Loceryl (amorolfine) is a topical antifungal medication used to treat fungal infections of the skin, nails, and scalp. It is a synthetically produced compound with a chemical structure similar to that of other antifungal agents like naftifine. The mechanism of action of amorolfine is not fully understood, but it is believed to inhibit the synthesis of ergosterol, a vital component of fungal cell membranes. This disruption leads to the death of fungal cells. Amorolfine is highly effective against dermatophytes, which are the fungi most commonly responsible for skin infections. It is also effective against yeasts and molds. Loceryl is available as a topical cream, solution, and nail lacquer. The drug is generally well-tolerated, but side effects can include skin irritation, redness, and itching. Loceryl has become an important treatment option for fungal infections due to its effectiveness, convenience, and relatively low incidence of side effects. Ongoing research focuses on exploring the potential of amorolfine for other medical applications, including treatment of onychomycosis (nail fungal infection) and even as an anti-cancer agent.'
amorolfine: RN given refers to parent cpd
amorolfine : A member of the class of morpholines that is cis-2,6-dimethylmorpholine in which the hydrogen attached to the nitrogen is replaced by a racemic 2-methyl-3-[p-(2-methylbutan-2-yl)phenyl]propyl group. An inhibitor of the action of squalene monooxygenase, Delta(14) reductase and D7-D8 isomerase and an antifungal agent, it is used (generally as its hydrochloride salt) for the topical treatment of fungal nail and skin infections.
ID Source | ID |
---|---|
PubMed CID | 54260 |
CHEMBL ID | 489411 |
CHEBI ID | 599440 |
SCHEMBL ID | 150666 |
MeSH ID | M0116979 |
Synonym |
---|
AC-1982 |
AB01274715-01 |
amorolfine (usan/inn) |
loceryl (tn) |
78613-35-1 |
D02923 |
cis-4-[3-[4-(1,1-dimethylpropyl)phenyl]-2-methylpropyl]-2,6-dimethylmorpholine |
amorolfine |
(2s,6r)-4-[3-[4-(1,1-dimethylpropyl)phenyl]-2-methyl-propyl]-2,6-dimethyl-morpholine |
NCGC00167524-01 |
HMS2089I20 |
amorolfinum |
(+-)-cis-2,6-dimethyl-4-(2-methyl-3-(p-tert-pentylphenyl)propyl)morpholine |
(2r,6s)-2,6-dimethyl-4-{2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl}morpholine |
CHEBI:599440 , |
meso-2,6-dimethyl-4-(2-methyl-3-(p-tert-pentylphenyl)propyl)morpholine |
meso-2,6-dimethyl-4-{2-methyl-3-[4-(2-methylbutan-2-yl)phenyl]propyl}morpholine |
CHEMBL489411 |
A839459 |
(2r,6s)-4-[3-[4-(1,1-dimethylpropyl)phenyl]-2-methyl-propyl]-2,6-dimethyl-morpholine |
cas-78613-35-1 |
tox21_112521 |
dtxcid8026690 |
dtxsid0046690 , |
NCGC00167524-03 |
AKOS015896221 |
DL-246 |
SCHEMBL150666 |
MQHLMHIZUIDKOO-AYHJJNSGSA-N |
tox21_112521_1 |
NCGC00167524-02 |
AB01274715-02 |
AB01274715_03 |
AB01274715_04 |
sr-05000001441 |
SR-05000001441-1 |
(2s,6r)-2,6-dimethyl-4-(2-methyl-3-(4-tert-pentylphenyl)propyl)morpholine |
(+/-)-cis-2,6-dimethyl-4-[2-methyl-3-(p-t-pentylphenyl)propyl]-morpholin |
DB09056 |
Q123195 |
AMY32521 |
EX-A4134 |
cis-2,6-dimethyl-4-(2-methyl-3-(4-(tert-pentyl)phenyl)propyl)morpholine |
EN300-18563881 |
Excerpt | Reference | Relevance |
---|---|---|
"One of the pre-requisite for a successful topical antifungal drug indicated for onychomycosis is its bioavailability into the nail unit for achieving fungal eradication and clinical benefit." | ( Ciclopirox vs amorolfine: in vitro penetration into and permeation through human healthy nails of commercial nail lacquers. Burgalassi, S; Chetoni, P; Mailland, F; Monti, D; Tampucci, S, 2014) | 0.4 |
"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 |
Loceryl nail lacquer was developed to provide the effective antifungal drug, amorolfine, in a once-weekly dosage regimen combined with a convenient mode of application.
