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tranilast

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Description

tranilast: antiallergic drug; potent inhibitor of homologous passive cutaneous anaphylaxis [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

tranilast : An amidobenzoic acid that is anthranilic acid in which one of the anilino hydrogens is replaced by a 3,4-dimethoxycinnamoyl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5282230
CHEMBL ID415324
CHEBI ID77572
CHEBI ID92320
SCHEMBL ID29875
MeSH IDM0059240

Synonyms (147)

Synonym
AC-940
MLS001077269
AB00382987-19
BRD-K17849083-001-02-2
MLS000028468 ,
tranilast
smr000058373
rizaben
sb-252218
nu-3450
2-({(2e)-3-[3,4-bis(methyloxy)phenyl]prop-2-enoyl}amino)benzoic acid
EU-0101193
tranilast, >=98% (hplc), powder
anthranilic acid, n-(3,4-dimethoxycinnamoyl)-
tranilast [usan:inn:jan]
benzoic acid, 2-((3-(3,4-dimethoxyphenyl)-1-oxo-2-propenyl)amino)-
tranilastum [inn-latin]
2-((3-(3,4-dimethoxyphenyl)-1-oxo-2-propenyl)amino)benzoic acid
n-(3',4'-dimethoxycinnamoyl) anthranilic acid
mk 341
n-(3,4-dimethoxycinnamoyl)anthranilic acid
BSPBIO_003561
LOPAC0_001193
HSCI1_000076
D27 ,
bdbm21613
n-(3 ,4 -dimethoxycinnamoyl)anthranilic acid
2-{[(2e)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino}benzoic acid
2-[(2e)-3-(3,4-dimethoxyphenyl)prop-2-enamido]benzoic acid
MLS000759509
rizaben (tn)
D02027
tranilast (jp17/usan/inn)
53902-12-8
SPECTRUM1505333
NCGC00021458-04
NCGC00021458-07
NCGC00021458-05
MLS001065902
NCGC00018185-05
HMS2051F05
T 0318 ,
HMS2089L07
HMS2094I21
NCGC00018185-09
MLS002207030
DB07615
nsc-758970
CHEMBL415324
chebi:77572 ,
mk-341
2-[[3-(3,4-dimethoxyphenyl)-1-oxo-2-propen-1-yl]amino]benzoic acid
AKOS002841076
2-[3-(3,4-dimethoxyphenyl)prop-2-enoylamino]benzoic acid
NCGC00018185-04
NCGC00018185-08
NCGC00018185-10
NCGC00018185-06
HMS3263P07
2-[[(e)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino]benzoic acid
n-(3',4'-dimethoxycinnamoyl)anthranilic acid
(e)-2-(3-(3,4-dimethoxyphenyl)acrylamido)benzoic acid
A829819
nsc758970
pharmakon1600-01505333
MLS001424045
cas-53902-12-8
dtxsid7023693 ,
dtxcid403693
tox21_110836
HMS2230F18
CCG-39992
sb 252218
tranpro
hvf50smy6e ,
nsc 758970
unii-hvf50smy6e
tranilastum
LP01193
S5871
gtpl6326
BRD-K19533706-001-01-9
tranilast [usan]
n-5'
tranilast [mart.]
tranilast [mi]
tranilast [who-dd]
tranilast [inn]
tranilast [jan]
HY-B0195
MLS006010043
NC00171
2-[[3-(3,4-dimethoxyphenyl)-1-oxo-2-propenyl]amino]benzoic acid
SCHEMBL29875
KS-1193
AB00382987-18
tox21_501193
NCGC00261878-01
53902-17-3
(e)-2-[[3-(3,4-dimethoxyphenyl)-1-oxo-2-propenyl]amino]benzoic acid
70806-55-2
Q-201849
AC-35254
HB1201
(2-phenylthiazol-5-yl)methylamine
trans-tranilast
HMS3648A16
OPERA_ID_1657
AB00382987_21
mfcd00864787
benzoic acid, 2-[[3-(3,4-dimethoxyphenyl)-1-oxo-2-propenyl]amino]-
tranilast (trans-)
tranilast trans-
CHEBI:92320
SR-01000003092-2
sr-01000003092
SR-01000003092-4
SR-01000003092-9
SBI-0051160.P003
NCGC00018185-20
HMS3713J04
tranilast (sb 252218)
SW197551-3
BCP15888
sb252218
BCP06359
2-[[3-(3,4-dimethoxyphenyl)-1-oxoprop-2-enyl]amino]benzoic acid
Q27164069
S1439
2-(3-(3,4-dimethoxyphenyl)acrylamido)benzoic acid
HMS3676G17
SR-01000003092-16
HMS3412G17
Q2325594
AMY14167
BRD-K17849083-001-03-0
SDCCGSBI-0051160.P004
NCGC00018185-26
mk 341;sb 252218
NCGC00018185-23
2-[3-(3,4-dimethoxyphenyl)-acryloylamino]-benzoic acid
2-(3,4-dimethoxy-trans-cinnamoylamino)benzoic acid
A923780
benzoic acid,2-[[3-(3-methoxy-4-propoxyphenyl)-1-oxo-2-propenyl]amino]-
tranilast- bio-x
BD164491
tranilast; 2-[[3-(3,4-dimethoxyphenyl)-1-oxo-2-propenyl]amino] benzoic acid

Research Excerpts

Overview

Tranilast (TRA) is an anti-allergic drug used to treat bronchial asthma and allergic rhinitis. Tranilast is a potential NLRP3 inflammasome inhibitor that may relieve progressive inflammation due to COVID-19.

