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etretinate

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Description

retinoid : Oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof. [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 CID5282375
CHEMBL ID464
CHEBI ID4913
CHEBI ID94591
SCHEMBL ID3123
MeSH IDM0007934

Synonyms (97)

Synonym
AC-6823
etrinoate, ethyl
AB01275503-01
ro-10-9359
tegison
ethyl (2e,4e,6e,8e)-3,7-dimethyl-9-[2,3,6-trimethyl-4-(methyloxy)phenyl]nona-2,4,6,8-tetraenoate
nsc 297936
etretinatum [inn-latin]
2,4,6,8-nonanetetraenoic acid, 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-, ethyl ester, all-trans-
retinoid
ethyl all-trans-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoate
2,4,6,8-nonatetraenoic acid, 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-, ethyl ester, (all-e)-
etretinato [inn-spanish]
einecs 259-119-3
ethyl etrinoate
ccris 3615
2,4,6,8-nonatetraenoic acid, 9-(4-methoxy-2,3,6-trimethylphenyl)-, ethyl ester, (all-e-)
3,7-dimethyl-9-(4-methoxy-2,3,6-trimethylphenyl)-2,4,6,8-nonanetetraenoic acid ethyl ester
hsdb 7185
ethyl (all-e)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoate
LMPR01090046
(2e,4e,6e,8e)-9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoic acid ethyl ester
2,6,8-nonatetraenoic acid, 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-, ethyl ester, (all e)-
2,6,8-nonatetraenoic acid, 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-, ethyl ester, (all-e)-
nsc-297936
etretinate ,
54350-48-0
tigason
ro 10-9359
nsc297936
ethyl (2e,4e,6e,8e)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoate
CHEBI:4913 ,
etretinatum
etretinato
tegison (tn)
D00316
etretinate (jan/usan/inn)
NCGC00167500-01
HMS2090G06
ro-109359
CHEMBL464
ethyl 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoate
cas-54350-48-0
dtxsid0023036 ,
dtxcid603036
tox21_112501
ethyl (2e,4e,6e,8e)-9-(4-methoxy-2,3,6-trimethyl-phenyl)-3,7-dimethyl-nona-2,4,6,8-tetraenoate;etretinate
A830117
S4699
2,4,6,8-nonatetraenoic acid, 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-, ethyl ester, (2e,4e,6e,8e)-
65m2udr9ag ,
unii-65m2udr9ag
etretinate [usan:inn:ban:jan]
AKOS015889992
BRD-K36248164-001-01-8
etretinate [hsdb]
etretinate [who-dd]
etretinate [mart.]
etretinate [vandf]
etretinate [mi]
etretinate [jan]
etretinate [usan]
etretinate [orange book]
acitretin impurity b [ep impurity]
etretinate [inn]
CCG-220590
gtpl7599
SCHEMBL3123
NCGC00167500-02
tox21_112501_1
CS-3926
HQMNCQVAMBCHCO-DJRRULDNSA-N
ethyl 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoate
W-105640
isopropyl-pyridin-4-yl-aminedihydrochloride
HY-B0797
SR-05000001511-2
sr-05000001511
CHEBI:94591
SR-05000001511-1
HMS3713F22
(2e,4e,6e,8e)-ethyl 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethylnona-2,4,6,8-tetraenoate
bdbm50248000
mfcd00866624
Q554297
A16356
etretinate 100 microg/ml in acetonitrile
AS-77381
(all e)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoic acid ethyl ester
ethyl-all-trans-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoate
(2e,4e,6e,8e)-9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoic acid, ethyl ester
d05bb01
etretinatum (inn-latin)
acitretin impurity b (ep impurity)
etretinate (mart.)
etretinato (inn-spanish)
E1293

Research Excerpts

Overview

Etretinate (Tigason) is an orally administered retinoid which is used primarily for the treatment of severe keratinization disorders of the skin. Etretinate is a synthetic derivative of vitamin A that infrequently induces bone and joint abnormalities in children.