Excerpt | Relevance | Reference |
---|---|---|
"Loceryl nail lacquer was developed to provide the effective antifungal drug, amorolfine, in a once-weekly dosage regimen combined with a convenient mode of application." | ( Loceryl nail lacquer--realization of a new galenical approach to onychomycosis therapy. Erni, W; Gerhards, J; Klecak, G; Pittrof, F, 1992) | 3.17 |
"Ro 14-4767, Loceryl is a member of a new class of antimycotics, and a number of dosage forms are being developed for its topical application." | ( Determination of Ro 14-4767 (Loceryl) by LC using automated column switching with ultraviolet and electrochemical detection. Czech, MA; Meltzer, M; Mouskountakis, J, 1991) | 0.95 |
" Study B: More subjects adhered to amorolfine dosage (81." | ( Patient-reported outcomes from two randomised studies comparing once-weekly application of amorolfine 5% nail lacquer to other methods of topical treatment in distal and lateral subungual onychomycosis. Sarkany, M; Schaller, M; Sigurgeirsson, B, 2017) | 0.46 |
Role | Description |
---|---|
EC 1.14.13.132 (squalene monooxygenase) inhibitor | An EC 1.14.13.* (oxidoreductase acting on paired donors, incorporating 1 atom of oxygen, with NADH or NADPH as one donor) inhibitor that interferes with the action of squalene monooxygenase (EC 1.14.13.132). |
EC 5.3.3.5 (cholestenol Delta-isomerase) inhibitor | An EC 5.3.3.* (intramolecular oxidase transposing C=C bonds) inhibitor that interferes with the action of a cholestenol Delta-isomerase (EC 5.3.3.5). |
EC 1.3.1.70 (Delta(14)-sterol reductase) inhibitor | An EC 1.3.1.* (oxidoreductase acting on donor CH-CH group, NAD(+) or NADP(+) as acceptor) inhibitor that interferes with the action of Delta(14)-sterol reductase (EC 1.3.1.70). |
[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] |
Class | Description |
---|---|
tertiary amino compound | A compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups. |
morpholine antifungal drug | Any morpholine antifungal agent used to treat fungal infections in humans or animals. |
[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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 26.8325 | 3.1890 | 29.8841 | 59.4836 | AID1224846; AID1224894 |
Fumarate hydratase | Homo sapiens (human) | Potency | 23.4850 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
USP1 protein, partial | Homo sapiens (human) | Potency | 50.1187 | 0.0316 | 37.5844 | 354.8130 | AID504865 |
TDP1 protein | Homo sapiens (human) | Potency | 33.4983 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
GLI family zinc finger 3 | Homo sapiens (human) | Potency | 26.6032 | 0.0007 | 14.5928 | 83.7951 | AID1259369; AID1259392 |
AR protein | Homo sapiens (human) | Potency | 27.3441 | 0.0002 | 21.2231 | 8,912.5098 | AID1259247; AID743035; AID743042; AID743054; AID743063 |
cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 15.4871 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 22.6142 | 0.0002 | 14.3764 | 60.0339 | AID720691; AID720692 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 28.2263 | 0.0030 | 41.6115 | 22,387.1992 | AID1159553; AID1159555 |
retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 2.3914 | 0.0008 | 17.5051 | 59.3239 | AID1159527 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 25.7565 | 0.0015 | 30.6073 | 15,848.9004 | AID1224848; AID1224849; AID1259403 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 11.2202 | 0.0054 | 28.0263 | 1,258.9301 | AID1346985 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 29.2153 | 0.0002 | 29.3054 | 16,493.5996 | AID743069; AID743075; AID743078; AID743079; AID743080; AID743091 |
G | Vesicular stomatitis virus | Potency | 24.5454 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2D6 | Homo sapiens (human) | Potency | 4.8975 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
polyprotein | Zika virus | Potency | 23.4850 | 0.0030 | 8.7949 | 48.0869 | AID1347053 |
peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 23.9145 | 0.0010 | 19.4141 | 70.9645 | AID743094 |
aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 29.8493 | 0.0007 | 23.0674 | 1,258.9301 | AID743085 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 33.4915 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 29.8493 | 0.0016 | 28.0151 | 77.1139 | AID1259385; AID1259395 |
activating transcription factor 6 | Homo sapiens (human) | Potency | 23.9145 | 0.1434 | 27.6121 | 59.8106 | AID1159516 |
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 26.8325 | 19.7391 | 45.9784 | 64.9432 | AID1159509 |
v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 15.6992 | 0.0578 | 21.1097 | 61.2679 | AID1159526; AID1159528 |
Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 49.1940 | 0.0391 | 47.5451 | 146.8240 | AID1224845 |
potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 12.5893 | 0.0178 | 9.6374 | 44.6684 | AID588834 |
thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 12.3572 | 0.0003 | 23.4451 | 159.6830 | AID743065; AID743067 |
nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 30.7312 | 0.0006 | 27.2152 | 1,122.0200 | AID743202; AID743219 |
nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 31.6228 | 0.0079 | 8.2332 | 1,122.0200 | AID2546 |
geminin | Homo sapiens (human) | Potency | 13.3359 | 0.0046 | 11.3741 | 33.4983 | AID624296 |
Interferon beta | Homo sapiens (human) | Potency | 24.5454 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 24.5454 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 29.8493 | 0.0023 | 19.5956 | 74.0614 | AID651631 |
Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 39.8107 | 0.0096 | 10.5250 | 35.4813 | AID1479145 |
Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 24.5454 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 24.5454 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347154 | Primary screen GU AMC 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 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
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 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1271232 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosta-7,22-dien-3-ol,(3a'22E) level at 0.125 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271243 | Antifungal activity against Aspergillus niger ATCC 10578 after 48 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID634087 | Antifungal activity against Candida albicans assessed as morphogenetic transformation after 3 hrs by phase-contrast microscopy | 2012 | European journal of medicinal chemistry, Jan, Volume: 47, Issue:1 | Antifungal activities of novel non-azole molecules against S. cerevisiae and C. albicans. |