ExcerptReferenceRelevance
"Tranilast is an anti-inflammatory drug in use for asthma and atopic dermatitis. "( Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates.
Cox, AJ; Gilbert, RE; Gow, RM; Kelly, DJ; Krum, H; Williams, SJ; Zammit, SC; Zhang, Y, 2009
)
1.8
"Tranilast is a potential NLRP3 inflammasome inhibitor that may relieve progressive inflammation due to COVID-19."( Tranilast as an Adjunctive Therapy in Hospitalized Patients with Severe COVID- 19: A Randomized Controlled Trial.
Ghadiri, AA; Hanafi, MG; Khodadadi, A; Mahmoudian-Sani, MR; Nakajima, M; Nashibi, R; Saeedi-Boroujeni, A; Salmanzadeh, S; Sharhani, A, 2022
)
3.61
"Tranilast is an antiallergic drug that suppresses the release of cytokines from various inflammatory cells."( Drug repositioning of tranilast to sensitize a cancer therapy by targeting cancer-associated fibroblast.
Nakata, K; Ochi, K; Okamoto, Y; Okazaki, M; Shien, K; Shien, T; Sugimoto, S; Suzawa, K; Takatsu, F; Takeda, T; Thu, YM; Tomida, S; Toyooka, S; Tsudaka, S; Yamamoto, H; Zhu, Y, 2022
)
1.76
"Tranilast (TRA) is an anti-allergic drug used to treat bronchial asthma and allergic rhinitis."( Tranilast-matrine co-amorphous system: Strong intermolecular interactions, improved solubility, and physiochemical stability.
Chen, X; Duan, Y; Hu, D; Huang, Y; Li, D; Zhang, H, 2023
)
3.07
"Tranilast (TRAN) is a small molecular weight anti-inflammatory and antiallergic agent."( Tranilast attenuates methotrexate-induced renal and hepatic toxicities: Role of apoptosis-induced tissue proliferation.
Helal, MG; Said, E, 2020
)
2.72
"Tranilast is an anti-allergic drug that inhibits TGF-β1, and is used in the treatment of keloids and hypertrophic scars."( Tranilast Inhibits TGF-β1-induced Epithelial-mesenchymal Transition and Invasion/Metastasis
Chen-Yoshikawa, TF; Date, H; Hamaji, M; Menju, T; Miyata, R; Nakajima, D; Nishikawa, S; Ohsumi, A; Sato, T; Sonobe, M; Takahashi, K; Tanaka, S; Yamada, Y; Yutaka, Y, 2020
)
2.72
"Tranilast is an anti-allergy drug that has been shown to possess good antioxidant activity in previous studies."( Tranilast prevents doxorubicin-induced myocardial hypertrophy and angiotensin II synthesis in rats.
Bai, N; Li, G; Li, J; Li, L; Li, T; Li, W; Liu, G; Lou, Q; Wang, Y; Yang, W; Zhan, C; Zhang, L; Zhao, H; Zheng, M, 2021
)
2.79
"Tranilast is an anti-allergy agent that was developed in Japan."( Study Protocol for a Multicenter, Open-Label, Single-Arm Study of Tranilast for Cardiomyopathy of Muscular Dystrophy.
Asakura, M; Funato, M; Hashimoto, H; Iwata, Y; Kimura, K; Matsumura, T; Nakajima, T; Ogata, K; Saito, AM; Segawa, K; Sekimizu, M; Tamura, T, 2021
)
1.58
"Tranilast, which is an anti-fibrotic drug, is also suggested as an anti-angiogenesis agent."( Teucrium polium Extract Enhances the Anti-Angiogenic Effect of Tranilast in a Three-Dimensional Fibrin Matrix Model.
Khazaei, M; Khazaei, MR; Khazayel, S; Nematollahi-Mahani, SN; Sheikhbahaei, F, 2021
)
1.58
"Tranilast is an anti-allergy medication that inhibits the release of chemical mediators such as histamine. "( Tranilast inhibits interleukin-33 production by macrophages.
Hiraide, S; Iizuka, K; Yanagawa, Y, 2018
)
3.37
"Tranilast is a widely used antiallergic agent in the treatment against bronchial asthma and keloid."( Tranilast Treatment Attenuates Cerebral Ischemia-Reperfusion Injury in Rats Through the Inhibition of Inflammatory Responses Mediated by NF-κB and PPARs.
Zhuo, J; Zhuo, Y, 2019
)
2.68
"Tranilast (TR) is an anti-allergic medicine which has been used in Japan and South Korea in clinic."( Next target of tranilast: inhibition of corneal neovascularization.
Ahmadi, K; Norooznezhad, AH; Norooznezhad, F, 2014
)
1.48
"Tranilast is an anti-inflammatory drug."( Tamoxifen and tranilast show a synergistic effect against breast cancer in vitro.
Bidmeshki Pour, A; Darakhshan, S; Ghanbari, A; Gholami Rad, F, 2015
)
1.5
"Tranilast is a potential agent that accelerates fracture repair by promoting the regulatory steps of endochondral ossification."( Tranilast stimulates endochondral ossification by upregulating SOX9 and RUNX2 promoters.
Hasegawa, S; Ishiguro, N; Kitoh, H; Masuda, A; Matsushita, M; Mishima, K; Ohkawara, B; Ohno, K, 2016
)
2.6
"The tranilast molecule is a drug used for treating allergic disorders."( Tranilast Blocks the Interaction between the Protein S100A11 and Receptor for Advanced Glycation End Products (RAGE) V Domain and Inhibits Cell Proliferation.
Chou, RH; Huang, YK; Yu, C, 2016
)
2.36
"Tranilast is a therapeutic agent used in treatment of allergic diseases, although it has been reported to show anti-tumor effects on some cancer cells. "( Tranilast inhibits hormone refractory prostate cancer cell proliferation and suppresses transforming growth factor beta1-associated osteoblastic changes.
Izumi, K; Kadono, Y; Keller, ET; Kitagawa, Y; Koh, E; Konaka, H; Li, YQ; Mizokami, A; Namiki, M; Narimoto, K; Sugimoto, K, 2009
)
3.24
"Tranilast (TL) is an anti-allergic agent and widely used in the clinical treatment of bronchial asthma, atopic rhinitis, atopic dermatitis and keloids. "( Novel crystalline solid dispersion of tranilast with high photostability and improved oral bioavailability.
Debari, K; Kawabata, Y; Onoue, S; Yamada, S; Yamamoto, K, 2010
)
2.07
"Tranilast is an anti-allergic compound with a potent membrane-stabilizing effect on mast cells and a wide range of anti-inflammatory effects, thus may be advantageous in the treatment of arthritis."( The anti-allergic compound tranilast attenuates inflammation and inhibits bone destruction in collagen-induced arthritis in mice.
Eklund, KK; Kovanen, PT; Niibayashi, T; Okunishi, H; Shibata, N; Shimbori, C; Shimoura, K; Shiota, N, 2010
)
1.38
"Tranilast is a therapeutic agent used in treatment of allergic diseases. "( Preliminary results of tranilast treatment for patients with advanced castration-resistant prostate cancer.
Izumi, K; Kobori, Y; Koh, E; Konaka, H; Maeda, Y; Mizokami, A; Namiki, M; Narimoto, K; Shima, T; Sugimoto, K, 2010
)
2.11
"Tranilast is an anti-allergic compound suppressing transforming growth factor-beta 1 (TGF-β1) induced fibrosis. "( Tranilast modulates fibrosis, epithelial-mesenchymal transition and peritubular capillary injury in unilateral ureteral obstruction rats.
Aoyagi, D; Ehara, T; Kaneyama, T; Kobayashi, S, 2010
)
3.25
"Tranilast is an anti-allergic drug now emerging as anti-angiogenesis and anti-inflammatory effects."( Tranilast could has potential therapeutic value in the treatment of psoriasis.
Keshavarz, M; Mansouri, K; Motlagh, HR, 2011
)
2.53
"Tranilast is a well tolerated drug used in the treatment of allergic disorders."( Tranilast treatment decreases cell growth, migration and inhibits colony formation of human breast cancer cells.
Ace, O; Jothy, S; Prud'homme, GJ; Subramaniam, V, 2011
)
2.53
"Tranilast is an orally active drug of low toxicity that exerts inhibitory effects on breast CSCs."( Neuropilin-1 is expressed by breast cancer stem-like cells and is linked to NF-κB activation and tumor sphere formation.
Glinka, Y; Jothy, S; Mohammed, N; Prud'homme, GJ; Subramaniam, V, 2012
)
1.1
"Tranilast was concluded to be a potent agent to inhibit proliferative activity of uterine leiomyoma cells."( Tranilast inhibits the proliferation of uterine leiomyoma cells in vitro through G1 arrest associated with the induction of p21(waf1) and p53.
Fujii, S; Fukuhara, K; Kanamori, T; Kariya, M; Kusakari, T; Momma, C; Nikaido, T; Orii, A; Shime, H; Takakura, K; Tsuruta, Y, 2002
)
2.48
"Tranilast is a clinical drug for inhibition of fibroblast growth."( Tranilast (N-3,4-dimethoxycinamoyl anthranilic acid): a novel inhibitor of invasion-stimulating interaction between gastric cancer cells and orthotopic fibroblasts.
Chung, KH; Koyama, T; Matsuoka, T; Murahashi, K; Nakazawa, K; Ohira, M; Osaka, H; Tanaka, H; Yashiro, M,
)
2.3
"Tranilast is an anti-allergic agent known to inhibit the release of histamine, interleukin-1beta, transforming growth factor beta1, and platelet-derived growth factor from various cells and currently is used to treat allergic diseases, keloids, and hypertrophic scars. "( Anti-allergic agent tranilast decreases development of obliterative airway disease in rat model of heterotopic tracheal transplantation.
Hoshikawa, Y; Kondo, T; Matsuda, Y; Matsumura, Y; Okada, Y; Oyaizu, T; Sado, T; Sato, M; Shimada, K; Sugawara, T; Takahashi, H, 2004
)
2.09
"Tranilast is an anti-allergic drug which exerts anti-inflammatory and anti-angiogenesis effects through inhibition of expression of MCP-1, TGF-beta, and antigen-induced IL-2 lymphocyte responsiveness."( Tranilast: a novel weapon against insulin resistance.
Namazi, MR; Soma, J, 2005
)
2.49
"Tranilast is an anti-allergic agent that blocks the release of chemical mediators, such as histamine and leukotrienes from mast cells, and has been reported to suppress keloid and hypertrophic scar formation. "( Effect of tranilast on matrix metalloproteinase production from neutrophils in-vitro.
Asano, K; Hisamitsu, T; Kanai, K; Kyo, Y; Shimizu, T; Suzaki, H, 2006
)
2.18
"Tranilast is an antifibrotic drug known to suppress collagen synthesis by fibroblasts by interfering with the effects of TGF-beta. "( Effect of tranilast in early-stage diabetic nephropathy.
Saito, H; Sato, K; Soma, J; Tsuchiya, Y, 2006
)
2.18
"Tranilast is an oral antiallergic agent widely used in Japan. "( Glucuronidation of antiallergic drug, Tranilast: identification of human UDP-glucuronosyltransferase isoforms and effect of its phase I metabolite.
Katoh, M; Matsui, T; Yokoi, T, 2007
)
2.05
"Tranilast is an antiallergic drug that interferes with proliferation and migration of vascular smooth muscle cell induced by platelet-derived growth factor (PDGF) and transforming growth factor-beta1 (TGF-beta1). "( Evaluation of neointimal hyperplasia on tranilast-coated synthetic vascular grafts: an experimental study.
Akdur, A; Basaran, O; Haberal, M; Haberal, N; Hasirci, N; Karakayali, F; Kiziltay, A; Sevmis, S; Tufan, H,
)
1.84
"Tranilast which is a typical anti-histaminic drug most strongly inhibited the enzyme activity and the Ki value of the medicine was 20.3 microM (noncompetitive)."( Inhibition of bovine leukocyte thioltransferase by anti-inflammatory drugs and anti-histaminic drugs.
Mizoguchi, T; Mizuta, J; Nishnaka, T; Terada, T; Toya, H; Uchida, G; Uchida, H, 1993
)
1.01
"Tranilast is an orally effective anti-allergic agent evaluated for clinical activity in prevention of symptoms of allergic rhinitis. "( Clinical and pathophysiological evaluation of tranilast in patients with pollinosis: the effects of pre-seasonal treatment.
Masuda, S; Sakakura, Y; Shinoki, J; Ukai, K, 1993
)
1.99
"Tranilast is an anti-allergic drug clinically used for the treatment of atopy or urticaria. "( Treatment of cutaneous sarcoidosis with tranilast.
Ide, A; Sugiura, M; Tajima, S; Yamada, H, 1995
)
2
"Tranilast is a useful drug to reduce the proliferation of scirrhous gastric carcinoma."( Tranilast (N-(3,4-dimethoxycinnamoyl) anthranilic acid) down-regulates the growth of scirrhous gastric cancer.
Chung, YS; Sowa, M; Yashiro, M,
)
3.02
"Tranilast is an antiallergic drug used widely in Japan that also inhibits the migration and proliferation of vascular smooth muscle cells. "( Effectiveness of tranilast on restenosis after directional coronary atherectomy.
Doi, T; Hsu, YS; Kosuga, K; Motohara, S; Myou-U, W; Ono, S; Tamai, H; Tanaka, S; Ueda, K; Uehata, H, 1997
)
2.08
"Tranilast, which is an antiallergic drug, has a potent effect on preventing postangioplasty restenosis. "( Tranilast inhibits vascular smooth muscle cell growth and intimal hyperplasia by induction of p21(waf1/cip1/sdi1) and p53.
Ishikawa, Y; Takahashi, A; Taniguchi, T; Yokoyama, M, 1999
)
3.19
"Tranilast is an antiallergic drug that suppresses the release of cytokines such as platelet-derived growth factor, transforming growth factor-beta1, and interleukin-1beta and prevents keloid formation after skin injury. "( Impact of tranilast on restenosis after coronary angioplasty: tranilast restenosis following angioplasty trial (TREAT).
Aizawa, T; Fujii, K; Katoh, O; Kurogane, H; Nishikawa, H; Sakai, K; Sone, T; Suzuki, S; Suzuki, T; Takase, Si; Tamai, H, 1999
)
2.15
"Tranilast is a unique drug in clinical development for the prevention of restenosis after percutaneous transluminal coronary revascularization (PTCR). "( The PRESTO (Prevention of restenosis with tranilast and its outcomes) protocol: a double-blind, placebo-controlled trial.
Chan, R; Fitzgerald, P; Goldberg, S; Granett, JR; Holmes, D; LaBlanche, Jm; Lincoff, AM; Poland, M; Savage, M; Serruys, PW; Shusterman, NH; Willerson, J, 2000
)
2.01
"Tranilast is an anti-allergic drug. "( [Antiallergic effects of tranilast in rats and guinea pigs].
Cai, S; Chen, J; Xie, Q; Ye, S; Yu, F, 1997
)
2.04
"Tranilast (SB 252218) is a compound initially identified as an anti-atopic agent. "( Modulation of human monocyte activities by tranilast, SB 252218, a compound demonstrating efficacy in restenosis.
Anderson, KM; Bolognese, BJ; Capper, EA; Dewitt, DL; Marshall, LA; Podolin, PL; Roshak, AK; Smith, T, 2000
)
2.01
"Tranilast is an anti-allergic drug that inhibits the release of chemical mediators from mast cells. "( Inhibitory influences of tranilast on multinucleated giant cell formation from monocytes by supernatant of concanavalin A-stimulated mononuclear cells.
Horio, T; Mizuno, K; Okamoto, H, 2000
)
2.05
"Tranilast is a promising drug that may prevent post-angioplasty restenosis."( Tranilast inhibits transplant-associated coronary arteriosclerosis in a murine model of cardiac transplantation.
Hirata, Y; Makuuchi, M; Nagai, R; Saiura, A; Sata, M, 2001
)
2.47
"Tranilast is an oral antiallergic agent developed in Japan. "( The effects of long term Tranilast administration on bronchial hypersensitivity in asthmatics.
Kaneshige, H; Nakagami, K; Noguchi, E; Suzuki, H; Tanaka, K,
)
1.88