ExcerptReferenceRelevance
"Etretinate (Ro 10-9359) is a new aromatic retinoic acid derivative for the treatment of severe psoriasis and other dyskeratoses. "( Etretinate. A review of its pharmacological properties and therapeutic efficacy in psoriasis and other skin disorders.
Avery, GS; Brogden, RN; Heel, RC; Speight, TM; Ward, A, 1983
)
3.15
"Etretinate is a good alternative to other systemic treatments of PPP."( A randomized trial of etretinate (Tigason) in palmoplantar pustulosis.
Foged, E; Holm, P; Larsen, PO; Laurberg, G; Reymann, F; Roesdahle, K; Ullman, S, 1983
)
1.3
"Etretinate (Tigason) is an orally administered retinoid which is used primarily for the treatment of severe keratinization disorders of the skin. "( [Teratogenic effects of etretinate in humans].
Bounameaux, Y; Fisch, T; Happle, R; Traupe, H, 1984
)
2.02
"Etretinate was found to be an effective therapy for this skin disorder."( Etretinate therapy for psoriasis: clinical responses, remission times, epidermal DNA and polyamine responses.
Kaplan, RP; Lowe, NJ; Russell, DH, 1983
)
2.43
"Etretinate is an aromatic retinoid given orally to treat severe psoriasis, a chronic disease that often requires long-term therapy."( The safety of etretinate as long-term therapy for psoriasis: results of the etretinate follow-up study.
Baughman, RD; Ellis, CN; Fitzgerald, E; Goldfarb, MT; Lowe, N; Stern, RS, 1995
)
2.09
"Etretinate is a safe and effective adjunctive treatment for recalcitrant palmar and plantar hyperkeratosis in erythrodermic CTCL patients undergoing photopheresis."( Etretinate as an effective adjunctive therapy for recalcitrant palmar/plantar hyperkeratosis in patients with erythrodermic cutaneous T cell lymphoma undergoing photopheresis.
Harris, HR; Lim, HW, 1995
)
3.18
"Etretinate is a synthetic aromatic retinoid used in the treatment of psoriasis and other disorders affecting the skin. "( Simultaneous determination of etretinate, acitretin and their metabolites in perfusate, perfusate plasma, bile or hepatic tissue with reversed-phase high-performance liquid chromatography.
Decker, MA; Zimmerman, CL, 1995
)
2.02
"Etretinate is a synthetic derivative of vitamin A that infrequently induces bone and joint abnormalities in children."( [Bone complications from chronic etretinate intoxication in children].
Bretagne, MC; Cointin, M; Cuny, JF; Sommelet-Olive, D, 1990
)
1.28
"Etretinate is an aromatic retinoid extensively used on Dermatology. "( Morphological and biochemical alterations in growing rats induced by etretinate.
Amo Bernal, C; Fuentes García, A; Méndez Sánchez, A; Sierra Plana, MA; Sinisterra Gago, JV, 1989
)
1.95
"Etretinate is a potent retinoid that is used in the treatment of psoriasis."( Evaluation of retinoids as inhibitors of [3H] all-trans retinoic acid binding to cellular retinoic acid-binding protein in rat skin and testes.
Bazzano, G; Chou, A; Madani, K, 1986
)
0.99
"Etretinate is a synthetic vitamin A derivate given orally for the treatment of severe skin psoriasis. "( Comparison of etretinate (Tigason) and parenteral gold in the treatment of psoriatic arthropathy.
Laulainen, M; Reunala, T; Seppälä, J, 1988
)
2.08
"Etretinate is a valuable addition to the treatment of psoriasis. "( Short-term and long-term considerations in the management of psoriasis with retinoids.
Ellis, CN; Goldfarb, MT; Voorhees, JJ, 1987
)
1.72
"Etretinate is a retinoid given orally for the treatment of psoriasis and many other dermatoses. "( Etretinate therapy.
Ellis, CN; Voorhees, JJ, 1987
)
3.16
"Etretinate is an aromatic retinoid and derivative of vitamin A soon to be approved for general use in the U.S. "( Long-term effects of etretinate on the liver in psoriasis.
Camuto, P; Feiner, H; Orbuch, P; Shupack, J; Sidhu, G; Tobias, H, 1987
)
2.03
"Etretinate (RO 10-9359) is a synthetic retinoid used instead of Vitamin A--toxic in large dose--during treatment of some skin diseases. "( [Effects of administration of moderate doses of etretinate (RO 10-9359) on rats deficient in vitamin A].
Garcin, H; Higueret, D; Higueret, P; Suberville, C; Taruoura, D, 1985
)
1.97

Effects

Etretinate has proven to be effective in the treatment of psoriasis. The drug has been implicated in the formation of spinal hyperostoses and calcification of extraspinal ligaments in patients taking the drug for many years.

