphidicolin, phosphonoformate and 5'-GMP.
Cheng, YC; Li, JS, 1988
)
1.24
"Aphidicolin was shown to inhibit DNA synthesis almost instantly and completely."( DNA synthesis and the control of embryonic gene expression in C. elegans.
Edgar, LG; McGhee, JD, 1988
)
1

Treatment

Aphidicolin treatment from the 32-cell stage affected, but did not completely suppress, the expression of lacZ. Patients and unaffected members in neuroblastoma families showed hypersensitivity to aphidicol. In aphidIColin-treated cells, the replication fork is stopped and there is no formation of DNA replication intermediates.

ExcerptReferenceRelevance
"In aphidicolin-treated cells, the nuclear length was correlated with the cell length."( Aphidicolin-induced nuclear elongation in tobacco BY-2 cells.
Kitamoto, K; Yasuhara, H, 2014
)
2.36
"Aphidicolin treatment from the 32-cell stage affected, but did not completely suppress, the expression of lacZ."( Mechanism of DNA replication-dependent transcriptional activation of the acetylcholinesterase gene in the Ciona intestinalis embryo.
Fujiwara, S; Kataoka, Y; Mishina, R, 2009
)
1.07
"In aphidicolin treated cultures, the patients and unaffected members in neuroblastoma families, showed hypersensitivity to aphidicolin, as evidenced by the significant increase in percentage of aberration/cell (ab/c) and damaged cells (dc), over that of controls (P < 0.01)."( Expression of folate sensitive and aphidicolin induced chromosomal fragile sites in familial neuroblastoma.
Ankathil, R; Krishnan Nair, M; Kusumakumary, P; Priyakumary, T, 2002
)
1.11
"Aphidicolin treatment revealed that eight blastomeres were specific to pigment cell lineage after the eighth cleavage, one cell cycle earlier than that in well-known sea urchins."( Behavior and differentiation process of pigment cells in a tropical sea urchin Echinometra mathaei.
Kominami, T; Takata, H,
)
0.85
"Aphidicolin treatment was the most effective, with almost 80% of the cells expressing green fluorescent protein from a silent ES."( Bloodstream form-specific up-regulation of silent vsg expression sites and procyclin in Trypanosoma brucei after inhibition of DNA synthesis or DNA damage.
Rudenko, G; Sheader, K; te Vruchte, D, 2004
)
1.04
"In aphidicolin-treated cells, the replication fork is stopped and there is no formation of DNA replication intermediates."( Aphidicolin inhibits the synthesis and joining of short DNA fragments but not the union of 10-kilobase DNA replication intermediates.
Lönn, S; Lönn, U, 1983
)
2.22
"Aphidicolin treatment reversibly blocked cytokine-stimulated Lin-/Sca+ cells at G1/S boundary, allowing their tight synchrony as they progress through first S phase and enter into second G1."( Cell cycle analysis and synchronization of pluripotent hematopoietic progenitor stem cells.
Hsieh, CC; Pang, L; Quesenberry, PJ; Reddy, GP; Tiarks, CY; Wuu, J, 1997
)
1.02
"Aphidicolin treatment caused a general lengthening of the G-strands and a large increase in C strand heterogeneity."( Coordinate regulation of G- and C strand length during new telomere synthesis.
Fan, X; Price, CM, 1997
)
1.02
"Aphidicolin treatment fully protected AA8 cells from camptothecin cytotoxicity."( The CHO XRCC1 mutant, EM9, deficient in DNA ligase III activity, exhibits hypersensitivity to camptothecin independent of DNA replication.
Anderson, M; Barrows, LR; D'Arpa, P; Holden, JA, 1998
)
1.02
"Aphidicolin treatment led to an accumulation of 81.9 +/- 4.9% of cells at the G1/S transition."( Cell cycle synchronization of porcine fetal fibroblasts: effects of serum deprivation and reversible cell cycle inhibitors.
Anger, M; Carnwath, JW; Kues, WA; Motlik, J; Niemann, H; Paul, D, 2000
)
1.03
"Aphidicolin treatment revealed that 10-15 pigment founder cells were formed."( Process of pigment cell specification in the sand dollar, Scaphechinus mirabilis.
Kominami, T; Takata, H, 2002
)
1.04
"Aphidicolin pretreated and irradiated cells showed a reduction in PLD-recovery, dependent on aphidicolin concentration and duration of pretreatment."( Effect of aphidicolin on DNA synthesis, PLD-recovery and DNA repair of human diploid fibroblasts.
Baumstark-Khan, C, 1992
)
1.41
"In aphidicolin-treated V79 cells, the increase in the dCTP level due to exogenous cytidine was almost completely blocked; caffeine also substantially overcame this effect of aphidicolin."( Abrogation of the effects of aphidicolin on NIH3T3 and V79 cells by caffeine.
Das, SK, 1987
)
1.08
"Treatment with aphidicolin, a known fragile site inducer, indicates that the hypoxia inducible fragile site is a common fragile site."( Tumor hypoxia: Impact on gene amplification in glioblastoma.
Fischer, U; Mayer, J; Meese, E; Mehraein, Y; Radermacher, J, 2008
)
0.69
"Treatment by aphidicolin and HU resulted in phosphorylation of Chk1, while HU, but not aphidicolin, induced focalization of gamma-H2AX and RPA."( Comparison of checkpoint responses triggered by DNA polymerase inhibition versus DNA damaging agents.
Kuo, SR; Liu, JS; Melendy, T, 2003
)
0.67
"Treatment with aphidicolin at 9-18 hpi arrested DNA replication without affecting formation of the pronuclei or embryo development."( Effect of microinjection time during postfertilization S-phase on bovine embryonic development.
Gagné, M; Pothier, F; Sirard, MA, 1995
)
0.63
"The treatment with aphidicolin at 5 x 10(-6) M concentration, which completely inhibited DNA synthesis and cell growth, induced morphological differentiation of small mononuclear cells to elongated, multinucleated (myotube-like) structures."( Aphidicolin induces myogenic differentiation in the human rhabdomyosarcoma cell line KFR.
Cinatl, J; Doerr, HW; Driever, PH; Kornhuber, B; Novak, M; Rabenau, H; Stefanik, M, 1994
)
2.05
"When treated with aphidicolin during S phase, luciferase activity decreased."( Differential response of the human cyclin B1 promoter to inhibitors of the cell cycle in NIH3T3 cells.
Butler, R; Katula, KS; Khan, AS; Nuckolls, FJ, 1998
)
0.62
"Treatment with aphidicolin resulted in a S phase block in which more than 85% of the cells showed S phase chromosomes."( Cell cycle analysis and synchronization of the Xenopus cell line XL2.
Arlot-Bonnemains, Y; Chartrain, I; Philippe, M; Uzbekov, R, 1998
)
0.64

Toxicity

ExcerptReferenceRelevance
" At levels of the drug which are toxic to the cell, these breaks are long-lived, and still measurable 24 hr after treatment."( Camptothecin cytotoxicity in mammalian cells is associated with the induction of persistent double strand breaks in replicating DNA.
Johnson, RT; Ryan, AJ; Squires, S; Strutt, HL, 1991
)
0.28
" The mechanism of action of this drug suggests in fact that it may be useful for controlling excessive cell proliferation in patients with cancer, psoriasis or other dermatitis with little or no adverse effect upon non-multiplying cells."( Control of cell division by aphidicolin without adverse effects upon resting cells.
Ciarrocchi, G; Falaschi, A; Focher, F; Koch, G; Pedrali-Noy, G; Sala, F; Spadari, S, 1985
)
0.56
" Irreversible DNA double-strand breaks are produced during DNA synthesis in the presence of camptothecin, suggesting that this agent should not be toxic to nondividing cells, such as neurons."( Induction of neuronal apoptosis by camptothecin, an inhibitor of DNA topoisomerase-I: evidence for cell cycle-independent toxicity.
Geller, HM; Morris, EJ, 1996
)
0.29
" We selected 44 compounds that exhibited toxic effects on HEL cells in the dividing phase from a chemical library containing 325 anticancer drugs and enzyme inhibitors."( Dividing phase-dependent cytotoxicity profiling of human embryonic lung fibroblast identifies candidate anticancer reagents.
Inagaki, Y; Matsumoto, Y; Sekimizu, K; Tang, W,
)
0.13

Compound-Compound Interactions

ExcerptReferenceRelevance
" We investigated the pharmacokinetics of aphidicolin in mice and examined its activity either alone or in combination with DDP in the DDP-sensitive M5076 (M5) murine reticular cell sarcoma as well as in a DDP-resistant subline (M5/DDP)."( Activity of aphidicolin glycinate alone or in combination with cisplatin in a murine ovarian tumor resistant to cisplatin.
Cavalli, F; D'Incalci, M; Damia, G; Davoli, E; Sessa, C; Tagliabue, G; Zucchetti, M, 1992
)
0.93
" Thus, we evaluated AG in combination with cisplatin in an in vivo model of cisplatin refractory human ovarian cancer."( Antitumor activity and biochemical effects of aphidicolin glycinate (NSC 303812) alone and in combination with cisplatin in vivo.
Cysyk, R; Hamilton, TC; Harrison, SD; Moyer, JD; O'Dwyer, PJ; Plowman, J; Suffness, M, 1994
)
0.55
" HL-60 and T24 cancer cell lines were treated with azacitidine or decitabine in combination with HC and DNA methylation of LRE1, MAGEA1 and CDKN2A was quantitatively measured by bisulphite-polymerase chain reaction pyrosequencing."( Hydroxycarbamide in combination with azacitidine or decitabine is antagonistic on DNA methylation inhibition.
Byun, HM; Choi, SH; Issa, JP; Kwan, JM; Yang, AS, 2007
)
0.34

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Regardless of the distribution of decay events, all treatment groups exhibited identical dose-response curves (D0: 101 125I decays/cell)."( Cell lethality after selective irradiation of the DNA replication fork.
Hofer, KG; Warters, RL, 1985
)
0.27
" However, BuPGdR did not accumulate single strand breaks in cells irradiated with 5 J/m2 UV-light even at the highest dosage tested, indicating that BuPGdR does not inhibit DNA repair."( Involvement of DNA polymerase delta and/or epsilon in joining UV-induced DNA single strand breaks in human fibroblasts (comparison of effects of butylphenyldeoxyguanosine with aphidicolin).
Itoh, R; Yamada, K, 1994
)
0.48
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (9)

RoleDescription
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
antiviral drugA substance used in the prophylaxis or therapy of virus diseases.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
EC 2.7.7.7 (DNA-directed DNA polymerase) inhibitorA DNA polymerase inhibitor that interferes with the action of a DNA-directed DNA polymerase (EC 2.7.7.7).
DNA synthesis inhibitorAny substance that inhibits the synthesis of DNA.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
fungal metaboliteAny eukaryotic metabolite produced during a metabolic reaction in fungi, the kingdom that includes microorganisms such as the yeasts and moulds.
Aspergillus metaboliteAny fungal metabolite produced during a metabolic reaction in the mould, Aspergillus.
antimitoticAny compound that inhibits cell division (mitosis).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
tetracyclic diterpenoidA diterpenoid with a tetracyclic skeleton.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (19)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID2517
Chain A, ATP-DEPENDENT DNA HELICASE Q1Homo sapiens (human)Potency5.62340.125919.1169125.8920AID2549
TDP1 proteinHomo sapiens (human)Potency0.11750.000811.382244.6684AID686978; AID686979
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency1.99530.00137.762544.6684AID914; AID915
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency6.30960.035520.977089.1251AID504332
huntingtin isoform 2Homo sapiens (human)Potency0.63100.000618.41981,122.0200AID2673
survival motor neuron protein isoform dHomo sapiens (human)Potency1.27580.125912.234435.4813AID1458
lamin isoform A-delta10Homo sapiens (human)Potency0.79430.891312.067628.1838AID1487
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA polymerase catalytic subunitHuman alphaherpesvirus 1 strain KOSIC50 (µMol)0.43800.43801.86903.3000AID340465
DNA polymerase catalytic subunitHuman alphaherpesvirus 1 strain 17IC50 (µMol)0.50000.50001.46673.3000AID255129
DNA polymerase betaHomo sapiens (human)IC50 (µMol)100.00001.40006.56679.0000AID547084
DNA polymerase betaRattus norvegicus (Norway rat)IC50 (µMol)100.00003.70006.20008.5000AID1155639
DNA polymerase catalytic subunitHuman herpesvirus 5 strain AD169IC50 (µMol)0.44350.40001.31742.5000AID255119; AID307427
DNA polymerase catalytic subunitHuman herpesvirus 3 strain DumasIC50 (µMol)1.60000.28001.93005.8000AID255124
DNA polymerase alpha catalytic subunitHomo sapiens (human)IC50 (µMol)5.15001.00002.74294.3000AID1449538; AID1614342; AID255106; AID35822; AID481809; AID547083
DNA polymerase delta catalytic subunitHomo sapiens (human)IC50 (µMol)40.00002.30002.30002.3000AID255107
DNA polymerase catalytic subunitHuman herpesvirus 6 (strain Uganda-1102)IC50 (µMol)0.40000.40000.40000.4000AID160323
DNA polymerase lambdaHomo sapiens (human)IC50 (µMol)200.00005.20005.30005.4000AID1323393
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
DNA polymerase alpha catalytic subunitHomo sapiens (human)EC50 (µMol)2.00002.00002.00002.0000AID53667
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (41)

Processvia Protein(s)Taxonomy
nucleotide-excision repair, DNA gap fillingDNA polymerase betaHomo sapiens (human)
in utero embryonic developmentDNA polymerase betaHomo sapiens (human)
DNA-templated DNA replicationDNA polymerase betaHomo sapiens (human)
DNA repairDNA polymerase betaHomo sapiens (human)
base-excision repairDNA polymerase betaHomo sapiens (human)
base-excision repair, gap-fillingDNA polymerase betaHomo sapiens (human)
pyrimidine dimer repairDNA polymerase betaHomo sapiens (human)
inflammatory responseDNA polymerase betaHomo sapiens (human)
DNA damage responseDNA polymerase betaHomo sapiens (human)
salivary gland morphogenesisDNA polymerase betaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damageDNA polymerase betaHomo sapiens (human)
response to gamma radiationDNA polymerase betaHomo sapiens (human)
somatic hypermutation of immunoglobulin genesDNA polymerase betaHomo sapiens (human)
response to ethanolDNA polymerase betaHomo sapiens (human)
lymph node developmentDNA polymerase betaHomo sapiens (human)
spleen developmentDNA polymerase betaHomo sapiens (human)
homeostasis of number of cellsDNA polymerase betaHomo sapiens (human)
neuron apoptotic processDNA polymerase betaHomo sapiens (human)
response to hyperoxiaDNA polymerase betaHomo sapiens (human)
immunoglobulin heavy chain V-D-J recombinationDNA polymerase betaHomo sapiens (human)
DNA biosynthetic processDNA polymerase betaHomo sapiens (human)
double-strand break repair via nonhomologous end joiningDNA polymerase betaHomo sapiens (human)
DNA repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleotide-excision repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA synthesis involved in UV-damage excision repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA synthesis involved in DNA repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replicationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replication, synthesis of primerDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replication initiationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA strand elongation involved in DNA replicationDNA polymerase alpha catalytic subunitHomo sapiens (human)
leading strand elongationDNA polymerase alpha catalytic subunitHomo sapiens (human)
lagging strand elongationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA repairDNA polymerase alpha catalytic subunitHomo sapiens (human)
double-strand break repair via nonhomologous end joiningDNA polymerase alpha catalytic subunitHomo sapiens (human)
regulation of type I interferon productionDNA polymerase alpha catalytic subunitHomo sapiens (human)
mitotic DNA replication initiationDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA synthesis involved in DNA repairDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA replicationDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA-templated DNA replicationDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA repairDNA polymerase delta catalytic subunitHomo sapiens (human)
base-excision repair, gap-fillingDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleotide-excision repair, DNA gap fillingDNA polymerase delta catalytic subunitHomo sapiens (human)
response to UVDNA polymerase delta catalytic subunitHomo sapiens (human)
cellular response to UVDNA polymerase delta catalytic subunitHomo sapiens (human)
fatty acid homeostasisDNA polymerase delta catalytic subunitHomo sapiens (human)
error-free translesion synthesisDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA biosynthetic processDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA replication proofreadingDNA polymerase delta catalytic subunitHomo sapiens (human)
base-excision repair, gap-fillingDNA polymerase subunit gamma-1Homo sapiens (human)
DNA metabolic processDNA polymerase subunit gamma-1Homo sapiens (human)
DNA-templated DNA replicationDNA polymerase subunit gamma-1Homo sapiens (human)
mitochondrial DNA replicationDNA polymerase subunit gamma-1Homo sapiens (human)
base-excision repairDNA polymerase subunit gamma-1Homo sapiens (human)
DNA replication proofreadingDNA polymerase subunit gamma-1Homo sapiens (human)
DNA biosynthetic processDNA polymerase subunit gamma-1Homo sapiens (human)
double-strand break repair via homologous recombinationDNA polymerase lambdaHomo sapiens (human)
DNA replicationDNA polymerase lambdaHomo sapiens (human)
base-excision repair, gap-fillingDNA polymerase lambdaHomo sapiens (human)
nucleotide-excision repairDNA polymerase lambdaHomo sapiens (human)
double-strand break repair via nonhomologous end joiningDNA polymerase lambdaHomo sapiens (human)
somatic hypermutation of immunoglobulin genesDNA polymerase lambdaHomo sapiens (human)
DNA biosynthetic processDNA polymerase lambdaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
damaged DNA bindingDNA polymerase betaHomo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase betaHomo sapiens (human)
DNA-(apurinic or apyrimidinic site) endonuclease activityDNA polymerase betaHomo sapiens (human)
protein bindingDNA polymerase betaHomo sapiens (human)
microtubule bindingDNA polymerase betaHomo sapiens (human)
lyase activityDNA polymerase betaHomo sapiens (human)
enzyme bindingDNA polymerase betaHomo sapiens (human)
metal ion bindingDNA polymerase betaHomo sapiens (human)
5'-deoxyribose-5-phosphate lyase activityDNA polymerase betaHomo sapiens (human)
class I DNA-(apurinic or apyrimidinic site) endonuclease activityDNA polymerase betaHomo sapiens (human)
nucleotide bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
chromatin bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase alpha catalytic subunitHomo sapiens (human)
protein bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
zinc ion bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
protein kinase bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
DNA replication origin bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
single-stranded DNA bindingDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleotide bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
chromatin bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
damaged DNA bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase delta catalytic subunitHomo sapiens (human)
protein bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
enzyme bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
metal ion bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
4 iron, 4 sulfur cluster bindingDNA polymerase delta catalytic subunitHomo sapiens (human)
3'-5'-DNA exonuclease activityDNA polymerase delta catalytic subunitHomo sapiens (human)
protease bindingDNA polymerase subunit gamma-1Homo sapiens (human)
DNA bindingDNA polymerase subunit gamma-1Homo sapiens (human)
chromatin bindingDNA polymerase subunit gamma-1Homo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase subunit gamma-1Homo sapiens (human)
protein bindingDNA polymerase subunit gamma-1Homo sapiens (human)
single-stranded DNA 3'-5' DNA exonuclease activityDNA polymerase subunit gamma-1Homo sapiens (human)
3'-5' exonuclease activityDNA polymerase subunit gamma-1Homo sapiens (human)
5'-deoxyribose-5-phosphate lyase activityDNA polymerase subunit gamma-1Homo sapiens (human)
DNA bindingDNA polymerase lambdaHomo sapiens (human)
DNA-directed DNA polymerase activityDNA polymerase lambdaHomo sapiens (human)
protein bindingDNA polymerase lambdaHomo sapiens (human)
metal ion bindingDNA polymerase lambdaHomo sapiens (human)
5'-deoxyribose-5-phosphate lyase activityDNA polymerase lambdaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (23)

Processvia Protein(s)Taxonomy
nucleusDNA polymerase betaHomo sapiens (human)
nucleoplasmDNA polymerase betaHomo sapiens (human)
cytoplasmDNA polymerase betaHomo sapiens (human)
microtubuleDNA polymerase betaHomo sapiens (human)
spindle microtubuleDNA polymerase betaHomo sapiens (human)
protein-containing complexDNA polymerase betaHomo sapiens (human)
nucleusDNA polymerase betaHomo sapiens (human)
nucleusDNA polymerase alpha catalytic subunitHomo sapiens (human)
nuclear envelopeDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleoplasmDNA polymerase alpha catalytic subunitHomo sapiens (human)
alpha DNA polymerase:primase complexDNA polymerase alpha catalytic subunitHomo sapiens (human)
nucleolusDNA polymerase alpha catalytic subunitHomo sapiens (human)
cytosolDNA polymerase alpha catalytic subunitHomo sapiens (human)
nuclear matrixDNA polymerase alpha catalytic subunitHomo sapiens (human)
chromatinDNA polymerase alpha catalytic subunitHomo sapiens (human)
chromosome, telomeric regionDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleusDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleoplasmDNA polymerase delta catalytic subunitHomo sapiens (human)
cytosolDNA polymerase delta catalytic subunitHomo sapiens (human)
membraneDNA polymerase delta catalytic subunitHomo sapiens (human)
aggresomeDNA polymerase delta catalytic subunitHomo sapiens (human)
delta DNA polymerase complexDNA polymerase delta catalytic subunitHomo sapiens (human)
nucleotide-excision repair complexDNA polymerase delta catalytic subunitHomo sapiens (human)
mitochondrionDNA polymerase subunit gamma-1Homo sapiens (human)
mitochondrial matrixDNA polymerase subunit gamma-1Homo sapiens (human)
gamma DNA polymerase complexDNA polymerase subunit gamma-1Homo sapiens (human)
mitochondrial nucleoidDNA polymerase subunit gamma-1Homo sapiens (human)
intracellular membrane-bounded organelleDNA polymerase subunit gamma-1Homo sapiens (human)
protein-containing complexDNA polymerase subunit gamma-1Homo sapiens (human)
mitochondrionDNA polymerase subunit gamma-1Homo sapiens (human)
site of double-strand breakDNA polymerase lambdaHomo sapiens (human)
nucleusDNA polymerase lambdaHomo sapiens (human)
nucleoplasmDNA polymerase lambdaHomo sapiens (human)
nucleusDNA polymerase lambdaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (90)

Assay IDTitleYearJournalArticle
AID307428Inhibition of HSV1 DNA polymerase by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID340466Inhibition of VZV DNA polymerase by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID503604Inhibition of B-myb-mediated mitotic deffects in zebrafish bmyb mutant embryo assessed as intra-Sphase and G2/M checkpoint inhibition in presence of 2 mM caffeine at 10 ug/ml2005Nature chemical biology, Dec, Volume: 1, Issue:7
Small molecules that delay S phase suppress a zebrafish bmyb mutant.
AID255124Inhibition of Varicella-Zoster virus DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID82561Antiviral activity in a cell-based plaque reduction assay, using an HFF cell line and the Davis strain of HCMV; no data2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase.
AID1270877Effect on cell cycle distribution in against mouse 92TAg cells assessed as cell accumulation at S-phase at 8 ug/ml incubated for 15 hrs by propidium iodide staining based cytofluorimetric analysis2015Journal of natural products, Nov-25, Volume: 78, Issue:11
Identification of 5-Methoxyflavone as a Novel DNA Polymerase-Beta Inhibitor and Neuroprotective Agent against Beta-Amyloid Toxicity.
AID307429Inhibition of VZV DNA polymerase by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID53467Effective concentration against DNA polymerase of Herpes simplex virus 2 (HSV-2)1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Isosteres of the DNA polymerase inhibitor aphidicolin as potential antiviral agents against human herpes viruses.
AID340467Inhibition of human polymerase alpha by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID481584Inhibition of HSV1 KOS DNA polymerase infected in african green monkey Vero cells2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
AID1449538Inhibition of human DNA polymerase alpha using 5' end radiolabeled 24nt DNA/48nt DNA as primer/template after 5 mins by PAGE analysis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
2'-Chloro,2'-fluoro Ribonucleotide Prodrugs with Potent Pan-genotypic Activity against Hepatitis C Virus Replication in Culture.
AID399272In vivo antitumor activity against mouse P388 cells
AID1155638Inhibition of calf thymus DNA polymerase alpha assessed as incorporation of [3H]dTTP into poly(dA)/oligo(dT)18 DNA-template primer after 60 mins2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Polyketides from the cultured lichen mycobiont of a Vietnamese Pyrenula sp.
AID160323Inhibitory activity against Human Cytomegalovirus (HCMV) polymerase2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID357848Antiviral activity against HSV1 in african green monkey Vero cells assessed as reduction in number of plaques at 0.005 mg/ml after 66 hrs
AID1270879Effect on cell cycle distribution in against polymerase-beta knock out mouse 88TAg cells assessed as cell accumulation at S-phase at 8 ug/ml incubated for 15 hrs by propidium iodide staining based cytofluorimetric analysis2015Journal of natural products, Nov-25, Volume: 78, Issue:11
Identification of 5-Methoxyflavone as a Novel DNA Polymerase-Beta Inhibitor and Neuroprotective Agent against Beta-Amyloid Toxicity.
AID481586Inhibition of VZV KOS DNA polymerase infected in HFF cells2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
AID299441Inhibition of VZV DNA polymerase2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID255119Inhibition of human cytomegalovirus DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID86065Concentration which caused 50% loss of the monolayer present around the viral plaques in ug/mL.2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents.
AID55151Ability of compound to inhibit DNA synthesis against the uptake of [3H]thymidine in freshly seeded cultures of SV-40 transformed WI-38 human lung fibroblast at a concentration 0.15 ug/mL.1984Journal of medicinal chemistry, Oct, Volume: 27, Issue:10
Synthesis of a tricyclic aphidicolin analogue that inhibits DNA synthesis in vitro.
AID83917In vitro antiviral activity against Herpes Simplex-1 virus (HSV-1) expressed as percent reduction in the number of viral plaques2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents.
AID86335Compound was evaluated for the effect on [3H]- Uridine incorporation by HeLa cells and percentage inhibition into RNA1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis, cell growth inhibition, and antitumor screening of 2-(p-n-butylanilino)purines and their nucleoside analogues.
AID86064Concentration which caused 50% loss of the monolayer present around the viral plaques in uM2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents.
AID307435Inhibition of human DNA polymerase alpha by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID503600Inhibition of B-myb-mediated mitotic deffects in zebrafish bmyb mutant crb embryos at 50 mM2005Nature chemical biology, Dec, Volume: 1, Issue:7
Small molecules that delay S phase suppress a zebrafish bmyb mutant.
AID1443138Inhibition of human DNA polymerase-alpha2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Discovery of a 2'-fluoro-2'-C-methyl C-nucleotide HCV polymerase inhibitor and a phosphoramidate prodrug with favorable properties.
AID324482Increase in light chain 3-GFP+ autophagosome vesicle area per cell in human H4 cells at 11.3 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID53667Effective concentration against DNA polymerase alpha1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Isosteres of the DNA polymerase inhibitor aphidicolin as potential antiviral agents against human herpes viruses.
AID481581Inhibition of HCMV DNA polymerase infected in HFF cells2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
AID86334Compound was evaluated for the effect on [3H]- Uridine incorporation by HeLa cells and percentage inhibition into DNA1987Journal of medicinal chemistry, Jan, Volume: 30, Issue:1
Synthesis, cell growth inhibition, and antitumor screening of 2-(p-n-butylanilino)purines and their nucleoside analogues.
AID512140Antiviral activity against HSV1 infected in african green monkey Vero cells assessed as minimum antiviral concentration after 6 hrs2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents.
AID324534Increase in light chain 3-GFP+ autophagosome vesicle intensity per cell in human H4 cells at 11.3 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID503603Inhibition of B-myb-mediated mitotic deffects in zebrafish bmyb mutant embryo assessed as intra-Sphase and G2/M checkpoint inhibition at 10 ug/ml2005Nature chemical biology, Dec, Volume: 1, Issue:7
Small molecules that delay S phase suppress a zebrafish bmyb mutant.
AID35822Compound was evaluated for the inhibitory activity against Human alpha polymerase2000Bioorganic & medicinal chemistry letters, Sep-18, Volume: 10, Issue:18
Naphthalene carboxamides as inhibitors of human cytomegalovirus DNA polymerase.
AID1503774Cytotoxicity against human HL cells assessed as cell viability at 50 uM after 72 hrs by resazurin dye based fluorescence assay relative to control2017Journal of natural products, 10-27, Volume: 80, Issue:10
Identification of Privileged Antichlamydial Natural Products by a Ligand-Based Strategy.
AID255107Inhibition of human delta DNA polymerase (95 uL) activity in a solution containg 6.4 mM HEPES (pH 7.5) upon incubation for 12 minutes at 26 degrees C with the compound dissolved in DMSO2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID512141Cytotoxicity against african green monkey Vero cells assessed as loss of monolayer present around the plaques2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents.
AID299437Inhibition of human cytomegalovirus DNA polymerase2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID481809Inhibition of human DNA polymerase alpha2010Bioorganic & medicinal chemistry letters, May-15, Volume: 20, Issue:10
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
AID547083Inhibition of human DNA polymerase alpha assessed as incorporation of [alpha-32P]dCTP up to 1mM preincubated for 30 mins by whatman DE81 paper binding assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1503775Antichlamydial activity against Chlamydia pneumoniae K7 infected in HL cells assessed as chlamydial inhibition at 50 uM after 70 hrs by fluorescent microscopic analysis2017Journal of natural products, 10-27, Volume: 80, Issue:10
Identification of Privileged Antichlamydial Natural Products by a Ligand-Based Strategy.
AID83747Minimum antiviral concentration proved to be lethal to viral population in ug/mL.2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents.
AID503599Inhibition of B-myb-mediated mitotic deffects in zebrafish bmyb mutant crb embryos at 10 ug/ml2005Nature chemical biology, Dec, Volume: 1, Issue:7
Small molecules that delay S phase suppress a zebrafish bmyb mutant.
AID340464Inhibition of HCMV DNA polymerase by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID464099Inhibition of Varicella zoster virus recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase.
AID255129Inhibition of herpes simplex virus type 1 DNA polymerase (95 uL) activity in a solution containing 6.4 mM HEPES (pH 7.5), incubation for 12 minutes at 26 degrees C2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID83746Minimum antiviral concentration proved to be lethal to viral population in uM2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
Synthesis and biological evaluation of certain alpha,beta-unsaturated ketones and their corresponding fused pyridines as antiviral and cytotoxic agents.
AID307427Inhibition of HCMV DNA polymerase by scintillation proximity assay2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
AID1614342Inhibition of human DNA polymerase alpha using 5-end radiolabeled 24nt to 48nt DNA as primer template after 5 mins in presence of dCTP/dGTP/dTTP/dATP by PAGE analysis2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Discovery of a Series of 2'-α-Fluoro,2'-β-bromo-ribonucleosides and Their Phosphoramidate Prodrugs as Potent Pan-Genotypic Inhibitors of Hepatitis C Virus.
AID512139Antiviral activity against HSV1 infected in african green monkey Vero cells after 6 hrs by plaque reduction assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents.
AID547085Inhibition of human DNA polymerase gamma assessed as incorporation of [alpha-32P]dCTP up to 1mM preincubated for 30 mins by whatman DE81 paper binding assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication.
AID1155639Inhibition of rat recombinant DNA polymerase beta expressed in Escherichia coli JMpbeta5 cells assessed as incorporation of [3H]dTTP into poly(dA)/oligo(dT)18 DNA-template primer after 60 mins2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Polyketides from the cultured lichen mycobiont of a Vietnamese Pyrenula sp.
AID1323394Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay2016Journal of natural products, 07-22, Volume: 79, Issue:7
Polyprenylated Benzoylphloroglucinols with DNA Polymerase Inhibitory Activity from the Fruits of Garcinia schomburgkiana.
AID1155640Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 24 hrs by WST-1 assay2014Journal of natural products, Jun-27, Volume: 77, Issue:6
Polyketides from the cultured lichen mycobiont of a Vietnamese Pyrenula sp.
AID255106Inhibition of human alpha DNA polymerase (95 uL) activity in a solution containg 6.4 mM HEPES (pH 7.5) upon incubation for 12 minutes at 26 degrees C with the compound dissolved in DMSO2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
4-Oxo-4,7-dihydrothieno[2,3-b]pyridines as non-nucleoside inhibitors of human cytomegalovirus and related herpesvirus polymerases.
AID299442Inhibition of human DNA polymerase alpha2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID324379Induction of light chain 3-GFP level in human H4 cells at 7.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID340465Inhibition of HSV1 DNA polymerase by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
AID464096Inhibition of HCMV recombinant DNA polymerase expressed in baculovirus infected SF9 cells after 12 mins by scintillation proximity assay2010Bioorganic & medicinal chemistry letters, Mar-15, Volume: 20, Issue:6
The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase.
AID547084Inhibition of human DNA polymerase beta assessed as incorporation of [alpha-32P]dCTP up to 1mM preincubated for 30 mins by whatman DE81 paper binding assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication.
AID1323392Inhibition of calf thymus DNA polymerase alpha assessed as reduction in [3H]dTTP incorporation using poly(dA)/oligo(dT)18 as template/primer preincubated for 10 mins followed by template/primer addition measured after 60 mins2016Journal of natural products, 07-22, Volume: 79, Issue:7
Polyprenylated Benzoylphloroglucinols with DNA Polymerase Inhibitory Activity from the Fruits of Garcinia schomburgkiana.
AID324431Increase in light chain 3-GFP+ autophagosome vesicle number per cell in human H4 cells at 7.4 uM after 24 hrs by high throughput fluorescence microscopy relative to control2007Proceedings of the National Academy of Sciences of the United States of America, Nov-27, Volume: 104, Issue:48
Small molecule regulators of autophagy identified by an image-based high-throughput screen.
AID1323393Inhibition of recombinant human His-tagged DNA polymerase lambda assessed as reduction in [3H]dTTP incorporation using poly(dA)/oligo(dT)18 as template/primer preincubated for 10 mins followed by template/primer addition measured after 60 mins2016Journal of natural products, 07-22, Volume: 79, Issue:7
Polyprenylated Benzoylphloroglucinols with DNA Polymerase Inhibitory Activity from the Fruits of Garcinia schomburgkiana.
AID299440Inhibition of HSV1 DNA polymerase2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
7-Oxo-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamides: synthesis and biological activity of a new class of highly potent inhibitors of human cytomegalovirus DNA polymerase.
AID1540241Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 48 hrs by MTT assay
AID357849Cytotoxicity against african green monkey Vero cells after 66 hrs
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
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
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,597)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990505 (31.62)18.7374
1990's569 (35.63)18.2507
2000's354 (22.17)29.6817
2010's143 (8.95)24.3611
2020's26 (1.63)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.86

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.86 (24.57)
Research Supply Index7.41 (2.92)
Research Growth Index4.34 (4.65)
Search Engine Demand Index64.10 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (0.18%)5.53%
Reviews23 (1.40%)6.00%
Case Studies3 (0.18%)4.05%
Observational0 (0.00%)0.25%
Other1,618 (98.24%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]