Effects

Tranilast has a renoprotective effect on adriamycin-induced nephrotic syndrome in rats. Tranilast can depress the expression of TGF-beta1, and TIMP-1 in the kidney.

Tranilast has been used in allergic diseases because of its inhibitory effect on mast cells. It also has an anti-fibrotic effect in several diseases. Tranilast exerts anti-oxidative stress effects in diabetic nephropathy.

ExcerptReferenceRelevance
"Tranilast has an ameliorative effect on myocardial fibrosis (MF), but the specific mechanism has not been studied. "( Tranilast inhibits angiotensin II-induced myocardial fibrosis through S100A11/ transforming growth factor-β (TGF-β1)/Smad axis.
Chen, Y; He, D; Huang, M; Yan, Y, 2021
)
3.51
"Tranilast has a renoprotective effect on adriamycin-induced nephrotic syndrome in rats, of which the mechanism may be related to that tranilast can depress the expression of TGF-beta1, and TIMP-1 in the kidney, with result in decreasing the synthesis and secretion of extracellular matrix. "( [Experimental study in renal protective effect of tranilast on rats with adriamycin nephropathy].
Bo, H; Li, DD; Liu, QF; Tao, Y; Wang, XR; Wu, X, 2008
)
2.04
"Tranilast has an ameliorative effect on myocardial fibrosis (MF), but the specific mechanism has not been studied. "( Tranilast inhibits angiotensin II-induced myocardial fibrosis through S100A11/ transforming growth factor-β (TGF-β1)/Smad axis.
Chen, Y; He, D; Huang, M; Yan, Y, 2021
)
3.51
"Tranilast has efficacy on the inhibition of degranulation and IL-13 production in BMMCs induced by the combination of DNP-BSA and IL-33."( Inhibition by Tranilast of the Synergistic Induction of Degranulation and IL-13 Expression by IL-33 and FcɛRI Cross-linking in Mast Cells.
Fukuda, K; Fukushima, A; Tsuji, K, 2017
)
2.26
"Tranilast has been used in allergic diseases because of its inhibitory effect on mast cells; it also has an anti-fibrotic effect in several diseases. "( Effects of tranilast and pentoxifylline in a mouse model of chronic asthma using house dust mite antigen.
Ahn, JH; Kim, CH; Kim, JS; Kim, JW; Kim, SC; Kim, SJ; Kim, YH; Kim, YK; Kwon, SS; Lee, JM; Lee, SH; Lee, SY; Yoon, HK, 2009
)
2.19
"Tranilast has been reported to not only act as an anti-inflammatory and anti-fibrotic compound, but it also exerts anti-oxidative stress effects in diabetic nephropathy."( Tranilast attenuates the up-regulation of thioredoxin-interacting protein and oxidative stress in an experimental model of diabetic nephropathy.
Cox, AJ; Kelly, DJ; Qi, W; Tan, SM; Zhang, Y, 2011
)
2.53
"Tranilast (TL) has been clinically used for the treatment of airway inflammatory diseases, although the clinical use of TL is limited because of its poor solubility and systemic side effects. "( Stable dry powder inhaler formulation of tranilast attenuated antigen-evoked airway inflammation in rats.
Aoki, Y; Kawabata, Y; Matsui, T; Onoue, S; Sato, H; Yamada, S; Yamamoto, K, 2011
)
2.08
"Tranilast has been shown to inhibit TGFβ1-related fibrosis and organ failure in various disease models. "( Early and delayed tranilast treatment reduces pathological fibrosis following myocardial infarction.
Boyle, AJ; Gilbert, RE; Kelly, DJ; Kompa, AR; Krum, H; See, F; Wang, BH; Watanabe, M, 2013
)
2.17
"Tranilast has been described as an effective treatment for cases of MRS, granulomatous cheilitis, and granulomatous blepharitis."( A case of vulvitis granulomatosa.
Katsuoka, K; Masuzawa, M; Tsuboi, H, 2005
)
1.05
"Tranilast has been reported to be mainly metabolized to a glucuronide and a phase I metabolite, 4-demethyltranilast (N-3)."( Glucuronidation of antiallergic drug, Tranilast: identification of human UDP-glucuronosyltransferase isoforms and effect of its phase I metabolite.
Katoh, M; Matsui, T; Yokoi, T, 2007
)
1.33
"Tranilast has a renoprotective effect on adriamycin-induced nephrotic syndrome in rats, of which the mechanism may be related to that tranilast can depress the expression of TGF-beta1, and TIMP-1 in the kidney, with result in decreasing the synthesis and secretion of extracellular matrix. "( [Experimental study in renal protective effect of tranilast on rats with adriamycin nephropathy].
Bo, H; Li, DD; Liu, QF; Tao, Y; Wang, XR; Wu, X, 2008
)
2.04
"Tranilast has been reported to reduce restenosis rate after angioplasty, but its mechanism is still unclear. "( Tranilast restores cytokine-induced nitric oxide production against platelet-derived growth factor in vascular smooth muscle cells.
Hirahashi, J; Hishikawa, K; Marumo, T; Nakaki, T; Saruta, T, 1996
)
3.18
"Tranilast has been clinically used for various allergic diseases. "( The effect of tranilast on experimental proliferative vitreoretinopathy.
Akazawa, K; Goto, Y; Inomata, H; Ishibashi, T; Ito, S; Sakamoto, T; Tahara, Y, 1999
)
2.11
"Tranilast, which has antikeloid and antiallergic properties and therefore may modulate the fibrotic and inflammatory tissue responses to angioplasty and stenting, has been shown to inhibit angiographic restenosis in small clinical trials. "( Inhibition of neointima formation by tranilast in pig coronary arteries after balloon angioplasty and stent implantation.
Chronos, NA; de Leon, H; Ishiwata, S; King, SB; Robinson, KA; Salame, MY; Verheye, S, 2000
)
2.02
"Tranilast has long been used clinically to treat allergic diseases such as bronchial asthma. "( Suppressive effect of tranilast on interleukin-5 prolonged eosinophils survival via apoptosis.
Cheng, G; Eda, F; Fukuda, T; Ishii, Y; Kinjyo, S; Nakajima, H; Ueda, T, 2001
)
2.07

Actions

Tranilast can inhibit the infiltration of mast cells in the kidneys of DKD rats. Tranilast could inhibit TGF-beta(2) expression in cultured human trabecular meshwork cells.

ExcerptReferenceRelevance
"Tranilast likely promotes fibrillation by shifting Aβ monomer conformations to those capable of seed formation and fibril elongation."( Tranilast binds to aβ monomers and promotes aβ fibrillation.
Belfort, G; Bitan, G; Connors, CR; Garcia, A; Lopes, DH; Mittal, S; Rosenman, DJ; Sorci, M; Wang, C, 2013
)
2.55
"Tranilast can inhibit the infiltration of mast cells in the kidneys of DKD rats. "( [Role and mechanism of tranilast preventing the progression of tubulointerstilial fibrosis in diabetic kidney diseases].
Duan, S; Li, H; Li, J; Li, Y; Liu, F; Liu, H; Liu, Y; Luo, J; Sun, L; Xi, Y; Yang, Y; You, Y, 2013
)
2.14
"Tranilast may inhibit the aggregation of MC and down-regulate the expression of CTGF, relieving myocardial fibrosis of mice with VMC."( [Tranilast inhibits myocardial fibrosis in mice with viral myocarditis].
Chen, CY; Huang, LF; Wen, C; Xie, G; Zeng, P, 2016
)
2.79
"Tranilast is known to suppress fibrosis or to work as a mast cell stabilizer and is reported to inhibit proliferation of vascular smooth muscle cells."( Tranilast inhibits the proliferation of uterine leiomyoma cells in vitro through G1 arrest associated with the induction of p21(waf1) and p53.
Fujii, S; Fukuhara, K; Kanamori, T; Kariya, M; Kusakari, T; Momma, C; Nikaido, T; Orii, A; Shime, H; Takakura, K; Tsuruta, Y, 2002
)
2.48
"Tranilast could inhibit TGF-beta(2) expression in cultured human trabecular meshwork cells. "( [The inhibitory effect of tranilast on transforming growth factor-beta(2) expression in cultured human trabecular meshwork cells].
Cao, Y; Da, BH; Wei, HR, 2004
)
2.07
"Tranilast was found to inhibit collagen synthesis in a dose-dependent manner to a maximum of 55% at 300 microM during 48 h of treatment; the synthesis of type I and type III collagens was equally affected."( Tranilast, a selective inhibitor of collagen synthesis in human skin fibroblasts.
Murad, S; Nishikawa, T; Pinnell, SR; Tajima, S; Yamada, H, 1994
)
2.45
"Tranilast did not cause cell toxicity and may therefore hold promising potential for the prevention of vascular proliferative diseases."( Antiproliferative and c-myc mRNA suppressive effect of tranilast on newborn human vascular smooth muscle cells in culture.
Hamano, S; Miyazawa, K; Ujiie, A, 1996
)
1.26
"Tranilast may thus allow us to prevent restenosis after PTCA by interfering with this mechanism."( Tranilast inhibits the proliferation of human coronary smooth muscle cell through the activation of p21waf1.
Baba, Y; Fujii, S; Katsuno, K; Kikuchi, S; Kusama, H; Nikaido, T; Tazawa, S; Zhai, YL, 1999
)
2.47
"Tranilast may inhibit scar formation after trabeculectomy for glaucoma and after excimer laser photorefractive keratectomy."( Tranilast inhibits cell proliferation and collagen synthesis by rabbit corneal and Tenon's capsule fibroblasts.
Kato, K; Kurosaka, D; Kurosaka, H; Mashima, Y; Oshima, T; Tajima, S; Tanaka, Y, 2000
)
3.19
"Tranilast did not inhibit the release of arachidonic acid metabolites from the lungs but it prevented the contraction of the rat aorta induced by thromboxane released from lungs."( New approach to the mechanism of antiasthmatic action of Tranilast.
García Mesa, M,
)
1.1

Treatment

Tranilast was found to prevent alterations in vascular reactivity and insulin sensitivity. Tranilast treatment of the in vivo mouse model reduced the pleural dissemination of cancer cells.

ExcerptReferenceRelevance
"Tranilast treatment of the in vivo mouse model reduced the pleural dissemination of cancer cells and suppressed vimentin and Smad4 expression."( Tranilast Inhibits TGF-β1-induced Epithelial-mesenchymal Transition and Invasion/Metastasis
Chen-Yoshikawa, TF; Date, H; Hamaji, M; Menju, T; Miyata, R; Nakajima, D; Nishikawa, S; Ohsumi, A; Sato, T; Sonobe, M; Takahashi, K; Tanaka, S; Yamada, Y; Yutaka, Y, 2020
)
2.72
"Tranilast treatment decreased the messenger RNA (mRNA) and protein levels of multiple proinflammatory cytokines, and affected NF-κB and inhibitor of kappa B protein expressions."( Tranilast Treatment Attenuates Cerebral Ischemia-Reperfusion Injury in Rats Through the Inhibition of Inflammatory Responses Mediated by NF-κB and PPARs.
Zhuo, J; Zhuo, Y, 2019
)
2.68
"Tranilast treatment was found to prevent alterations in vascular reactivity and insulin sensitivity and to prevent increases in plasma glucose and insulin noted in the high-fat emulsion-treated rats."( Tranilast alleviates endothelial dysfunctions and insulin resistance via preserving glutathione peroxidase 1 in rats fed a high-fat emulsion.
Feng, L; Li, C; Li, Y; Yang, X, 2014
)
2.57
"Tranilast treatment significantly decreased the myocardial pathological changes and collagen volume fraction compared with the VMC group (P<0.05)."( [Tranilast inhibits myocardial fibrosis in mice with viral myocarditis].
Chen, CY; Huang, LF; Wen, C; Xie, G; Zeng, P, 2016
)
2.07
"Tranilast treatment upregulates p53, induces PARP cleavage in vitro, consistent with a promotion of tumor cell apoptosis."( Tranilast inhibits cell proliferation and migration and promotes apoptosis in murine breast cancer.
Chakrabarti, R; Jothy, S; Prud'homme, GJ; Subramaniam, V, 2010
)
2.52
"Tranilast treatment of MI rats from 24h until seven days post-MI reduced myocardial collagen content, α1 (I) procollagen, TGFβ1 and CTGF mRNA transcripts, monocyte/macrophage infiltration and exacerbated infarct expansion compared with vehicle-treatment. "( Early and delayed tranilast treatment reduces pathological fibrosis following myocardial infarction.
Boyle, AJ; Gilbert, RE; Kelly, DJ; Kompa, AR; Krum, H; See, F; Wang, BH; Watanabe, M, 2013
)
2.17
"Tranilast treatment did not influence plasma glucose or systemic blood pressure."( Tranilast attenuates vascular hypertrophy, matrix accumulation and growth factor overexpression in experimental diabetes.
Bonnet, F; Cao, Z; Cooper, ME; Cox, AJ; Gilbert, RE; Kelly, DJ, 2003
)
2.48
"Tranilast treatment decreased albuminuria and hyperfiltration."( Tranilast prevents the progression of experimental diabetic nephropathy through suppression of enhanced extracellular matrix gene expression.
Akahori, H; Ando, H; Kaneko, S; Ota, T; Takamura, T; Torita, M, 2005
)
2.49
"Tranilast treatment using various vehicles and dosages was compared to vehicle alone versus no treatment."( Reduction of post-surgical adhesion formation with tranilast.
Cooper, K; Cui, H; diZerega, GS; Rodgers, KE; Wadsworth, S; Young, J, 2007
)
1.31
"Tranilast treatment resulted in a significant reduction in mesangial cell proliferation, macrophage infiltration, activated (alpha-smooth muscle actin positive) mesangial cells, glomerular type IV collagen deposition and proteinuria compared to control rats. "( Tranilast ameliorates experimental mesangial proliferative glomerulonephritis.
Cox, A; Gilbert, RE; Kelly, DJ; Nikolic-Paterson, DJ; Thai, K; Tokuyama, H; Zhang, Y, 2008
)
3.23
"Tranilast treatment was found to suppress the aortic area covered with plaque."( Suppression of atherosclerotic development in Watanabe heritable hyperlipidemic rabbits treated with an oral antiallergic drug, tranilast.
Doi, H; Kugiyama, K; Matsumura, T; Ogata, N; Oka, H; Ota, Y; Sugiyama, S; Yasue, H, 1999
)
1.23
"Tranilast treatment completely prevented the increase in chymaselike activity, reduced the chymase mRNA levels by 43%, and decreased the carotid intima/media ratio by 63%."( Tranilast suppresses vascular chymase expression and neointima formation in balloon-injured dog carotid artery.
Mikoshiba, I; Miyazaki, M; Okunishi, H; Sakonjo, H; Shibata, N; Shiota, N; Takai, S, 1999
)
2.47
"Tranilast-treated rats had a 70% (P<0.001) smaller neointima/media area ratio at 14 days after balloon injury compared with the controls."( Tranilast inhibits vascular smooth muscle cell growth and intimal hyperplasia by induction of p21(waf1/cip1/sdi1) and p53.
Ishikawa, Y; Takahashi, A; Taniguchi, T; Yokoyama, M, 1999
)
2.47
"Treatment with tranilast led to inhibition of IL-6 secretion from the CAFs, which, in turn, resulted in inhibition of CAF-induced phospho-STAT3 upregulation."( Drug repositioning of tranilast to sensitize a cancer therapy by targeting cancer-associated fibroblast.
Nakata, K; Ochi, K; Okamoto, Y; Okazaki, M; Shien, K; Shien, T; Sugimoto, S; Suzawa, K; Takatsu, F; Takeda, T; Thu, YM; Tomida, S; Toyooka, S; Tsudaka, S; Yamamoto, H; Zhu, Y, 2022
)
1.38
"Treatment with tranilast suppressed the expression of ECM proteins, such as fibronectin and type IV collagen, and attenuated SMAD2 phosphorylation in TGFβ2-stimulated A549 cells. "( Tranilast Inhibits Pulmonary Fibrosis by Suppressing TGFβ/SMAD2 Pathway.
Baskoro, H; Fujimura, T; Hidayat, M; Ihara, H; Kato, M; Kobayashi, I; Kumasaka, T; Mineki, R; Mitsuishi, Y; Murakami, A; Niwa, SI; Nurwidya, F; Sasaki, S; Sato, T; Shimada, N; Tajima, K; Takahashi, F; Takahashi, K, 2020
)
2.35
"Treatment with tranilast significantly suppressed the progression of peritoneal fibrosis in CRF rats."( Mast cell involvement in the progression of peritoneal fibrosis in rats with chronic renal failure.
Baba, A; Ejima, Y; Endo, Y; Kazama, I; Matsubara, M; Tachi, M; Toyama, H, 2015
)
0.76
"Treatment with tranilast did not suppress the progression of renal fibrosis, nor did it ameliorate the progression of glomerulosclerosis and the interstitial proliferation of inflammatory leukocytes."( Less contribution of mast cells to the progression of renal fibrosis in Rat kidneys with chronic renal failure.
Abe, N; Baba, A; Ejima, Y; Endo, Y; Kazama, I; Miura, C; Saito, K; Tachi, M; Toyama, H; Yamauchi, M, 2017
)
0.79
"Treatment with tranilast for 4 weeks significantly attenuated Txnip up-regulation in diabetic rats and this was associated with a reduction in ROS, fibrosis and macrophage infiltration (all P < 0.05)."( Tranilast attenuates the up-regulation of thioredoxin-interacting protein and oxidative stress in an experimental model of diabetic nephropathy.
Cox, AJ; Kelly, DJ; Qi, W; Tan, SM; Zhang, Y, 2011
)
2.15
"Treated with tranilast varying from 12.5 mg/L to 100.0 mg/L concentration, the proliferation of fibroblasts declined in a dose dependent manner. "( [The investigation of tranilast on the proliferation and migration of human Tenon's capsule fibroblasts].
Ding, ZP; Hu, YZ; Ji, CN; Li, GG, 2004
)
1.01
"Treatment with tranilast significantly reduced the serum level of TNF-alpha, numbers of total and degranulating MCs, % apoptotic cardiomyocytes, and CVF at D30 (all p<0.05)."( Mast cell contributes to cardiomyocyte apoptosis after coronary microembolization.
Chen, JZ; Ge, JB; Lau, CP; Tse, HF; Zhang, LH; Zhang, QY; Zhu, JH, 2006
)
0.67
"Treatment with tranilast prevented the development of diastolic dysfunction and the histopathological features of DCM."( Tranilast attenuates diastolic dysfunction and structural injury in experimental diabetic cardiomyopathy.
Connelly, K; Cox, AJ; Gilbert, RE; Kelly, DJ; Krum, H; Martin, J; Zhang, Y, 2007
)
2.12
"Treatment with tranilast significantly suppressed insulin secretion in INS-1E cells and rat islets induced by 16.7 mmol/l glucose."( Tranilast inhibits glucose-induced insulin secretion from pancreatic beta-cells.
Mizutani, N; Oiso, Y; Ozaki, N; Taguchi, S; Umeda, H; Yamada, T, 2008
)
2.13
"Pretreatment with tranilast (10(-3) M) also significantly reduced A23187-induced LTC4 production (p < 0.05)."( Inhibitory effects of azelastine and tranilast on leukotriene B4 and leukotriene C4 generation by rat colonic mucosa.
Igarashi, J; Shimizu, T; Yabuta, K; Yamashiro, Y, 1995
)
0.89
"Treatment with tranilast increased the number of cells in the G1 phase suggesting that this compound induced G1 arrest."( Inhibition of proliferation of MCF-7 breast cancer cells by a blocker of Ca(2+)-permeable channel.
Doi, I; Kojima, I; Nie, L; Oishi, Y; Shibata, H, 1997
)
0.64
"Treatment with tranilast and topical corticosteroid was dramatically effective."( Unilateral Schamberg disease in a 14-year-old Japanese boy.
Danno, K; Nagata, K; Tanaka, S, 1999
)
0.64
"Treatment with tranilast, a mast cell-stabilizing agent, also prevented the evolution from compensated hypertrophy to heart failure."( Evidence for a role of mast cells in the evolution to congestive heart failure.
Hara, M; Hwang, MW; Iwasaki, A; Matsumori, A; Nakatani, K; Okada, M; Ono, K; Sasayama, S, 2002
)
0.65
"Treatment with Tranilast of 45 patients (87 ears) with secretory otitis media was studied. "( Use of Tranilast [N-(3,4-dimethoxycinnamoyl) anthranilic acid] in secretory otitis media.
Harada, T; Matsunaga, T; Ogino, S; Tominaga, Y, 1992
)
1.09

Toxicity

ExcerptReferenceRelevance
"Identification of reliable markers to predict drug-related adverse events (DRAEs) is an important goal of the pharmaceutical industry and others within the healthcare community."( Pharmacogenetics to predict drug-related adverse events.
Danoff, TM; Hosford, DA; Lai, EH; Riley, JH; Roses, AD; Xu, CF,
)
0.13
" However, one of the major challenges of the application of CsA is the occurrence of the serious adverse effects, namely, acute and chronic nephrotoxicity, severe hypertension and neurotoxicity."( Combination of N-(3'4'-dimethoxycinnamoyl) anthranilic acid with cyclosporin A treatment preserves immunosuppressive effect and reduces the side effect of cyclosporin A in rat.
Jin-Yan, Z; Jun-Ming, X; Ming-Zhe, W; Yong-Gang, X; Zhi-Hai, P, 2014
)
0.4
" Nephrotoxicity is a side effect frequently encountered with cyclophosphamide (CP), which is also well-known to cause acute and chronic lung toxicities."( Tranilast ameliorates cyclophosphamide-induced lung injury and nephrotoxicity.
Abdelaziz, RR; Elkashef, WF; Said, E, 2016
)
1.88

Pharmacokinetics

ExcerptReferenceRelevance
" Pharmacokinetic profiling of orally dosed TL formulations in rats was also carried out using UPLC/ESI-MS."( Physicochemical and pharmacokinetic characterization of amorphous solid dispersion of tranilast with enhanced solubility in gastric fluid and improved oral bioavailability.
Aoki, Y; Kawabata, Y; Kojo, Y; Onoue, S; Yamada, S; Yamauchi, Y, 2012
)
0.6

Compound-Compound Interactions

ExcerptReferenceRelevance
" The aim of this study was to understand whether tranilast could inhibit renal uptake transporters (Oat1, Oat3, and Oct2) and whether MTX combined with TL would have drug-drug interactions."( The key role of organic anion transporter 3 in the drug-drug interaction between tranilast and methotrexate.
Huang, X; Jiang, Z; Shen, Q; Wang, J; Wu, Q; Wu, W; Yuan, W; Zhang, L, 2022
)
1.2

Bioavailability

Tranilast (TL) composite particles with α-glucosyl rutin (Rutin-G) were developed to improve the solubility and oral bioavailability of TL.

ExcerptReferenceRelevance
" According to these observations, taken together with dissolution and pharmacokinetic behaviors, crystalline solid dispersion strategy would be efficacious to enhance bioavailability of TL with high photochemical stability."( Novel crystalline solid dispersion of tranilast with high photostability and improved oral bioavailability.
Debari, K; Kawabata, Y; Onoue, S; Yamada, S; Yamamoto, K, 2010
)
0.63
" After oral administration of the Eudragit EPO-based ASD formulation in rats, enhanced TL exposure was observed with an increase of oral bioavailability by 19-fold, and the variation of AUC was ca."( Physicochemical and pharmacokinetic characterization of amorphous solid dispersion of tranilast with enhanced solubility in gastric fluid and improved oral bioavailability.
Aoki, Y; Kawabata, Y; Kojo, Y; Onoue, S; Yamada, S; Yamauchi, Y, 2012
)
0.6
" Currently licensed as an anti-allergy drug, the oral bioavailability and safe therapeutic profile of DAA make it a candidate for the prevention of rejection of transplanted cornea and other tissues."( Suppression of the allogeneic response by the anti-allergy drug N-(3,4-dimethoxycinnamonyl) anthranilic acid results from T-cell cycle arrest.
Chai, JG; Coe, D; George, AJ; Larkin, DF; Zaher, SS, 2013
)
0.39
"The present study aimed to develop an effective oral formulation of tranilast (TL), a poorly soluble anti-inflammatory drug, via the formation of drug complex with 3-aminopropyl functionalized magnesium phyllosilicate (AMP clay) and improve the pH-dependent drug dissolution and bioavailability of TL."( Preparation and in vitro/in vivo characterization of tranilast-AMP clay complex for improving drug dissolution and bioavailability.
Han, HK; Shao, Y; Yang, L, 2014
)
0.89
"Tranilast (TL) composite particles with α-glucosyl rutin (Rutin-G) were developed to improve the solubility and oral bioavailability of TL."( Absorption improvement of tranilast by forming highly soluble nano-size composite structures associated with α-glucosyl rutin via spray drying.
Fujimori, M; Kadota, K; Onoue, S; Sato, H; Shirakawa, Y; Suzuki, H; Tozuka, Y, 2015
)
2.16
" The oral bioavailability of TL in TNBS-treated rats was calculated to be as low as ca."( Protective effects of tranilast on experimental colitis in rats.
Kaneko, Y; Kato, K; Kojo, Y; Onoue, S; Sato, H; Seto, Y; Suzuki, H; Tsukada, R, 2017
)
0.77
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Systemic exposure of TL after intratracheal administration of CSD/TL-RP at a pharmacologically effective dose (100 μg of TL/rat) was found to be fivefold less than that of the oral TL dosage form at clinical dose (1."( Development of inhalable nanocrystalline solid dispersion of tranilast for airway inflammatory diseases.
Aoki, Y; Kawabata, Y; Matsui, T; Onoue, S; Sato, H; Yamada, S; Yamamoto, K; Yamauchi, Y, 2011
)
0.61
" Pharmacokinetic profiling of orally dosed TL formulations in rats was also carried out using UPLC/ESI-MS."( Physicochemical and pharmacokinetic characterization of amorphous solid dispersion of tranilast with enhanced solubility in gastric fluid and improved oral bioavailability.
Aoki, Y; Kawabata, Y; Kojo, Y; Onoue, S; Yamada, S; Yamauchi, Y, 2012
)
0.6
" Pharmacokinetic behaviors of orally dosed TL formulations were evaluated in rats using UPLC/ESI-MS."( Development of novel solid dispersion of tranilast using amphiphilic block copolymer for improved oral bioavailability.
Hashimoto, N; Kawabata, Y; Kojo, Y; Kou, K; Onoue, S; Suzuki, H; Yamada, S; Yamauchi, Y; Yuminoki, K, 2013
)
0.66
" The hepatoprotective effects of orally dosed TL formulations were evaluated in a carbon tetrachloride (CCl4)-treated rat model of acute liver injury."( In vitro/in vivo characterization of nanocrystalline formulation of tranilast with improved dissolution and hepatoprotective properties.
Kawabata, Y; Onoue, S; Yamada, S; Yamamoto, K, 2013
)
0.63
" In this study, we used the dark agouti (DA)-Lewis rat orthotopic liver transplantation (OLT) model to investigate whether the combination of 3,4-DAA with CsA is a promising and useful strategy to lower CsA dosage for reducing CsA side effect and preserve therapeutic effect of CsA."( Combination of N-(3'4'-dimethoxycinnamoyl) anthranilic acid with cyclosporin A treatment preserves immunosuppressive effect and reduces the side effect of cyclosporin A in rat.
Jin-Yan, Z; Jun-Ming, X; Ming-Zhe, W; Yong-Gang, X; Zhi-Hai, P, 2014
)
0.4
"SMSD/TL-RP might be an attractive dosage form to improve the anti-inflammatory effects and safety of TL."( Strategic application of self-micellizing solid dispersion technology to respirable powder formulation of tranilast for improved therapeutic potential.
Hashimoto, N; Kojo, Y; Onoue, S; Suzuki, H; Yakushiji, K; Yuminoki, K, 2016
)
0.65
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (7)

RoleDescription
anti-asthmatic drugA drug used to treat asthma.
nephroprotective agentAny protective agent that is able to prevent damage to the kidney.
anti-allergic agentA drug used to treat allergic reactions.
calcium channel blockerOne of a class of drugs that acts by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
aryl hydrocarbon receptor agonistAn agonist that binds to and activates aryl hydrocarbon receptors (AhRs).
hepatoprotective agentAny compound that is able to prevent damage to the liver.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
cinnamamidesAn enamide which is cinnamamide or a derivative of cinnamamide obtained by replacement of one or more of its hydrogens.
dimethoxybenzeneAny methoxybenzene that consists of a benzene skeleton substituted with two methoxy groups and its derivatives.
amidobenzoic acid
secondary carboxamideA carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
[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]

Pathways (1)

PathwayProteinsCompounds
Uricosurics Pathway, Pharmacodynamics123

Protein Targets (81)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency39.81070.003245.467312,589.2998AID1705
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency31.74820.177814.390939.8107AID2147
LuciferasePhotinus pyralis (common eastern firefly)Potency3.30570.007215.758889.3584AID411; AID588342; AID624030
dopamine D1 receptorHomo sapiens (human)Potency29.09290.00521.30228.1995AID624455
ATAD5 protein, partialHomo sapiens (human)Potency6.20020.004110.890331.5287AID493106; AID493107; AID504466; AID504467
USP1 protein, partialHomo sapiens (human)Potency76.11040.031637.5844354.8130AID504865
NFKB1 protein, partialHomo sapiens (human)Potency28.18380.02827.055915.8489AID895; AID928
TDP1 proteinHomo sapiens (human)Potency18.83750.000811.382244.6684AID686978
ThrombopoietinHomo sapiens (human)Potency10.00000.02517.304831.6228AID917; AID918
AR proteinHomo sapiens (human)Potency14.22980.000221.22318,912.5098AID743035; AID743036; AID743042; AID743053; AID743054; AID743063
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency7.94330.00137.762544.6684AID914; AID915
nonstructural protein 1Influenza A virus (A/WSN/1933(H1N1))Potency5.01190.28189.721235.4813AID2326
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency6.00700.000214.376460.0339AID720692
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency1.45430.001530.607315,848.9004AID1224819; AID1224820; AID1224821
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.99400.000229.305416,493.5996AID743069; AID743075; AID743080; AID743091
ParkinHomo sapiens (human)Potency13.08160.819914.830644.6684AID720572; AID720573
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.12510.707936.904389.1251AID504333
arylsulfatase AHomo sapiens (human)Potency6.74561.069113.955137.9330AID720538
pyruvate kinaseLeishmania mexicana mexicanaPotency12.58930.398113.744731.6228AID945; AID959
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.83180.035520.977089.1251AID504332
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency2.07490.016525.307841.3999AID504836; AID602332
aryl hydrocarbon receptorHomo sapiens (human)Potency3.34910.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.16790.001723.839378.1014AID743083
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency0.53490.01262.451825.0177AID485313
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency7.568623.934123.934123.9341AID1967
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency11.29470.316212.443531.6228AID902; AID924
polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)Potency7.07951.000012.232631.6228AID1452
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency14.12540.001815.663839.8107AID894
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency9.52830.134610.395030.1313AID1347049
chromobox protein homolog 1Homo sapiens (human)Potency0.00600.006026.168889.1251AID488953
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency35.48133.548119.542744.6684AID743266
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency7.08500.000323.4451159.6830AID743065; AID743067
mitogen-activated protein kinase 1Homo sapiens (human)Potency2.27400.039816.784239.8107AID1454; AID995
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency3.68980.00669.809418.4927AID1347050
ras-related protein Rab-9AHomo sapiens (human)Potency0.36110.00022.621531.4954AID485297
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency22.38720.010323.856763.0957AID2662
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency7.07950.15855.287912.5893AID540303
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency3.39810.00798.23321,122.0200AID2546; AID2551
gemininHomo sapiens (human)Potency33.49830.004611.374133.4983AID624296
survival motor neuron protein isoform dHomo sapiens (human)Potency0.49290.125912.234435.4813AID1458
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency10.00000.031610.279239.8107AID884; AID885
M-phase phosphoprotein 8Homo sapiens (human)Potency0.19950.177824.735279.4328AID488949
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency18.82170.00419.962528.1838AID2675
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.12590.00106.000935.4813AID943
pyruvate kinase PKM isoform bHomo sapiens (human)Potency19.95262.511912.262825.1189AID954; AID958
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.58930.015812.3113615.5000AID1461
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Integrin beta-3Homo sapiens (human)Potency10.00000.316211.415731.6228AID924
Integrin alpha-IIbHomo sapiens (human)Potency10.00000.316211.415731.6228AID924
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
GABA theta subunitRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency1.06610.011917.942071.5630AID651632; AID720516
Ataxin-2Homo sapiens (human)Potency2.00330.011912.222168.7989AID588378; AID651632
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency10.00001.000012.224831.6228AID885
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency26.54580.060110.745337.9330AID485367; AID485368; AID492961
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)1.00000.20005.677410.0000AID1473741
Hematopoietic prostaglandin D synthaseHomo sapiens (human)IC50 (µMol)11.60000.07100.92223.8000AID1798101; AID319190
Transient receptor potential cation channel subfamily A member 1Homo sapiens (human)IC50 (µMol)125.94650.05102.47257.5000AID1549772
Bile salt export pumpHomo sapiens (human)IC50 (µMol)41.50000.11007.190310.0000AID1473738
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC50 (µMol)25.00000.00041.441910.0000AID1846680
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Transient receptor potential cation channel subfamily V member 2Homo sapiens (human)IC50 (µMol)10.00000.80002.93336.5000AID1623895
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
MSHDrosophila melanogaster (fruit fly)AC500.59400.20909.578848.6900AID743444
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (157)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin biosynthetic processHematopoietic prostaglandin D synthaseHomo sapiens (human)
prostaglandin metabolic processHematopoietic prostaglandin D synthaseHomo sapiens (human)
signal transductionHematopoietic prostaglandin D synthaseHomo sapiens (human)
locomotory behaviorHematopoietic prostaglandin D synthaseHomo sapiens (human)
negative regulation of male germ cell proliferationHematopoietic prostaglandin D synthaseHomo sapiens (human)
glutathione metabolic processHematopoietic prostaglandin D synthaseHomo sapiens (human)
monoatomic ion transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellular calcium ion homeostasisTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cell surface receptor signaling pathwayTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to coldTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to xenobiotic stimulusTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to organic cyclic compoundTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium-mediated signalingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
response to painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
thermoceptionTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
detection of chemical stimulus involved in sensory perception of painTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
protein homotetramerizationTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to hydrogen peroxideTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
cellular response to organic substanceTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
negative regulation of low-density lipoprotein receptor activityIntegrin beta-3Homo sapiens (human)
positive regulation of protein phosphorylationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
cell-substrate junction assemblyIntegrin beta-3Homo sapiens (human)
cell adhesionIntegrin beta-3Homo sapiens (human)
cell-matrix adhesionIntegrin beta-3Homo sapiens (human)
integrin-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
embryo implantationIntegrin beta-3Homo sapiens (human)
blood coagulationIntegrin beta-3Homo sapiens (human)
positive regulation of endothelial cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of gene expressionIntegrin beta-3Homo sapiens (human)
negative regulation of macrophage derived foam cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast migrationIntegrin beta-3Homo sapiens (human)
negative regulation of lipid storageIntegrin beta-3Homo sapiens (human)
response to activityIntegrin beta-3Homo sapiens (human)
smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell migrationIntegrin beta-3Homo sapiens (human)
platelet activationIntegrin beta-3Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
cell-substrate adhesionIntegrin beta-3Homo sapiens (human)
activation of protein kinase activityIntegrin beta-3Homo sapiens (human)
negative regulation of lipid transportIntegrin beta-3Homo sapiens (human)
regulation of protein localizationIntegrin beta-3Homo sapiens (human)
regulation of actin cytoskeleton organizationIntegrin beta-3Homo sapiens (human)
cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of cell adhesion mediated by integrinIntegrin beta-3Homo sapiens (human)
positive regulation of osteoblast proliferationIntegrin beta-3Homo sapiens (human)
heterotypic cell-cell adhesionIntegrin beta-3Homo sapiens (human)
substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
tube developmentIntegrin beta-3Homo sapiens (human)
wound healing, spreading of epidermal cellsIntegrin beta-3Homo sapiens (human)
cellular response to platelet-derived growth factor stimulusIntegrin beta-3Homo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayIntegrin beta-3Homo sapiens (human)
wound healingIntegrin beta-3Homo sapiens (human)
apoptotic cell clearanceIntegrin beta-3Homo sapiens (human)
regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
positive regulation of angiogenesisIntegrin beta-3Homo sapiens (human)
positive regulation of bone resorptionIntegrin beta-3Homo sapiens (human)
symbiont entry into host cellIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
positive regulation of fibroblast proliferationIntegrin beta-3Homo sapiens (human)
mesodermal cell differentiationIntegrin beta-3Homo sapiens (human)
positive regulation of smooth muscle cell proliferationIntegrin beta-3Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationIntegrin beta-3Homo sapiens (human)
negative regulation of lipoprotein metabolic processIntegrin beta-3Homo sapiens (human)
negative chemotaxisIntegrin beta-3Homo sapiens (human)
regulation of release of sequestered calcium ion into cytosolIntegrin beta-3Homo sapiens (human)
regulation of serotonin uptakeIntegrin beta-3Homo sapiens (human)
angiogenesis involved in wound healingIntegrin beta-3Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeIntegrin beta-3Homo sapiens (human)
platelet aggregationIntegrin beta-3Homo sapiens (human)
cellular response to mechanical stimulusIntegrin beta-3Homo sapiens (human)
cellular response to xenobiotic stimulusIntegrin beta-3Homo sapiens (human)
positive regulation of glomerular mesangial cell proliferationIntegrin beta-3Homo sapiens (human)
blood coagulation, fibrin clot formationIntegrin beta-3Homo sapiens (human)
maintenance of postsynaptic specialization structureIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor internalizationIntegrin beta-3Homo sapiens (human)
regulation of postsynaptic neurotransmitter receptor diffusion trappingIntegrin beta-3Homo sapiens (human)
positive regulation of substrate adhesion-dependent cell spreadingIntegrin beta-3Homo sapiens (human)
positive regulation of adenylate cyclase-inhibiting opioid receptor signaling pathwayIntegrin beta-3Homo sapiens (human)
regulation of trophoblast cell migrationIntegrin beta-3Homo sapiens (human)
regulation of extracellular matrix organizationIntegrin beta-3Homo sapiens (human)
cellular response to insulin-like growth factor stimulusIntegrin beta-3Homo sapiens (human)
negative regulation of endothelial cell apoptotic processIntegrin beta-3Homo sapiens (human)
positive regulation of T cell migrationIntegrin beta-3Homo sapiens (human)
cell migrationIntegrin beta-3Homo sapiens (human)
positive regulation of leukocyte migrationIntegrin alpha-IIbHomo sapiens (human)
cell-matrix adhesionIntegrin alpha-IIbHomo sapiens (human)
integrin-mediated signaling pathwayIntegrin alpha-IIbHomo sapiens (human)
angiogenesisIntegrin alpha-IIbHomo sapiens (human)
cell-cell adhesionIntegrin alpha-IIbHomo sapiens (human)
cell adhesion mediated by integrinIntegrin alpha-IIbHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell population proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of B cell proliferationATPase family AAA domain-containing protein 5Homo sapiens (human)
nuclear DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
signal transduction in response to DNA damageATPase family AAA domain-containing protein 5Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
isotype switchingATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of DNA replicationATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of isotype switching to IgG isotypesATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloadingATPase family AAA domain-containing protein 5Homo sapiens (human)
regulation of mitotic cell cycle phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorATPase family AAA domain-containing protein 5Homo sapiens (human)
positive regulation of cell cycle G2/M phase transitionATPase family AAA domain-containing protein 5Homo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
response to temperature stimulusTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
sensory perceptionTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
positive regulation of axon extensionTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
calcium ion transmembrane transportTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
positive regulation of calcium ion importTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
positive regulation of cold-induced thermogenesisTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
calcium ion import across plasma membraneTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (61)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
magnesium ion bindingHematopoietic prostaglandin D synthaseHomo sapiens (human)
glutathione transferase activityHematopoietic prostaglandin D synthaseHomo sapiens (human)
prostaglandin-D synthase activityHematopoietic prostaglandin D synthaseHomo sapiens (human)
calcium ion bindingHematopoietic prostaglandin D synthaseHomo sapiens (human)
protein bindingHematopoietic prostaglandin D synthaseHomo sapiens (human)
protein homodimerization activityHematopoietic prostaglandin D synthaseHomo sapiens (human)
calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
intracellularly gated calcium channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
identical protein bindingTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
temperature-gated cation channel activityTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
fibroblast growth factor bindingIntegrin beta-3Homo sapiens (human)
C-X3-C chemokine bindingIntegrin beta-3Homo sapiens (human)
insulin-like growth factor I bindingIntegrin beta-3Homo sapiens (human)
neuregulin bindingIntegrin beta-3Homo sapiens (human)
virus receptor activityIntegrin beta-3Homo sapiens (human)
fibronectin bindingIntegrin beta-3Homo sapiens (human)
protease bindingIntegrin beta-3Homo sapiens (human)
protein disulfide isomerase activityIntegrin beta-3Homo sapiens (human)
protein kinase C bindingIntegrin beta-3Homo sapiens (human)
platelet-derived growth factor receptor bindingIntegrin beta-3Homo sapiens (human)
integrin bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin beta-3Homo sapiens (human)
coreceptor activityIntegrin beta-3Homo sapiens (human)
enzyme bindingIntegrin beta-3Homo sapiens (human)
identical protein bindingIntegrin beta-3Homo sapiens (human)
vascular endothelial growth factor receptor 2 bindingIntegrin beta-3Homo sapiens (human)
metal ion bindingIntegrin beta-3Homo sapiens (human)
cell adhesion molecule bindingIntegrin beta-3Homo sapiens (human)
extracellular matrix bindingIntegrin beta-3Homo sapiens (human)
fibrinogen bindingIntegrin beta-3Homo sapiens (human)
protein bindingIntegrin alpha-IIbHomo sapiens (human)
identical protein bindingIntegrin alpha-IIbHomo sapiens (human)
metal ion bindingIntegrin alpha-IIbHomo sapiens (human)
extracellular matrix bindingIntegrin alpha-IIbHomo sapiens (human)
molecular adaptor activityIntegrin alpha-IIbHomo sapiens (human)
fibrinogen bindingIntegrin alpha-IIbHomo sapiens (human)
integrin bindingIntegrin alpha-IIbHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
protein bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
ATP hydrolysis activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA clamp unloader activityATPase family AAA domain-containing protein 5Homo sapiens (human)
DNA bindingATPase family AAA domain-containing protein 5Homo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
monoatomic ion channel activityTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
monoatomic cation channel activityTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
calcium channel activityTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
protein bindingTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
monoatomic ion transmembrane transporter activityTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (56)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
nucleoplasmHematopoietic prostaglandin D synthaseHomo sapiens (human)
cytoplasmHematopoietic prostaglandin D synthaseHomo sapiens (human)
cytosolHematopoietic prostaglandin D synthaseHomo sapiens (human)
intracellular membrane-bounded organelleHematopoietic prostaglandin D synthaseHomo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
stereocilium bundleTransient receptor potential cation channel subfamily A member 1Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
glutamatergic synapseIntegrin beta-3Homo sapiens (human)
nucleusIntegrin beta-3Homo sapiens (human)
nucleoplasmIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin beta-3Homo sapiens (human)
cell-cell junctionIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
external side of plasma membraneIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
apical plasma membraneIntegrin beta-3Homo sapiens (human)
platelet alpha granule membraneIntegrin beta-3Homo sapiens (human)
lamellipodium membraneIntegrin beta-3Homo sapiens (human)
filopodium membraneIntegrin beta-3Homo sapiens (human)
microvillus membraneIntegrin beta-3Homo sapiens (human)
ruffle membraneIntegrin beta-3Homo sapiens (human)
integrin alphav-beta3 complexIntegrin beta-3Homo sapiens (human)
melanosomeIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
postsynaptic membraneIntegrin beta-3Homo sapiens (human)
extracellular exosomeIntegrin beta-3Homo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin beta-3Homo sapiens (human)
glycinergic synapseIntegrin beta-3Homo sapiens (human)
integrin complexIntegrin beta-3Homo sapiens (human)
protein-containing complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-PKCalpha complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-IGF-1-IGF1R complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-HMGB1 complexIntegrin beta-3Homo sapiens (human)
receptor complexIntegrin beta-3Homo sapiens (human)
alphav-beta3 integrin-vitronectin complexIntegrin beta-3Homo sapiens (human)
alpha9-beta1 integrin-ADAM8 complexIntegrin beta-3Homo sapiens (human)
focal adhesionIntegrin beta-3Homo sapiens (human)
cell surfaceIntegrin beta-3Homo sapiens (human)
synapseIntegrin beta-3Homo sapiens (human)
plasma membraneIntegrin alpha-IIbHomo sapiens (human)
focal adhesionIntegrin alpha-IIbHomo sapiens (human)
cell surfaceIntegrin alpha-IIbHomo sapiens (human)
platelet alpha granule membraneIntegrin alpha-IIbHomo sapiens (human)
extracellular exosomeIntegrin alpha-IIbHomo sapiens (human)
integrin alphaIIb-beta3 complexIntegrin alpha-IIbHomo sapiens (human)
blood microparticleIntegrin alpha-IIbHomo sapiens (human)
integrin complexIntegrin alpha-IIbHomo sapiens (human)
external side of plasma membraneIntegrin alpha-IIbHomo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
cytosolNACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
Elg1 RFC-like complexATPase family AAA domain-containing protein 5Homo sapiens (human)
nucleusATPase family AAA domain-containing protein 5Homo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
cell surfaceTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
growth cone membraneTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
melanosomeTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
axonal growth coneTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
cell bodyTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
plasma membraneTransient receptor potential cation channel subfamily V member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (130)

Assay IDTitleYearJournalArticle
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1549770Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx at 100 uM incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assay relative to CA2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1057543AUC (0 to infinity) in Sprague-Dawley rat at 20 mg/kg, po2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1079931Moderate 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]
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1474063AUC in human at 80 to 600 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1549775Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition in WS5-induced increase in calcium influx incubated for 10 mins prior to WS5 challenge by Fluo-4-AM dye based fluorescence assay2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1079935Cytolytic 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]
AID1057550Plasma clearance in Sprague-Dawley rat at 5 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID1057542Tmax in Sprague-Dawley rat at 20 mg/kg, po2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID220016Inhibition of human coronary artery smooth muscle cells (SMC's) proliferation, induced by platelet-derived growth factor (PDGF-BB) 20 ng mL.2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1057551Apparent half life in Sprague-Dawley rat at 5 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1057546Apparent half life in Sprague-Dawley rat at 20 mg/kg, po2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1474065Ratio of drug concentration at steady state in human at 80 to 600 mg, po QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1846680Inhibition of NLRP3 inflammasome activation in LPS-primed C57BL/6 mouse bone marrow derived macrophages incubated for 30 mins in presence of ATP by immunoblotting analysis2021Bioorganic & medicinal chemistry letters, 07-15, Volume: 44Small molecule approaches to treat autoimmune and inflammatory diseases (Part II): Nucleic acid sensing antagonists and inhibitors.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID219893Evaluated for inhibition of proliferation of human coronary artery endothelial cells (ECs), induced by 5 % FBS.2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells.
AID1057544Cmax in Sprague-Dawley rat at 20 mg/kg, po2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID470773Antifibrotic activity in rat 1097 cells assessed as inhibition of TGF-beta-stimulated [3H]proline incorporation in to collagen at 100 uM2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates.
AID1079933Acute 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
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079938Chronic 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]
AID1057547AUC (0 to infinity) in Sprague-Dawley rat at 5 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID359218Inhibition of rat RBL2H3 cell degranulation assessed as inhibition of beta-hexosamidase release after 10 mins by microplate reader assay2002Journal of natural products, Oct, Volume: 65, Issue:10
Absolute stereostructures of three new sesquiterpenes from the fruit of Alpinia oxyphylla with inhibitory effects on nitric oxide production and degranulation in RBL-2H3 cells.
AID1057548Volume of distribution at steady state in Sprague-Dawley rat at 5 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1549797Agonist activity at human TRPM8 expressed in HEK293 cells assessed as increase in calcium influx at 100 uM by Fluo-4-AM dye based fluorescence assay relative to calcimycin2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID470774Antifibrotic activity in rat 1097 cells assessed as inhibition of TGF-beta-stimulated [3H]proline incorporation in to collagen at 30 uM2009Bioorganic & medicinal chemistry letters, Dec-15, Volume: 19, Issue:24
Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1549772Antagonist activity at human TRPA1 expressed in HEK293 cells assessed as inhibition of CA-induced increase in calcium influx incubated for 10 mins prior to CA addition by Fluo-4-AM dye based fluorescence assayy2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID333179Antiallergic activity in ddY mouse ear at 200 mg/kg, po by passive cutaneous anaphylaxis reaction2004Journal of natural products, Sep, Volume: 67, Issue:9
Structures of new beta-carboline-type alkaloids with antiallergic effects from Stellaria dichotoma(1,2).
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID182636Cytoprotective activity against ethanol-induced gastric lesions in male conscious rats; Inactive.1992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Antiallergic and cytoprotective activity of new N-phenylbenzamido acid derivatives.
AID1057552Antifibrotic activity in rat renal mesangial cells assessed as inhibition of TGF-beta1-induced [3H]-proline incorporation into collagen at 30 uM treated 4 hrs before TGF-beta1 addition measured after 44 hrs by liquid scintillation counting2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1549771Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1549769Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx at 30 uM by Fluo-4-AM dye based fluorescence assay relative to calcimycin2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID319190Inhibition of glutathione-S-transferase activity of prostaglandin D2 synthase2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Novel prostaglandin D synthase inhibitors generated by fragment-based drug design.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079936Choleostatic 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]
AID1057541Oral bioavailability in Sprague-Dawley rat at 20 mg/kg2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1057553Antifibrotic activity in rat renal mesangial cells assessed as inhibition of TGF-beta1-induced [3H]-proline incorporation into collagen at 10 uM treated 4 hrs before TGF-beta1 addition measured after 44 hrs by liquid scintillation counting2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1549774Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as increase in calcium influx at 100 uM incubated for 10 mins prior to WS5 challenge by Fluo-4-AM dye based fluorescence assay relative to WS52019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID109999In vivo inhibitory activity against leakage of dye on ear PCA reaction 30 min after 400 mg/kg oral administration in mice2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Antiallergic principles from Alpinia galanga: structural requirements of phenylpropanoids for inhibition of degranulation and release of TNF-alpha and IL-4 in RBL-2H3 cells.
AID1057549Drug level in Sprague-Dawley rat urine at 5 mg/kg, iv2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID1623895Antagonist activity at TRPV2 (unknown origin)2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID179612Antiallergic activity against rat passive cutaneous anaphylaxis (PCA) reaction induced by 25 mg/kg of ovalbumin given iv (bolus).1992Journal of medicinal chemistry, Oct-02, Volume: 35, Issue:20
Antiallergic and cytoprotective activity of new N-phenylbenzamido acid derivatives.
AID109997In vivo inhibitory activity against leakage of dye on ear PCA reaction 30 min after 200 mg/kg oral administration in mice2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Antiallergic principles from Alpinia galanga: structural requirements of phenylpropanoids for inhibition of degranulation and release of TNF-alpha and IL-4 in RBL-2H3 cells.
AID232660Ratio of inhibitory activity on proliferation of human coronary artery smooth muscle cells to that of human coronary artery endothelial cells2001Bioorganic & medicinal chemistry letters, Feb-26, Volume: 11, Issue:4
Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells.
AID1549796Dissociation constant, pKa of the compound at pH 7.42019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1057545Drug level in Sprague-Dawley rat urine at 20 mg/kg, po2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1474064Drug concentration at steady state in human at 80 to 600 mg, po QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID109995In vivo inhibitory activity against leakage of dye on ear PCA reaction 30 min after 100 mg/kg oral administration in mice2003Bioorganic & medicinal chemistry letters, Oct-06, Volume: 13, Issue:19
Antiallergic principles from Alpinia galanga: structural requirements of phenylpropanoids for inhibition of degranulation and release of TNF-alpha and IL-4 in RBL-2H3 cells.
AID1549773Agonist activity at human TRPM8 expressed in HEK293 cells assessed as increase in calcium influx at 30 uM by Fluo-4-AM dye based fluorescence assay relative to calcimycin2019European journal of medicinal chemistry, May-15, Volume: 170N-Cinnamoylanthranilates as human TRPA1 modulators: Structure-activity relationships and channel binding sites.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID333181Inhibition of beta-hexosaminidase in anti-DNP IgE sensitized rat RBL2H3 cells after 10 mins2004Journal of natural products, Sep, Volume: 67, Issue:9
Structures of new beta-carboline-type alkaloids with antiallergic effects from Stellaria dichotoma(1,2).
AID337578Antiallergic activity in ip dosed ddY mouse assessed as inhibition of passive cutaneous anaphylaxis administered 15 mins before egg albumin challenge1993Journal of natural products, Feb, Volume: 56, Issue:2
Production of an anti-allergic triterpene bryonolic acid, by plant cell cultures.
AID1057535Reduction of albuminuria in (mRen-2)27 rat streptozotocin-induced diabetic nephropathy model assessed as reduction of albumin level in urine at 400 mg/kg, po qd for 8 weeks administered 8 weeks post-streptozotocin treatment by radioimmunoassay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
3',4'-Bis-difluoromethoxycinnamoylanthranilate (FT061): an orally-active antifibrotic agent that reduces albuminuria in a rat model of progressive diabetic nephropathy.
AID1474066Ratio of drug concentration at steady state in human at 80 to 600 mg, po QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347411qHTS 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) Libary2020ACS 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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
AID1798101In Vitro GST Activity Assay from Article 10.1021/jm701509k: \\Novel prostaglandin d synthase inhibitors generated by fragment-based drug design.\\2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Novel prostaglandin D synthase inhibitors generated by fragment-based drug design.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS one, , Volume: 11, Issue:10
Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (561)

TimeframeStudies, This Drug (%)All Drugs %
pre-199074 (13.19)18.7374
1990's119 (21.21)18.2507
2000's148 (26.38)29.6817
2010's153 (27.27)24.3611
2020's67 (11.94)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.10

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.

MetricThis Compound (vs All)
Research Demand Index53.10 (24.57)
Research Supply Index6.42 (2.92)
Research Growth Index4.74 (4.65)
Search Engine Demand Index88.13 (26.88)
Search Engine Supply Index2.01 (0.95)

This Compound (53.10)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials28 (4.80%)5.53%
Reviews35 (6.00%)6.00%
Case Studies52 (8.92%)4.05%
Observational1 (0.17%)0.25%
Other467 (80.10%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (12)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-Blind, Crossover, Pharmacodynamic and Pharmacokinetic Drug Interaction Study of Tranilast in Combination With Allopurinol Compared With Tranilast Alone and Allopurinol Alone in Healthy Subjects With Hyperuricemia [NCT01052987]Phase 224 participants (Anticipated)Interventional2010-01-31Completed
Efficacy and Safety of Tranilast in Patients With Cryopyrin-Associated Periodic Syndrome (CAPS): A Single-Arm Prospective Cohort Study [NCT03923140]Phase 271 participants (Anticipated)Interventional2019-05-23Recruiting
A Clinical Study of Tranilast in the Treatment of Sarcoidosis [NCT03528070]Early Phase 156 participants (Anticipated)Interventional2018-05-31Not yet recruiting
A Clinical Study of Tranilast in the Treatment of Mucinoses [NCT03490708]Early Phase 156 participants (Anticipated)Interventional2018-04-30Not yet recruiting
A Randomized, Double-Blind, Crossover, Pharmacodynamic and Pharmacokinetic Drug Interaction Study of Tranilast in Combination With Febuxostat Compared With Tranilast Alone and Febuxostat Alone in Healthy Subjects With Hyperuricemia [NCT00995618]Phase 224 participants (Actual)Interventional2009-09-30Completed
A Phase 1, Blinded, Randomised, Crossover Pilot Study to Investigate the Safety, Tolerability and Pharmacokinetics of Tranilast in Patients With Rheumatoid Arthritis on Methotrexate [NCT00717808]Phase 10 participants (Actual)Interventional2008-09-30Withdrawn(stopped due to Due to unforeseen circumstances this study will not now start.)
A Phase II, Randomized Multi-Center, Double-Blind Study of Tranilast With Concomitant Methotrexate (MTX) Compared to MTX Alone in Patients With Active Rheumatoid Arthritis (RA) [NCT00882024]Phase 2250 participants (Anticipated)Interventional2009-03-31Completed
Evaluation of Tranilast as Adjunctive Therapy Before Primary Pterygium Excision Compared With Conjunctival Autograft [NCT01003613]Phase 332 participants (Actual)Interventional2009-02-28Completed
Application of Tranilast as a Radiosensitizer in the Treatment of Radiotherapy Resistant Nasopharyngeal Carcinoma: a Phase II Clinical Study [NCT05626829]Phase 218 participants (Anticipated)Interventional2022-07-20Recruiting
[NCT00818805]Phase 450 participants (Actual)Interventional2008-07-31Completed
A Clinical Study of Tranilast in the Treatment of Scleredema Diabeticorum [NCT03512873]Early Phase 156 participants (Anticipated)Interventional2018-06-30Not yet recruiting
Effect of Inflammasome Inhibitor on High-sensitivity C-reactive Protein in Patients After Percutaneous Coronary Intervention [NCT05130892]Phase 4132 participants (Actual)Interventional2021-11-15Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00818805 (1) [back to overview]"Change in Ocular Itching Score (5-point Scale) in Subjective Symptom Questionnaire"

"Change in Ocular Itching Score (5-point Scale) in Subjective Symptom Questionnaire"

Ocular itching score was assessed using a 5 point scale, with 1 meaning no itching and 4 meaning worst itching. (NCT00818805)
Timeframe: 0-180 minutes after entering the examination room

,,,
InterventionUnits on a scale (Mean)
15 minutes30 minutes45 minutes60 minutes75 minutes90 minutes105 minutes120 minutes135 minutes150 minutes165 minutes180 minutes
Olopatadine 0.1% One Eye0.190.440.500.670.810.920.941.031.171.251.281.39
Placebo (Olopatadine)0.060.330.500.750.920.921.031.191.331.361.391.44
Placebo (Tranilast)0.080.280.560.610.780.940.971.081.191.251.331.47
Tranilast 0.5% One Eye0.110.250.360.500.670.860.861.031.141.141.141.39

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