AID416040 | Fungicidal activity against tebuconazole-nonadapted wild type Colletotrichum graminicola CgM2 assessed as inhibition of radial growth rate at 23 degC in darkness | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Treatment of a clinically relevant plant-pathogenic fungus with an agricultural azole causes cross-resistance to medical azoles and potentiates caspofungin efficacy. |
AID1271240 | Antifungal activity against Candida glabrata NCYC 388 after 72 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271253 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as squalene level at 0.25 ug/ml for 24 hrs by spectrophotometry (Rvb = 7.17 +/- 0.35 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271260 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosterol level at 0.25 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271252 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosterol level at 0.125 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271261 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosta-7,22-dien-3-ol,(3a'22E) level at 0.25 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271237 | Antifungal activity against Cryptococcus neoformans ATCC 34664 after 24 to 36 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271251 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as lichesterol level at 0.125 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271239 | Antifungal activity against Candida glabrata NCYC 388 after 24 to 36 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271259 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as lichesterol level at 0.25 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271254 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosterol level at 0.25 ug/ml for 24 hrs by spectrophotometry (Rvb = 73.34 +/- 2.53 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID416041 | Fungicidal activity against tebuconazole-adapted wild type Colletotrichum graminicola CgM2 assessed as inhibition of radial growth rate at 23 degC in darkness | 2007 | Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10 | Treatment of a clinically relevant plant-pathogenic fungus with an agricultural azole causes cross-resistance to medical azoles and potentiates caspofungin efficacy. |
AID1271264 | Toxicity in human RBC assessed as hemolysis upto 128 ug/ml | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271236 | Antifungal activity against Candida albicans ATCC 10231 after 72 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271233 | Antifungal activity against Candida albicans ATCC 24433 after 24 to 36 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271245 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as squalene level at 0.125 ug/ml for 24 hrs by spectrophotometry (Rvb = 7.17 +/- 0.35 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271241 | Antifungal activity against Candida tropicalis ATCC 750 after 24 to 36 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271256 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosta-5,8-dien-3-ol,(3a') level at 0.25 ug/ml for 24 hrs by spectrophotometry (Rvb = 5.15 +/- 0.44 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271247 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosterol level at 0.125 ug/ml for 24 hrs by spectrophotometry (Rvb = 73.34 +/- 2.53 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271257 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as cholesta-5,24-dien-3-ol level at 0.25 ug/ml for 24 hrs by spectrophotometry (Rvb = 3.58 +/- 0.52 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271242 | Antifungal activity against Candida tropicalis ATCC 750 after 72 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271234 | Antifungal activity against Candida albicans ATCC 24433 after 72 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271248 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ergosta-5,8-dien-3-ol,(3a') level at 0.125 ug/ml for 24 hrs by spectrophotometry (Rvb = 5.15 +/- 0.44 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271250 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ignosterol level at 0.125 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271244 | Antifungal activity against Aspergillus niger ATCC 10578 after 72 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271246 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as cholesta-8,24-dien-3-ol,4-methyl-(3a',4a') level at 0.125 ug/ml for 24 hrs by spectrophotometry (Rvb = 7.19 +/- 0.65 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271235 | Antifungal activity against Candida albicans ATCC 10231 after 24 to 36 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271255 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as cholesta-8,24-dien-3-ol,4-methyl-(3a',4a') level at 0.25 ug/ml for 24 hrs by spectrophotometry (Rvb = 7.19 +/- 0.65 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271258 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as ignosterol level at 0.25 ug/ml for 24 hrs by spectrophotometry | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271249 | Effect on sterol profile of Candida albicans ATCC 24433 assessed as cholesta-5,24-dien-3-ol level at 0.125 ug/ml for 24 hrs by spectrophotometry (Rvb = 3.58 +/- 0.52 %) | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID1271238 | Antifungal activity against Cryptococcus neoformans ATCC 34664 after 72 hrs by broth microdilution method | 2015 | ACS medicinal chemistry letters, Nov-12, Volume: 6, Issue:11 | Silicon Incorporated Morpholine Antifungals: Design, Synthesis, and Biological Evaluation. |
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 16 (8.79) | 18.7374 |
1990's | 46 (25.27) | 18.2507 |
2000's | 41 (22.53) | 29.6817 |
2010's | 60 (32.97) | 24.3611 |
2020's | 19 (10.44) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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 very strong demand-to-supply ratio for research on this compound.
| This Compound (51.15) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 37 (18.78%) | 5.53% |
Reviews | 23 (11.68%) | 6.00% |
Case Studies | 22 (11.17%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 115 (58.38%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |