mofezolac profile

Mofezolac is a non-steroidal anti-inflammatory drug (NSAID) that was developed as a potential treatment for osteoarthritis. It acts by inhibiting the enzyme cyclooxygenase (COX), which is involved in the production of prostaglandins, inflammatory mediators that contribute to pain and swelling. Mofezolac was studied for its potential analgesic and anti-inflammatory effects, and it showed promising results in clinical trials. However, its development was discontinued due to concerns about its potential for liver toxicity. Despite its discontinuation, research on mofezolac continues, focusing on its mechanism of action, potential therapeutic applications, and safety profile.'

mofezolac: Cyclooxygenase 1 inhibitor; structure in first source; RN from Toxlit [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	4237
CHEMBL ID	259972
CHEBI ID	31860
SCHEMBL ID	151701
MeSH ID	M0155057

Synonym
BB 0262402
IFLAB1_003830
n-22
disopain
mofezolac
3,4-bis(p-methoxyphenyl)-5-isoxazoleacetic acid
brn 5986171
3,4-bis((4-methoxyphenyl)-5-isooxazolyl)acetic acid
mofezolacum [inn-latin]
ccris 4316
acetic acid, 3,4-bis(4-methoxyphenyl)-5-isooxazolyl-
mofezolac [inn]
mofezolaco [inn-spanish]
5-isoxazoleacetic acid, 3,4-bis(4-methoxyphenyl)-
3,4-bis(4-methoxyphenyl)-5-isoxazoleacetic acid
(3,4-bis(4-methoxyphenyl)-5-isoxazolyl)acetic acid
IDI1_009937
CBKINASE1_024622
OPREA1_588700
CBKINASE1_012222
OPREA1_261181
78967-07-4
D01718
mofezolac (jan/inn)
mofezolac (tn)
NCGC00167563-01
CHEMBL259972 ,
AKOS000523630
BRD-K49372556-001-01-7
HMS1422O02
2-[3,4-bis(4-methoxyphenyl)-1,2-oxazol-5-yl]acetic acid
STK973280
[3,4-bis(4-methoxyphenyl)-1,2-oxazol-5-yl]acetic acid
dtxsid1046716 ,
cas-78967-07-4
tox21_112558
dtxcid9026716
CCG-107450
[3,4-bis-(4-methoxyphenyl)isoxazol-5-yl]-acetic acid
mofezolaco
rvj0bv3h3y ,
unii-rvj0bv3h3y
mofezolacum
bdbm50376383
2-(3,4-bis(4-methoxyphenyl)isoxazol-5-yl)acetic acid
smr000069874
[3,4-bis(4-methoxyphenyl)-5-isoxazolyl]acetic acid
MLS006011640
SCHEMBL151701
mofezolac [who-dd]
mofezolac [mi]
mofezolac [mart.]
mofezolac [jan]
DJEIHHYCDCTAAH-UHFFFAOYSA-N
3,4,-di(p-methoxyphenyl)isoxazol-5-acetic acid
[3,4-bis(4-methoxyphenyl)isoxazol-5-yl]acetic acid
[3,4-bis-(4-methoxy-phenyl)isoxazol-5-yl]acetic acid
AS-68999
CHEBI:31860
63X ,
'[3,4-bis(4-methoxyphenyl)-1,2-oxazol-5-yl]acetic acid'
Q15409378
BRD-K49372556-001-02-5
N16836
A914371
HY-120824
CS-0079262

Excerpt	Reference	Relevance
"Mofezolac (N-22) is a newly developed analgesic and anti-inflammatory agent. "	( Acute toxicity tests of mofezolac (N-22) in mice and rats. Ichiki, T; Kodama, R; Kuwasaki, E; Kuwata, M; Satoh, K; Sone, H; Yamamoto, N; Yamashita, K, 1990)	2.03
"Mofezolac (N-22) is a new developed analgesic and anti-inflammatory agent. "	( [Reproductive and developmental toxicity study of mofezolac (N-22) (3)--Teratogenicity study in rabbits by oral administration]. Fuchigami, K; Kodama, R; Matsunaga, K; Otsuka, T; Sameshima, K; Yamakita, O, 1990)	1.97
"Mofezolac (N-22) is a new developed analgesic and anti-inflammatory agent. "	( [Three-month subacute oral toxicity study of mofezolac (N-22) in dogs]. Iwata, M; Kiguchi, M; Nasu, Y; Shimpo, K; Takeuchi, M; Yada, H; Yamashita, K, 1990)	1.98

Excerpt	Reference	Relevance
"Mofezolac also has a potent inhibitory activity on the algesic responses induced by the mechanical stimulus of the inflammed tissue."	( [Pharmacological profile of mofezolac, a new non-steroidal analgesic anti-inflammatory drug]. Miyake, H; Ono, N; Sunami, A; Yamamoto, N; Yamasaki, Y, 1990)	1.29
"Mofezolac also has a potent inhibitory activity on the algesic responses induced by the mechanical stimulus of the inflammed tissue."	( [Pharmacological profile of mofezolac, a new non-steroidal analgesic anti-inflammatory drug]. Miyake, H; Ono, N; Sunami, A; Yamamoto, N; Yamasaki, Y, 1990)	1.29

Excerpt	Reference	Relevance
"Mofezolac was chosen because is the most potent and selective reversible COX-1 inhibitor [COX-1 IC"	( Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability. Boccarelli, A; Cabral, LM; de Pádula, M; Di Mauro, GD; Ferorelli, S; Fortuna, CG; Iaselli, M; Miciaccia, M; Pati, ML; Perrone, MG; Rodrigues Pereira da Silva, LC; Sathler, PC; Scilimati, A; Souza Domingos, TF; Vacca, A; Vitale, P, 2019)	1.47

Excerpt	Reference	Relevance
" LD50 values of N-22 in mice were 1528 mg/kg (p."	( Acute toxicity tests of mofezolac (N-22) in mice and rats. Ichiki, T; Kodama, R; Kuwasaki, E; Kuwata, M; Satoh, K; Sone, H; Yamamoto, N; Yamashita, K, 1990)	0.59
" Toxic signs caused by N-22 administration, observed only in the 200 mg/kg group, were as follows: soiling around the mouth and/or nose, piloerection, anemia, diarrhea, emaciation and decreased spontaneous locomotor activity."	( [Three-month oral subacute toxicity study of mofezolac (N-22) in rats]. Aoki, Y; Hashimoto, Y; Kiguchi, M; Kuwata, M; Okazaki, S; Shimpo, K; Takeuchi, M; Yamashita, K, 1990)	0.54

Excerpt	Reference	Relevance
"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

Excerpt	Relevance	Reference
"2%) of chromosomes were observed in the groups of dosing 600 micrograms/ml with dose dependency."	( Mutagenicity tests of mofezolac (N-22). Furukawa, A; Ohuchida, A, 1990)	0.59
" Respectively 3 dogs of both sexes receiving 20 mg/kg/day died during dosing period."	( [Three-month subacute oral toxicity study of mofezolac (N-22) in dogs]. Iwata, M; Kiguchi, M; Nasu, Y; Shimpo, K; Takeuchi, M; Yada, H; Yamashita, K, 1990)	0.54
" Male F344 rats were injected subcutaneously with 15 mg/kg body weight of AOM in the back twice at 7-day intervals from 5 weeks of age, and fed a diet containing 600 or 1200 ppm mofezolac for 32 weeks, starting 1 day before the first dosing of AOM."	( Suppression of azoxymethane-induced colon cancer development in rats by a cyclooxygenase-1 selective inhibitor, mofezolac. Kitamura, T; Matsuura, M; Mutoh, M; Niho, N; Sato, H; Sugimura, T; Takahashi, M; Wakabayashi, K, 2006)	0.74

Class	Description
methoxybenzenes	Any aromatic ether that consists of a benzene skeleton substituted with one or more methoxy groups.
[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)
AR protein	Homo sapiens (human)	Potency	6.6284	0.0002	21.2231	8,912.5098	AID743036; AID743053
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	2.1314	0.0002	29.3054	16,493.5996	AID743069; AID743075
geminin	Homo sapiens (human)	Potency	13.3359	0.0046	11.3741	33.4983	AID624297
peripheral myelin protein 22	Rattus norvegicus (Norway rat)	Potency	28.6954	0.0056	12.3677	36.1254	AID624032
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	39.8107	0.0096	10.5250	35.4813	AID1479145
ATP-dependent phosphofructokinase	Trypanosoma brucei brucei TREU927	Potency	56.2341	0.0601	10.7453	37.9330	AID492961
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Prostaglandin G/H synthase 1	Ovis aries (sheep)	IC50 (µMol)	0.0075	0.0003	2.1774	10.0000	AID1205447; AID1499553; AID1623328; AID1706790
Prostaglandin G/H synthase 1	Homo sapiens (human)	IC50 (µMol)	0.0036	0.0002	1.5574	10.0000	AID1492702; AID1709972; AID328205
Prostaglandin G/H synthase 2	Homo sapiens (human)	IC50 (µMol)	30.1760	0.0001	0.9950	10.0000	AID1492704; AID1623329; AID1706792; AID1709973; AID328206
Prostaglandin G/H synthase 2	Ovis aries (sheep)	IC50 (µMol)	25.2200	0.0010	1.4539	10.0000	AID1205448; AID1499554
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
prostaglandin biosynthetic process	Prostaglandin G/H synthase 1	Homo sapiens (human)
response to oxidative stress	Prostaglandin G/H synthase 1	Homo sapiens (human)
regulation of blood pressure	Prostaglandin G/H synthase 1	Homo sapiens (human)
cyclooxygenase pathway	Prostaglandin G/H synthase 1	Homo sapiens (human)
regulation of cell population proliferation	Prostaglandin G/H synthase 1	Homo sapiens (human)
cellular oxidant detoxification	Prostaglandin G/H synthase 1	Homo sapiens (human)
prostaglandin biosynthetic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
angiogenesis	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to oxidative stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
embryo implantation	Prostaglandin G/H synthase 2	Homo sapiens (human)
learning	Prostaglandin G/H synthase 2	Homo sapiens (human)
memory	Prostaglandin G/H synthase 2	Homo sapiens (human)
regulation of blood pressure	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of cell population proliferation	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to xenobiotic stimulus	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to nematode	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to fructose	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to manganese ion	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of vascular endothelial growth factor production	Prostaglandin G/H synthase 2	Homo sapiens (human)
cyclooxygenase pathway	Prostaglandin G/H synthase 2	Homo sapiens (human)
bone mineralization	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of prostaglandin biosynthetic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of fever generation	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of synaptic plasticity	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of synaptic transmission, dopaminergic	Prostaglandin G/H synthase 2	Homo sapiens (human)
prostaglandin secretion	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to estradiol	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to lipopolysaccharide	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of peptidyl-serine phosphorylation	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to vitamin D	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to heat	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to tumor necrosis factor	Prostaglandin G/H synthase 2	Homo sapiens (human)
maintenance of blood-brain barrier	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of protein import into nucleus	Prostaglandin G/H synthase 2	Homo sapiens (human)
hair cycle	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of apoptotic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of nitric oxide biosynthetic process	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of cell cycle	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of vasoconstriction	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of smooth muscle contraction	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of smooth muscle contraction	Prostaglandin G/H synthase 2	Homo sapiens (human)
decidualization	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Prostaglandin G/H synthase 2	Homo sapiens (human)
regulation of inflammatory response	Prostaglandin G/H synthase 2	Homo sapiens (human)
brown fat cell differentiation	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to glucocorticoid	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of calcium ion transport	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergic	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to fatty acid	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to mechanical stimulus	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to lead ion	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to ATP	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to hypoxia	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to non-ionic osmotic stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to fluid shear stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of transforming growth factor beta production	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesis	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of fibroblast growth factor production	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of brown fat cell differentiation	Prostaglandin G/H synthase 2	Homo sapiens (human)
positive regulation of platelet-derived growth factor production	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular oxidant detoxification	Prostaglandin G/H synthase 2	Homo sapiens (human)
regulation of neuroinflammatory response	Prostaglandin G/H synthase 2	Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress	Prostaglandin G/H synthase 2	Homo sapiens (human)
cellular response to homocysteine	Prostaglandin G/H synthase 2	Homo sapiens (human)
response to angiotensin	Prostaglandin G/H synthase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
peroxidase activity	Prostaglandin G/H synthase 1	Homo sapiens (human)
prostaglandin-endoperoxide synthase activity	Prostaglandin G/H synthase 1	Homo sapiens (human)
protein binding	Prostaglandin G/H synthase 1	Homo sapiens (human)
heme binding	Prostaglandin G/H synthase 1	Homo sapiens (human)
metal ion binding	Prostaglandin G/H synthase 1	Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygen	Prostaglandin G/H synthase 1	Homo sapiens (human)
peroxidase activity	Prostaglandin G/H synthase 2	Homo sapiens (human)
prostaglandin-endoperoxide synthase activity	Prostaglandin G/H synthase 2	Homo sapiens (human)
protein binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
enzyme binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
heme binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
protein homodimerization activity	Prostaglandin G/H synthase 2	Homo sapiens (human)
metal ion binding	Prostaglandin G/H synthase 2	Homo sapiens (human)
oxidoreductase activity, acting on single donors with incorporation of molecular oxygen, incorporation of two atoms of oxygen	Prostaglandin G/H synthase 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
photoreceptor outer segment	Prostaglandin G/H synthase 1	Homo sapiens (human)
cytoplasm	Prostaglandin G/H synthase 1	Homo sapiens (human)
endoplasmic reticulum membrane	Prostaglandin G/H synthase 1	Homo sapiens (human)
Golgi apparatus	Prostaglandin G/H synthase 1	Homo sapiens (human)
intracellular membrane-bounded organelle	Prostaglandin G/H synthase 1	Homo sapiens (human)
extracellular exosome	Prostaglandin G/H synthase 1	Homo sapiens (human)
cytoplasm	Prostaglandin G/H synthase 1	Homo sapiens (human)
neuron projection	Prostaglandin G/H synthase 1	Homo sapiens (human)
nuclear inner membrane	Prostaglandin G/H synthase 2	Homo sapiens (human)
nuclear outer membrane	Prostaglandin G/H synthase 2	Homo sapiens (human)
cytoplasm	Prostaglandin G/H synthase 2	Homo sapiens (human)
endoplasmic reticulum	Prostaglandin G/H synthase 2	Homo sapiens (human)
endoplasmic reticulum lumen	Prostaglandin G/H synthase 2	Homo sapiens (human)
endoplasmic reticulum membrane	Prostaglandin G/H synthase 2	Homo sapiens (human)
caveola	Prostaglandin G/H synthase 2	Homo sapiens (human)
neuron projection	Prostaglandin G/H synthase 2	Homo sapiens (human)
protein-containing complex	Prostaglandin G/H synthase 2	Homo sapiens (human)
neuron projection	Prostaglandin G/H synthase 2	Homo sapiens (human)
cytoplasm	Prostaglandin G/H synthase 2	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (95)

Assay ID	Title	Year	Journal	Article
AID1623376	Induction of apoptosis in human NCI-H929 cells assessed as early apoptotic cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 17.1%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1492703	Inhibition of human COX1 assessed as reduction in appearance of oxidized TMPD at 50 uM using arachidonic acid as substrate by colorimetric assay relative to control	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1623335	Anticoagulant activity in human platelet poor plasma assessed as activated partial thromboplastin time at 100 uM incubated for 15 mins at room temperature and subsequent incubation for 2 mins at 37 degreeC followed by cephalin addition and measured after	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623334	Antiplatelet activity in human platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation preincubated for 2 mins followed by arachidonic acid addition by turbidimetric method	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623401	Induction of apoptosis in human RPMI8226 cells assessed as late apoptotic cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 0.21%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623337	Hemolytic activity in erythrocytes (unknown origin) at 100 uM after 3 hrs by spectrophotometric analysis	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623414	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at S phase at 7.9 nM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1079949	Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1706795	Antiplatelet activity in human platelet-rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation by turbidimetric method	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1623342	Genotoxicity in Escherichia coli PQ35 at 500 uM after overnight incubation by SOS chromotest	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1706806	Mutagenicity in Escherichia coli PQ37 at 10 to 500 uM by SOS-chromotest	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1492700	Cell cycle arrest in human Caco2 cells assessed as accumulation at G2/M-phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1623379	Induction of apoptosis in human NCI-H929 cells assessed as viable cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 82.6%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623351	Potentiation of bortezomib-induced cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability at 7.9 nM after 48 hrs in presence of bortezomib by CCK8 assay	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623341	Mutagenicity in Salmonella typhimurium TA102 at 500 uM by Ames test	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1706802	Genotoxicity in Salmonella typhimurium TA98 at 10 to 500 uM by AMES test	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1499555	Selectivity ratio of IC50 for recombinant ovine COX2 catalytic activity to IC50 for ovine COX1 catalytic activity	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Structural basis for selective inhibition of Cyclooxygenase-1 (COX-1) by diarylisoxazoles mofezolac and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6).
AID1492701	Cell cycle arrest in human Caco2 cells assessed as accumulation at G0/G1-phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1623343	Genotoxicity in Escherichia coli PQ37 at 500 uM after overnight incubation by SOS chromotest	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1706803	Genotoxicity in Salmonella typhimurium TA100 at 10 to 500 uM by AMES test	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079935	Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1706801	Genotoxicity in Salmonella typhimurium TA97 at 10 to 500 uM by AMES test	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1492699	Cell cycle arrest in human Caco2 cells assessed as accumulation at S-phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1623374	Induction of apoptosis in human NCI-H929 cells assessed as necrotic cells at 7.9 nM after 48 hrs by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 0.0034%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1706798	Hemolytic activity against human erythrocytes assessed as hemolysis incubated for 3 hrs by spectrophotometric analysis relative to control	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1492707	Inhibition of COX1 in mouse BV2 cells assessed as reduction in LPS-stimulated PGE2 release by measuring PGE2 level at 0.5 uM preincubated for 1 hr followed by LPS addition measured after 48 hrs by immunoassay (Rvb = 0.7555 +/- 0.032 ng/ml)	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1079938	Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1706805	Mutagenicity in Escherichia coli PQ35 at 10 to 500 uM by SOS-chromotest	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1079933	Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1709973	Inhibition of COX2 (unknown origin)	2021	ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5	Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.
AID1706799	Cytotoxicity against African green monkey Vero cells at 10 uM measured after 48 hrs by MTT assay relative to control	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1623329	Inhibition of human COX2 using arachidonic acid as substrate by colorimetric assay	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623356	Cell cycle arrest in human NCI-H929 cells assessed as accumulation at G0/G1 phase at 7.9 nM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib alone	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1623353	Potentiation of bortezomib-induced cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability at 7.9 nM after 48 hrs in presence of bortezomib by CCK8 assay	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1079936	Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1623328	Inhibition of ovine COX1 using arachidonic acid as substrate by colorimetric assay	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623363	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at S phase at 7.9 nM after 48 hrs by propidium iodide/RNase staining based flow cytometric method	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1706796	Anticoagulant activity in human plasma assessed as activated partial thromboplastin time at 100 uM	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1492696	Permeability across basolateral to apical side in human Caco2 cells assessed as GLUT1-mediated drug transport by transportability method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1079934	Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1492702	Inhibition of human COX1 assessed as reduction in appearance of oxidized TMPD using arachidonic acid as substrate by colorimetric assay	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1205447	Inhibition of ovine COX-1 assessed as inhibition of PGH2 production using arachidonic acid as substrate by TMPD oxidation based colorimetric assay	2015	European journal of medicinal chemistry, Apr-13, Volume: 94	General role of the amino and methylsulfamoyl groups in selective cyclooxygenase(COX)-1 inhibition by 1,4-diaryl-1,2,3-triazoles and validation of a predictive pharmacometric PLS model.
AID1623377	Induction of apoptosis in human NCI-H929 cells assessed as late apoptotic cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 0.23%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623415	Cell cycle arrest in human RPMI8226 cells assessed as reduction in accumulation at G2/M phase at 7.9 nM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623336	Anticoagulant activity in human platelet poor plasma assessed as prothrombin time at 100 uM incubated for 15 mins at room temperature and subsequent incubation for 2 mins at 37 degreeC followed by PBS addition and measured after 3 mins for every secs in p	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623344	Cytotoxicity against human NCI-H929 cells assessed as reduction in cell viability at 7.9 nM after 48 hrs by CCK8 assay	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1079931	Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1623400	Induction of apoptosis in human RPMI8226 cells assessed as early apoptotic cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 1.05%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623338	Mutagenicity in Salmonella typhimurium TA97 at 500 uM by Ames test	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623340	Mutagenicity in Salmonella typhimurium TA100 at 500 uM by Ames test	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1205448	Inhibition of ovine COX-2 assessed as inhibition of PGH2 production using arachidonic acid as substrate by TMPD oxidation based colorimetric assay	2015	European journal of medicinal chemistry, Apr-13, Volume: 94	General role of the amino and methylsulfamoyl groups in selective cyclooxygenase(COX)-1 inhibition by 1,4-diaryl-1,2,3-triazoles and validation of a predictive pharmacometric PLS model.
AID1492691	Apparent permeability across basolateral to apical side in human Caco2 cells assessed as GLUT1-mediated drug transport at 100 uM after 120 mins by UV-Visible spectroscopic method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1623403	Induction of apoptosis in human RPMI8226 cells assessed as viable cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 98.7%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1709972	Inhibition of COX1 (unknown origin)	2021	ACS medicinal chemistry letters, May-13, Volume: 12, Issue:5	Development of Fluorescence Imaging Probes for Labeling COX-1 in Live Ovarian Cancer Cells.
AID1706790	Inhibition of ovine COX-1 assessed as peroxidase activity using arachidonic acid as substrate by colorimetric method	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1492695	Permeability across basolateral to apical side in human Caco2 cells assessed as GLUT1-mediated drug transport by immunofluorescence method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1706794	Selectivity index, ratio of IC50 for human COX-2 to IC50 for ovine COX-1	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1623378	Induction of apoptosis in human NCI-H929 cells assessed as necrotic cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 0.0034%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623372	Induction of apoptosis in human NCI-H929 cells assessed as early apoptotic cells at 7.9 nM after 48 hrs by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 17.1%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1706792	Inhibition of human COX-2 assessed as peroxidase activity using arachidonic acid as substrate by colorimetric method	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1623347	Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability at 42 nM after 48 hrs by CCK8 assay relative to control	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623373	Induction of apoptosis in human NCI-H929 cells assessed as late apoptotic cells at 7.9 nM after 48 hrs by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 0.23%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1706800	Cytotoxicity against African green monkey Vero cells at 100 uM measured after 48 hrs by MTT assay relative to control	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1492705	Inhibition of human COX2 assessed as reduction in appearance of oxidized TMPD at 50 uM using arachidonic acid as substrate by colorimetric assay relative to control	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1623402	Induction of apoptosis in human RPMI8226 cells assessed as necrotic cells at 7.9 nM after 48 hrs in presence of bortezomib by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 0.090%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623413	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at G0/G1 phase at 7.9 nM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID1499553	Inhibition of ovine COX1 catalytic activity using arachidonic acid as substrate preincubated for 5 mins followed by substrate and hemin addition measured after 2 mins by colorimetric method	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Structural basis for selective inhibition of Cyclooxygenase-1 (COX-1) by diarylisoxazoles mofezolac and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6).
AID1492704	Inhibition of human COX2 assessed as reduction in appearance of oxidized TMPD using arachidonic acid as substrate by colorimetric assay	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1492693	Apparent permeability across apical to basolateral side in human Caco2 cells at 100 uM after 120 mins by UV-Visible spectroscopic method	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1623357	Cell cycle arrest in human NCI-H929 cells assessed as accumulation at S phase at 7.9 nM in presence of bortezomib after 48 hrs by propidium iodide/RNase staining based flow cytometric method relative to bortezomib alone	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623362	Cell cycle arrest in human RPMI8226 cells assessed as accumulation at G0/G1 phase at 7.9 nM after 48 hrs by propidium iodide/RNase staining based flow cytometric method	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1623339	Mutagenicity in Salmonella typhimurium TA98 at 500 uM by Ames test	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1492706	Selectivity index, ratio of IC50 for inhibition of human COX2 to IC50 for inhibition of human COX1	2017	European journal of medicinal chemistry, Dec-01, Volume: 141	Effect of mofezolac-galactose distance in conjugates targeting cyclooxygenase (COX)-1 and CNS GLUT-1 carrier.
AID1706804	Genotoxicity in Salmonella typhimurium TA102 at 10 to 500 uM by AMES test	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
AID328206	Inhibition of COX2	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.
AID1499554	Inhibition of recombinant ovine COX2 catalytic activity using arachidonic acid as substrate preincubated for 5 mins followed by substrate and hemin addition measured after 2 mins by colorimetric method	2017	European journal of medicinal chemistry, Sep-29, Volume: 138	Structural basis for selective inhibition of Cyclooxygenase-1 (COX-1) by diarylisoxazoles mofezolac and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6).
AID1623375	Induction of apoptosis in human NCI-H929 cells assessed as viable cells at 7.9 nM after 48 hrs by Annexin-V/propidium iodide staining based flow cytometric method (Rvb = 82.6%)	2019	European journal of medicinal chemistry, Feb-15, Volume: 164	Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability.
AID328205	Inhibition of COX1	2008	Journal of medicinal chemistry, Apr-24, Volume: 51, Issue:8	Cyclooxygenase-1-selective inhibitors are attractive candidates for analgesics that do not cause gastric damage. design and in vitro/in vivo evaluation of a benzamide-type cyclooxygenase-1 selective inhibitor.
AID1706797	Anticoagulant activity in human plasma assessed as prothrombin time at 100 uM	2021	European journal of medicinal chemistry, Jan-01, Volume: 209	An attempt to chemically state the cross-talk between monomers of COX homodimers by double/hybrid inhibitors mofezolac-spacer-mofezolac and mofezolac-spacer-arachidonic acid.
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.
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.
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.
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	2 (5.26)	18.7374
1990's	16 (42.11)	18.2507
2000's	8 (21.05)	29.6817
2010's	7 (18.42)	24.3611
2020's	5 (13.16)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	40 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
aspirin Aspirin: The prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5). acetylsalicylate : A benzoate that is the conjugate base of acetylsalicylic acid, arising from deprotonation of the carboxy group.. acetylsalicylic acid : A member of the class of benzoic acids that is salicylic acid in which the hydrogen that is attached to the phenolic hydroxy group has been replaced by an acetoxy group. A non-steroidal anti-inflammatory drug with cyclooxygenase inhibitor activity.	3.2	5	benzoic acids; phenyl acetates; salicylates	anticoagulant; antipyretic; cyclooxygenase 1 inhibitor; cyclooxygenase 2 inhibitor; drug allergen; EC 1.1.1.188 (prostaglandin-F synthase) inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug; plant activator; platelet aggregation inhibitor; prostaglandin antagonist; teratogenic agent
celecoxib [no description available]	2.52	2	organofluorine compound; pyrazoles; sulfonamide; toluenes	cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug
indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.	2.73	3	aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole	analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic
nimesulide nimesulide: structure. nimesulide : An aromatic ether having phenyl and 2-methylsulfonamido-5-nitrophenyl as the two aryl groups.	2.42	2	aromatic ether; C-nitro compound; sulfonamide	cyclooxygenase 2 inhibitor; non-steroidal anti-inflammatory drug
n-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide N-(2-cyclohexyloxy-4-nitrophenyl)methanesulfonamide: structure given in first source. NS-398 : A C-nitro compound that is N-methylsulfonyl-4-nitroaniline bearing an additional cyclohexyloxy substituent at position 2.	2.71	3	aromatic ether; C-nitro compound; sulfonamide	antineoplastic agent; cyclooxygenase 2 inhibitor
4-nitroquinoline-1-oxide 4-nitroquinoline N-oxide : A quinoline N-oxide carrying a nitro substituent at position 4.	2.66	2	C-nitro compound; quinoline N-oxide	carcinogenic agent
galactose galactopyranose : The pyranose form of galactose.	7.15	1	D-galactose; galactopyranose	Escherichia coli metabolite; mouse metabolite
isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent.	9.77	31	isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
oxazoles Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.	2.89	4	1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
phenylbenzoquinone phenylbenzoquinone: RN given refers to parent cpd	2.4	2
azoxymethane Azoxymethane: A potent carcinogen and neurotoxic compound. It is particularly effective in inducing colon carcinomas.	7.42	2
jte 522 tiracoxib: The combined administration of tiracoxib with probucol significantly inhibited the tumor growth. The angiogenesis was markedly reduced; no further information available 1/31/2001. tilmacoxib : A member of the class of 1,3-oxazoles that is that is 1,3-oxazole which is substituted at positions 2, 4 and 5 by methyl, cyclohexyl, and 3-fluoro-4-sulfamoylphenyl groups, respectively.	2.01	1	1,3-oxazoles; organofluorine compound; sulfonamide	cyclooxygenase 2 inhibitor
fr 122047 [no description available]	2.04	1	aromatic amide; thiazoles
bortezomib [no description available]	7.21	1	amino acid amide; L-phenylalanine derivative; pyrazines	antineoplastic agent; antiprotozoal drug; protease inhibitor; proteasome inhibitor
arachidonic acid icosa-5,8,11,14-tetraenoic acid : Any icosatetraenoic acid with the double bonds at positions 5, 8, 11 and 14.. arachidonate : A long-chain fatty acid anion resulting from the removal of a proton from the carboxy group of arachidonic acid.	7.31	1	icosa-5,8,11,14-tetraenoic acid; long-chain fatty acid; omega-6 fatty acid	Daphnia galeata metabolite; EC 3.1.1.1 (carboxylesterase) inhibitor; human metabolite; mouse metabolite
ovalbumin Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.	1.97	1
sc 560 SC560 : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3 and 5 by 4-methoxyphenyl, trifluoromethyl and 4-chlorophenyl groups, respectively. Unlike many members of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors, SC-560 is selective for COX-1.	2.93	3	aromatic ether; monochlorobenzenes; organofluorine compound; pyrazoles	angiogenesis modulating agent; antineoplastic agent; apoptosis inducer; cyclooxygenase 1 inhibitor; non-steroidal anti-inflammatory drug
dinoprostone prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.	2.02	1	prostaglandins E	human metabolite; mouse metabolite; oxytocic
thromboxane a2 Thromboxane A2: An unstable intermediate between the prostaglandin endoperoxides and thromboxane B2. The compound has a bicyclic oxaneoxetane structure. It is a potent inducer of platelet aggregation and causes vasoconstriction. It is the principal component of rabbit aorta contracting substance (RCS).. thromboxane A2 : A thromboxane which is produced by activated platelets and has prothrombotic properties: it stimulates activation of new platelets as well as increases platelet aggregation.	2.02	1	epoxy monocarboxylic acid; thromboxanes A	mouse metabolite
6-ketoprostaglandin f1 alpha 6-Ketoprostaglandin F1 alpha: The physiologically active and stable hydrolysis product of EPOPROSTENOL. Found in nearly all mammalian tissue.. 6-oxoprostaglandin F1alpha : A prostaglandin Falpha that is prostaglandin F1alpha bearing a keto substituent at the 6-position.	1.99	1	prostaglandins Falpha	human metabolite; mouse metabolite
4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1h-pyrazol-1-yl)benzenesulfonamide 4-(5-(4-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide: a long-acting COX-2 inhibitor; structure in first source. mavacoxib : A member of the class of pyrazoles that is 1H-pyrazole which is substituted at positions 1, 3 and 5 by 4-sulfamoylphenyl, trifluoromethyl and 4-fluorophenyl groups, respectively. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine to treat pain and inflammation in dogs with degenerative joint disease.	2.31	1	organofluorine compound; pyrazoles; sulfonamide	cyclooxygenase 2 inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug
rivaroxaban Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.	2.21	1	aromatic amide; lactam; monocarboxylic acid amide; morpholines; organochlorine compound; oxazolidinone; thiophenes	anticoagulant; EC 3.4.21.6 (coagulation factor Xa) inhibitor
fk 881 3-methoxy-1,5-bis(4-methoxyphenyl)-1H-1,2,4-triazole: structure in first source	2.58	2
3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole: inhibits cyclooxygenase-1; structure in first source	7.53	2

Condition	Relationship Strength	Studies
Kahler Disease [description not available]	2.21	1
Multiple Myeloma A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.	7.21	1
Blood Clot [description not available]	2.31	1
Thrombosis Formation and development of a thrombus or blood clot in the blood vessel.	2.31	1
Acute Ischemic Stroke [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.73	3
Ischemic Stroke Stroke due to BRAIN ISCHEMIA resulting in interruption or reduction of blood flow to a part of the brain. When obstruction is due to a BLOOD CLOT formed within in a cerebral blood vessel it is a thrombotic stroke. When obstruction is formed elsewhere and moved to block a cerebral blood vessel (see CEREBRAL EMBOLISM) it is referred to as embolic stroke. Wake-up stroke refers to ischemic stroke occurring during sleep while cryptogenic stroke refers to ischemic stroke of unknown origin.	2.25	1
Cancer of Ovary [description not available]	2.21	1
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	2.21	1
Bone Loss, Osteoclastic [description not available]	2.05	1
Cancer of Intestines [description not available]	2.42	2
Intestinal Neoplasms Tumors or cancer of the INTESTINES.	2.42	2
Carcinoma, Lewis Lung A carcinoma discovered by Dr. Margaret R. Lewis of the Wistar Institute in 1951. This tumor originated spontaneously as a carcinoma of the lung of a C57BL mouse. The tumor does not appear to be grossly hemorrhagic and the majority of the tumor tissue is a semifirm homogeneous mass. (From Cancer Chemother Rep 2 1972 Nov;(3)1:325) It is also called 3LL and LLC and is used as a transplantable malignancy.	2.01	1
Angiogenesis, Pathologic [description not available]	2.01	1
Sarcoma 180 An experimental sarcoma of mice.	2.01	1
Experimental Neoplasms [description not available]	2.02	1
Intestinal Polyps Discrete abnormal tissue masses that protrude into the lumen of the INTESTINE. A polyp is attached to the intestinal wall either by a stalk, pedunculus, or by a broad base.	2.02	1
Rheumatoid Arthritis [description not available]	2.02	1
Arthritis, Rheumatoid A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.	2.02	1
Carcinoma, Anaplastic [description not available]	2.03	1
Cancer of Colon [description not available]	2.03	1
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	2.03	1
Colonic Neoplasms Tumors or cancer of the COLON.	2.03	1
Ache [description not available]	2.4	2
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	7.4	2
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	2.67	3
Adjuvant Arthritis [description not available]	1.97	1
Anasarca [description not available]	1.97	1
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	1.97	1
Cholera Infantum [description not available]	2.38	2
Ileal Diseases Pathological development in the ILEUM including the ILEOCECAL VALVE.	1.97	1
Jejunal Diseases Pathological development in the JEJUNUM region of the SMALL INTESTINE.	1.97	1
Ulcer A lesion on the surface of the skin or a mucous surface, produced by the sloughing of inflammatory necrotic tissue.	2.38	2
Weight Gain Increase in BODY WEIGHT over existing weight.	2.38	2
Intestinal Diseases Pathological processes in any segment of the INTESTINE from DUODENUM to RECTUM.	1.97	1
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	7.89	4
Abnormalities, Drug-Induced Congenital abnormalities caused by medicinal substances or drugs of abuse given to or taken by the mother, or to which she is inadvertently exposed during the manufacture of such substances. The concept excludes abnormalities resulting from exposure to non-medicinal chemicals in the environment.	2.38	2
Fetal Resorption The disintegration and assimilation of the dead FETUS in the UTERUS at any stage after the completion of organogenesis which, in humans, is after the 9th week of GESTATION. It does not include embryo resorption (see EMBRYO LOSS).	1.97	1
Fetal Death Death of the developing young in utero. BIRTH of a dead FETUS is STILLBIRTH.	1.97	1
Abnormalities, Autosome [description not available]	1.97	1
Chromosome-Defective Micronuclei [description not available]	1.97	1
Anaphylactic Reaction [description not available]	1.97	1
Anaphylaxis An acute hypersensitivity reaction due to exposure to a previously encountered ANTIGEN. The reaction may include rapidly progressing URTICARIA, respiratory distress, vascular collapse, systemic SHOCK, and death.	1.97	1
Chronic Illness [description not available]	1.97	1
Anemia A reduction in the number of circulating ERYTHROCYTES or in the quantity of HEMOGLOBIN.	1.97	1
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	1.97	1
Kidney Diseases Pathological processes of the KIDNEY or its component tissues.	1.97	1
Curling Ulcer Acute stress DUODENAL ULCER, usually observed in patients with extensive third-degree burns.	1.97	1
Gastric Ulcer [description not available]	1.97	1
Duodenal Ulcer A PEPTIC ULCER located in the DUODENUM.	1.97	1
Stomach Ulcer Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).	1.97	1

mofezolac

Description

Cross-References

Synonyms (67)

Research Excerpts

Overview

Effects

Actions

Toxicity

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (10)

Potency Measurements

Inhibition Measurements

Biological Processes (60)

Molecular Functions (8)

Ceullar Components (14)

Bioassays (95)

Research

Studies (38)

Market Indicators

Research Demand Index: 23.25

Study Types

mofezolac

Description

Cross-References

Synonyms (67)

Research Excerpts

Overview

Effects

Actions

Toxicity

Bioavailability

Dosage Studied

Drug Classes (1)

Protein Targets (10)

Potency Measurements

Inhibition Measurements

Biological Processes (60)

Molecular Functions (8)

Ceullar Components (14)

Bioassays (95)

Research

Studies (38)

Market Indicators

Research Demand Index: 23.25

Study Types

Related Drugs (24)

Related Conditions (51)