ExcerptReferenceRelevance
"Etretinate has proven to be effective in the treatment of psoriasis. "( Effects of etretinate on keratinocyte proliferation and secretion of interleukin-1 alpha (IL-1 alpha) and IL-8.
Iwatsuki, K; Kaneko, F; Maruyama, K; Nihei, Y; Ono, I; Zhang, JZ, 1994
)
2.12
"Etretinate has been known to produce a variety of skeletal manifestations when administered for prolonged periods. "( Bone mineral density of the lumbar spine in psoriatic patients with long term etretinate therapy.
Morimoto, S; Nomura, M; Ogihara, T; Okada, N; Yoshikawa, K, 1994
)
1.96
"Etretinate has proven efficacy in advanced mycosis fungoides."( Combined treatment with oral etretinate and electron beam therapy in patients with cutaneous T-cell lymphoma (mycosis fungoides and Sézary syndrome).
Jones, G; McLean, J; Roberts, J; Rosenthal, D; Sauder, DN, 1992
)
1.3
"Etretinate has been implicated in the formation of spinal hyperostoses and calcification of extraspinal ligaments in patients who had taken the drug for many years."( [Rheumatologic effects of etretinate].
Aussedat, R; Beurey, J; Cointin, M; Cuny, JF; Schmutz, JL; Terver, MN; Weber, M, 1989
)
1.3
"Etretinate therapy has been shown to produce both prophylactic and therapeutic effects on premalignant epithelial tumors of mice."( Preventative effect of etretinate therapy on multiple actinic keratoses.
Watson, AB, 1986
)
1.3

Treatment

Etretinate-pretreated cells underwent apoptosis in response to ALA-based PDT. Etretinate treatment significantly augmented suppressor function over baseline values at 1, 3, and 6 months.

ExcerptReferenceRelevance
"Etretinate-pretreated cells underwent apoptosis in response to ALA-based PDT."( Etretinate enhances the susceptibility of human skin squamous cell carcinoma cells to 5-aminolaevulic acid-based photodynamic therapy.
Akita, Y; Ishida, N; Kuhara, T; Matsumoto, Y; Nakano, A; Takeo, T; Tamada, Y; Watanabe, D; Yamashita, N; Yanagishita, T, 2009
)
2.52
"In etretinate-treated embryos, neuroepithelial cells proliferated in the presacral region on E9.5."( Sharing of the same embryogenic pathway in anorectal malformations and anterior sacral myelomeningocele formation.
Liu, Y; Ohkawa, H; Sugiyama, F; Yagami, K, 2003
)
0.83
"Etretinate treated MRL/lpr mice did not have skin lesions or dermatopathological characteristics including an increase in cells infiltrating the dermis."( The effects of vitamin A derivative etretinate on the skin of MRL mice.
Furukawa, F; Ikeda, T; Nishide, T; Ohtani, T, 2005
)
1.32
"Etretinate treatment proved beneficial during the first year of therapy."( Ichthyosis hystrix (Curth-Macklin). Light and electron microscopic studies performed before and after etretinate treatment.
Kanerva, L; Karvonen, J; Lauharanta, J; Niemi, KM; Oikarinen, A; Ruokonen, A, 1984
)
1.2
"Etretinate treatment produced a marked shedding of the horny layer without significant improvement of the clinical appearance."( [Generalized ichthyosis associated with a spastic syndrome of the lower limbs, a variant of Sjögren-Larsson syndrome? Light and electron microscopy study of ichthyosis and its evolution with oral etretinate treatment].
Frenk, E; Gharbi, R; Lahmar, L; Walzer, C, 1984
)
1.18
"Etretinate treatment significantly reduced ODC activity in both involved and uninvolved skin in psoriatics to a similar level of activity before any improvement in clinical appearance was noted."( Etretinate treatment for psoriasis inhibits epidermal ornithine decarboxylase.
Breeding, J; Kaplan, R; Lowe, NJ, 1982
)
2.43
"With etretinate treatment, the verrucous nodules completely disappeared within two months."( A reactive acrosyringeal proliferation in a patient with ectodermal dysplasia: eccrine syringofibroadenoma-like lesion.
Hattori, Y; Utani, A, 1999
)
0.76
"Etretinate treatment significantly augmented suppressor function over baseline values at 1, 3, and 6 months."( Etretinate augments interferon beta-1b effects on suppressor cells in multiple sclerosis.
Arnason, BG; Jensen, MW; Pliskin, N; Qu, ZX; White, D, 2001
)
2.47
"Etretinate treatment at a dose of 10 mg twice or three times daily augments suppressor cell function in patients with MS receiving interferon beta-1b. "( Etretinate augments interferon beta-1b effects on suppressor cells in multiple sclerosis.
Arnason, BG; Jensen, MW; Pliskin, N; Qu, ZX; White, D, 2001
)
3.2
"Etretinate treatment did not alter the type or degree of otitis externa."( Use of etretinate for treatment of primary keratinization disorders (idiopathic seborrhea) in cocker spaniels, west highland white terriers, and basset hounds.
Backus, KQ; Ihrke, PJ; Power, HT; Stannard, AA, 1992
)
1.46
"Etretinate treatment resulted in a substantial decrease in tumor necrosis factor-alpha levels, whereas an unpredictable increase was found during the late phase of cyclosporine treatment."( Differential effects of cyclosporine and etretinate on serum cytokine levels in patients with psoriasis.
Imanishi, K; Nagashima, M; Sagawa, Y; Shiohara, T, 1992
)
1.27
"Etretinate treatment gave good results in terms of cutaneous modifications: reduction of hyperkeratosis, disappearance of ectropion and eclabium."( Harlequin fetus: a case report.
Bonomi, A; Capalbo, P; Crosato, M; Gomirato, G,
)
0.85
"Etretinate treatment of bullous congenital ichthyosiform erythroderma is more difficult, and it is advisable to begin with a low dosis of 0.25-0.5 mg/kg."( Retinoids in disorders of keratinization: their use in adults.
Happle, R; Traupe, H; van de Kerkhof, PC, 1987
)
0.99
"The etretinate-treated group still showed clinical improvement and a significantly lower pustule count after 12 weeks."( Low-dose etretinate in the maintenance of remission of palmoplantar pustular psoriasis.
Marks, JM; Puttick, L; White, SI, 1986
)
1.17
"Oral treatment with etretinate brought about disappearance of the pseudo-ainhums and normalization of the digital blood circulation."( Mutilating palmoplantar keratoderma successfully treated with etretinate.
Wereide, K, 1984
)
0.82
"Treatment with etretinate alone does not affect the normal epithelial growth rate or normal differentiation."( Prevention and reversal by a retinoid of 3,4-benzpyrene- and cigarette smoke condensate-induced hyperplasia and metaplasia of rodent respiratory epithelia in organ culture.
Bollag, W; Lasnitzki, I, 1982
)
0.6
"The treatment with etretinate did not influence these structures."( New observations on the fine structure of lamellar ichthyosis and the effect of treatment with etretinate.
Kanerva, L; Lassus, A; Lauharanta, J; Niemi, KM, 1983
)
0.8
"Treatment with etretinate resulted in remission of the fully developed KA and reduced the occurrence of new ones."( [Multiple keratoacanthomas (Witten-Zak type) in prurigo simplex subacuta].
Boateng, B; Hornstein, OP; Kiesewetter, F; von den Driesch, P, 1995
)
0.63
"Treatment with etretinate was successful."( [Filiform keratosis].
Christophers, E; Fölster-Holst, R, 1994
)
0.63
"Treatment with etretinate was effective for the palms and fingers, but resulted in no improvement of the keratoderma of the soles."( Partial improvement of Olmsted syndrome with etretinate.
Hayashi, K; Ichihashi, M; Nakagawa, K; Shimizu, R; Ueda, M, 1993
)
0.89
"Treatment with etretinate (50 mg/day) proved effective on skin lesions."( Sweet's syndrome in a patient with idiopathic myelofibrosis and thymoma-myasthenia gravis-immunodeficiency complex: efficacy of treatment with etretinate.
Altomare, G; Capella, GL; Frigerio, E,
)
0.67
"The treatment with etretinate induced a decrease of the duodenal and jejunal disaccharidase activity."( [Effect of etretinate on the activity of intestinal disaccharidases].
Kietzmann, M; Lubach, D, 1992
)
0.99
"Treatment with etretinate did not benefit the daughter."( Familial occurrence of KID (keratitis, ichthyosis, deafness) syndrome. Case reports of a mother and daughter.
Blanchet-Bardon, C; Civatte, J; Lorette, G; Nazzaro, V, 1990
)
0.62
"Treatment with etretinate and in a later phase with indomethacin and prednisolone was not effective, except for a limited initial response of the tumour to etretinate."( Xeroderma pigmentosum: squamous cell carcinoma of the tongue.
Keukens, F; Kleijer, WJ; Oosterhuis, JW; Panders, AK; van Voorst Vader, PC; Vinks, S, 1989
)
0.62
"Treatment with etretinate is known to be effective for patients with psoriasis. "( [A case of psoriasis vulgaris whose lipoprotein lipase activity decreased during treatment with etretinate].
Mori, S; Noma, A; Seishima, M, 1989
)
0.85
"Treatment with etretinate permits a less aggressive surgical excision and recurrence rate than surgical excision alone."( Nevoid basal cell carcinoma syndrome: combined etretinate and surgical treatment.
Camacho, F; Sanchez-Conejo-Mir, J, 1989
)
0.87
"The treatment with etretinate initially improved the clinical picture, but it had to be discontinued because of personality changes, particularly depressive crisis."( [Progressive symmetric erythrokeratodermia. Report of a case with delayed onset treated by etretinate].
Almagro Sanchez, M; Borbujo Martinez, J; Casado Jimenez, M; Jimenez Acosta, F; Martinez Gomez, W; Soto Melo, J, 1988
)
0.81
"Treatment with etretinate resulted in a marked improvement of the palmar and plantar skin lesions."( [The Papillon-Lefevre syndrome (keratosis palmoplantaris with periodontopathy). Treatment with etretinate].
Happle, R; Traupe, H; Wehrmann, W, 1985
)
0.83
"Treatment with etretinate in a patient with multiple keratoacanthoma is described. "( Immunological findings during treatment of multiple keratoacanthoma with etretinate.
Blitstein-Willinger, E; Haas, N; Nürnberger, F; Stüttgen, G, 1986
)
0.86

Toxicity

Long-term etretinate therapy (up to 4 years) does not appear to be accompanied by a substantial increased risk of major adverse effects. The results indicate that the intracellular concentrations combined with the intrinsic sensitivities of each cell line to etretinates and vindesine determines the toxic response.

ExcerptReferenceRelevance
"Dermatitis occurring as a side effect in psoriatic patients during oral administration of the retinoid acid derivative Ro 10-9359 is described."( [Side effects of oral retinoid Ro 10-9359 on the unaffected skin of psoriatic patients: retinoid dermatitis].
Rüst, O; Tufli, T, 1979
)
0.26
" Hepatic toxicity is an uncommon but serious side-effect of several Vitamin A derivatives which may lead to cirrhosis."( Hepatic toxicity of vitamin A and synthetic retinoids.
Boyer, JL; Fallon, MB,
)
0.13
" The results indicate that the intracellular concentrations combined with the intrinsic sensitivities of each cell line to etretinate and vindesine determines the toxic response."( Cytotoxicity of etretinate and vindesine.
Gaukroger, JM; MacKie, R; Wilson, L, 1985
)
0.82
" The absence of toxic effects on the bones by Ro 15-1570 was confirmed by X-ray-film examinations, densitometry of the X-rayed femora and tibiae, examination of the thickness of the femoral and tibial compacta in histological slides plus the determination of the femoral ash weight and its main inorganic constituents (calcium, magnesium, sodium, and potassium)."( Ro 15-1570, a new sulfur-containing retinoid devoid of bone toxicity in rats.
Kistler, A; Sterz, H; Teelmann, K, 1984
)
0.27
" Based on our 6-month evaluation, etretinate does not produce a consistent toxic effect on the liver."( A study of potential hepatotoxicity of etretinate used in the treatment of psoriasis.
Glazer, SD; Roenigk, HH; Sparberg, M; Yokoo, H, 1982
)
0.81
" In the last 2 patients liver biopsy showed changes of toxic hepatitis."( Side effects due to RO 10-9359 (Tigason). A retrospective study.
Foged, EK; Jacobsen, FK, 1982
)
0.26
"Osteoporosis has been observed with chronic hypervitaminosis A but has not been established as a toxic effect of synthetic retinoid therapy in humans."( Osteoporosis is a toxic effect of long-term etretinate therapy.
Abangan, DL; DiGiovanna, JJ; Reynolds, JC; Sollitto, RB; Steinberg, SM, 1995
)
0.55
"This 5-year prospective study of a cohort of 956 patients with psoriasis treated with etretinate assessed the frequency of adverse events in relation to total use and in relation to the frequency of these events in control populations."( The safety of etretinate as long-term therapy for psoriasis: results of the etretinate follow-up study.
Baughman, RD; Ellis, CN; Fitzgerald, E; Goldfarb, MT; Lowe, N; Stern, RS, 1995
)
0.88
"With proper patient selection and monitoring, long-term etretinate therapy (up to 4 years) does not appear to be accompanied by a substantial increased risk of major adverse effects."( The safety of etretinate as long-term therapy for psoriasis: results of the etretinate follow-up study.
Baughman, RD; Ellis, CN; Fitzgerald, E; Goldfarb, MT; Lowe, N; Stern, RS, 1995
)
0.9
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32

Pharmacokinetics

The use of the carboxylic acid ester analogue, etretinate, has been hampered by an extremely long elimination half-life of up to 120 days for this drug. The purpose of the present study was to investigate the pharmacokinetic profile of Etretinate and acitretin in a genetically obese rodent model, the Zucker rat.

ExcerptReferenceRelevance
" The purpose of the present study was to investigate the pharmacokinetic profile of etretinate and acitretin in a genetically obese rodent model, the Zucker rat."( Pharmacokinetic profile of two aromatic retinoids (etretinate and acitretin) in the obese Zucker rat.
Blouin, RA; McNamara, PJ, 1990
)
0.76
" When compared with a matched group a significantly higher mean value for the maximum plasma concentration Cmax (992 nmol/L +/- 94 SE vs 721 nmol/L +/- 35 SE) for methotrexate was found (P less than ."( Interaction of etretinate with methotrexate pharmacokinetics in psoriatic patients.
Jakobsen, P; Kragballe, K; Larsen, FG; Nielsen-Kudsk, F; Schrøder, H, 1990
)
0.63
" The large Vdss (214 +/- 228 liters/kg) of ET and terminal half-life of greater than 300 hr indicated the wide distribution and prolonged storage of ET in the tissues."( The pharmacokinetics of etretinate and its metabolites in the dog.
Massarella, JW; Thongnopnua, P; Zimmerman, CL,
)
0.44
" Hitherto, the use of the carboxylic acid ester analogue, etretinate, has been hampered by an extremely long elimination half-life of up to 120 days for this drug."( Pharmacokinetics of etretin and etretinate during long-term treatment of psoriasis patients.
Jakobsen, P; Kragballe, K; Larsen, CG; Larsen, FG; Nielsen-Kudsk, F, 1988
)
0.8
" These differences between the results obtained in vivo and in vitro could be resolved by pharmacokinetic investigations using HPLC methods."( Transplacental pharmacokinetics of teratogenic doses of etretinate and other aromatic retinoids in mice.
Kochhar, DM; Kraft, JC; Löfberg, B; Nau, H; Reiners, J, 1988
)
0.52
"The pharmacokinetic profile of 14C-etretinate, a retinoid that is effective in the treatment of psoriasis, was studied in six healthy male volunteers and two biliary T-tube patients."( Pharmacokinetics of 14C-etretinate in healthy volunteers and two patients with biliary T-tube drainage.
Bugge, CJ; Carter, DE; Colburn, WA; Crews, T; Cunningham, W; Dickerson, J; Lucek, RW; Vane, FM,
)
0.72
" Pharmacokinetically, the major difference between isotretinoin and etretinate is the much longer elimination half-life (120 days) of etretinate following long term administration."( Clinical pharmacokinetics of the retinoids.
Colburn, WA; Lucek, RW,
)
0.37
"The clinical pharmacokinetic profiles of two orally administered retinoids, isotretinoin and etretinate, are discussed and compared."( Pharmacokinetics of the retinoids isotretinoin and etretinate. A comparative review.
Brazzell, RK; Colburn, WA, 1982
)
0.74
" The purpose of this study was to validate an HPLC method for the determination of acitretin and etretinate and to investigate the pharmacokinetic characteristics of acitretin in healthy Korean subjects."( A fully validated HPLC method for the simultaneous determination of acitretin and etretinate in plasma and its application to a pharmacokinetic study in healthy Korean subjects.
Chun, MR; Huh, WS; Kim, DW; Kim, HG; Kim, HK; Kim, JW; Kim, MH; Kim, YG; Lee, JH; Lee, SY; Park, HD; Youn, JI, 2009
)
0.8
" The mean +/- SD pharmacokinetics of acitretin in Koreans were as follows: Cmax 148."( A fully validated HPLC method for the simultaneous determination of acitretin and etretinate in plasma and its application to a pharmacokinetic study in healthy Korean subjects.
Chun, MR; Huh, WS; Kim, DW; Kim, HG; Kim, HK; Kim, JW; Kim, MH; Kim, YG; Lee, JH; Lee, SY; Park, HD; Youn, JI, 2009
)
0.58
"A simple HPLC method for the simultaneous determination of acitretin and etretinate was validated, and the pharmacokinetic characteristics of acitretin in the Korean population were investigated."( A fully validated HPLC method for the simultaneous determination of acitretin and etretinate in plasma and its application to a pharmacokinetic study in healthy Korean subjects.
Chun, MR; Huh, WS; Kim, DW; Kim, HG; Kim, HK; Kim, JW; Kim, MH; Kim, YG; Lee, JH; Lee, SY; Park, HD; Youn, JI, 2009
)
0.81

Compound-Compound Interactions

The present study shows that acitretin is as effective as etretinate in the combination with bath PUVA.

ExcerptReferenceRelevance
" The present study shows that acitretin is as effective as etretinate in the combination with bath PUVA."( A double-blind comparison of acitretin and etretinate in combination with bath PUVA in the treatment of extensive psoriasis.
Geiger, JM; Lauharanta, J, 1989
)
0.78
"Eleven patients with mycosis fungoides (MF) were treated with recombinant alpha-interferon (rIFN-alpha 2a2) in combination with etretinate (seven patients) or alone."( Treatment of mycosis fungoides with recombinant interferon-alpha 2a2 alone and in combination with etretinate.
Hammer, R; Kaltoft, K; Søgaard, H; Thestrup-Pedersen, K; Zachariae, H, 1988
)
0.7
"Twenty five patients with severe and extensive psoriasis were treated with trimethylpsoralen (trioxsalen) bath plus ultraviolet A (bath PUVA) combined with oral retinoid, etretinate (Ro 10-9359)."( Trimethylpsoralen bath plus ultraviolet A combined with oral retinoid (etretinate) in the treatment of severe psoriasis.
Fräki, JE; Hollmen, A; Väätäinen, N, 1985
)
0.7
" The retinoids given in combination with MMC produced additive effects."( [Inhibitory effects of aromatic retinoic acid analog, administered alone or in combination with mitomycin C, on the in vitro growth of rat bladder carcinoma cells].
Fujita, J; Yoshida, O, 1984
)
0.27
"An aromatic retinoic acid analog (Ro 10-9359) was given orally in combination with intraperitoneal administration of mitomycin C (MMC), in an attempt to reduce the toxicity and enhance the therapeutic effect."( Therapeutic effect of an aromatic retinoic acid analog on rats with bladder carcinoma upon administration alone or in combination with mitomycin C.
Fujita, J; Miyakawa, M; Tokuda, H; Yoshida, O, 1982
)
0.26
" The difference between the effect of MMC alone and that of MMC given in combination with Ro 10-9359 was not statistically significant."( Therapeutic effect of a retinoid (Ro 10-9359) on rats with bladder tumours induced by N-butyl-N-(4-hydroxybutyl)-nitrosamine upon administration alone or in combination with mitomycin C.
Fujita, J; Ito, Y; Tokuda, H; Yoshida, O, 1983
)
0.27
" Based on the findings, the antitumor effects of a selected retinoid either alone or in combination with cisplatin were also investigated in a preclinical mouse melanoma model."( Comparison of the in vitro and in vivo effects of retinoids either alone or in combination with cisplatin and 5-fluorouracil on tumor development and metastasis of melanoma.
Chan, SY; Ho, PC; Liu, X, 2008
)
0.35
"Cell proliferation and invasion analyses of murine melanoma B16-F10 cells were assessed in the presence of different retinoids, either alone or in combination with cisplatin (CDDP) or 5-fluorouracil (5-FU)."( Comparison of the in vitro and in vivo effects of retinoids either alone or in combination with cisplatin and 5-fluorouracil on tumor development and metastasis of melanoma.
Chan, SY; Ho, PC; Liu, X, 2008
)
0.35

Bioavailability

Etretinate is an aromatic retinoid useful in the treatment of psoriasis and other skin disorders. The maximum fraction disappearing from the intestinal lumen was approximately 0.5%.

ExcerptReferenceRelevance
" Monitoring of plasma concentrations of etretinate, acitretin and 13-cis-acitretin by HPLC revealed sufficient short-time absorption (4 h) and bioavailability of the drug (30 days; two out of three patients)."( Elephantiasis nostras verrucosa: beneficial effect of oral etretinate therapy.
Biczó, S; Fekete, J; Gollnick, H; Orfanos, CE; Reupke, HJ; Rinck, G; Szabó, M; Zouboulis, CC, 1992
)
0.79
" Whether concomitant retinoid administration influences the bioavailability of 8-MOP was considered an interesting question."( [Influence of retinoids on the bioavailability of methoxy-8-psoralen].
Amblard, P; Beani, JC; Beriel, H; Berthod, F; Boitard, M; Bonnot, D; Reymond, JL, 1991
)
0.28
" Peak circulating concentrations of parent all-trans-retinoic acid were less than those observed after an equivalent oral dose, but prolonged absorption from the skin appears to contribute to high total bioavailability of topical retinoid."( Percutaneous retinoid absorption and embryotoxicity.
Allen, PV; Berry, DL; Sharma, RP; Willhite, CC, 1990
)
0.28
" Administration of ET, ETA, and c-ETA by several routes of administration allowed the use of a physiologically based model to assess the relative contributions of absorption and presystemic metabolism to the oral bioavailability of these compounds."( The pharmacokinetics of etretinate and its metabolites in the dog.
Massarella, JW; Thongnopnua, P; Zimmerman, CL,
)
0.44
"Since etretinate, an aromatic retinoid useful in the treatment of psoriasis and other skin disorders is lipid-soluble, it may be poorly absorbed in the absence of a fat load."( Etretinate: effect of milk intake on absorption.
DiGiovanna, JJ; Gantt, G; Gross, EG; McClean, SW; Peck, GL; Ruddel, ME, 1984
)
2.19
"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

This study evaluated the maximum permitted dosage of etretinate (75 mg/day) as the first mode of systemic treatment of patients with symptomatic oral lichen planus. Chronic dosing of Etretinate with milk or a high fat meal compared with fasting conditions will result in higher concentrations.

ExcerptRelevanceReference
" Secondary maxima were induced by administering ethanol alone at 5 and 8 h after dosing with acitretin."( A potentially new metabolic pathway: ethyl esterification of acitretin.
Chou, RC; Huselton, CA; Wiegand, UW; Wyss, R, 1992
)
0.28
" In addition we advise that dosage should not exceed 1 mg/kg/day."( Bone changes and their significance in children with ichthyosis on long-term etretinate therapy.
Atherton, DJ; Harper, JI; Judge, MR; Paige, DG; Shaw, DG, 1992
)
0.51
"This study evaluated the maximum permitted dosage of etretinate (75 mg/day) as the first mode of systemic treatment of patients with symptomatic oral lichen planus."( Efficacy of etretinate (Tigason) in symptomatic oral lichen planus.
Gorsky, M; Raviv, M, 1992
)
0.91
"These preliminary findings suggest that etretinate, at the dosage administered, may provide therapeutic efficacy for solar-induced preneoplastic lesions in the dog, particularly for those multifocal lesions not easily managed by local methods of therapy."( Clinical evaluation of etretinate for the treatment of canine solar-induced squamous cell carcinoma and preneoplastic lesions.
Marks, SL; Power, HT; Song, MD; Stannard, AA, 1992
)
0.86
" The in vitro incubation was performed using rat and human liver 12,000 g supernatant, and the in vivo experiment was conducted in rats after oral dosing of acitretin."( A newly discovered xenobiotic metabolic pathway: ethyl ester formation.
Chou, RC; Huselton, CA; Wiegand, UW; Wyss, R, 1991
)
0.28
" Using the standard dosage of 1 mg/kg/day, 3 patients showed exacerbation of cutaneous lesions 4-6 weeks after initiation of treatment."( Exacerbation of porokeratosis during etretinate therapy.
Knobler, RM; Neumann, RA, 1990
)
0.55
" and 161 ng/ml for A 4h after dosing (tmax)."( [Pharmacokinetics of etretinate, acitretin and 13-cis-acitretin: new results and advantages of blood level oriented clinical use].
Bitterling, T; Gollnick, H; Orfanos, CE; Rinck, G, 1990
)
0.6
" Pairs of obese and lean Zucker rats were dosed intravenously (0."( Pharmacokinetic profile of two aromatic retinoids (etretinate and acitretin) in the obese Zucker rat.
Blouin, RA; McNamara, PJ, 1990
)
0.53
" In the rodent, overt skin toxicity under continued dosing could increase the amounts of retinoid penetrating the skin and reaching the embryo."( Percutaneous retinoid absorption and embryotoxicity.
Allen, PV; Berry, DL; Sharma, RP; Willhite, CC, 1990
)
0.28
" We advocate use of the minimum effective dosage and regular monitoring of patients."( [Bone complications from chronic etretinate intoxication in children].
Bretagne, MC; Cointin, M; Cuny, JF; Sommelet-Olive, D, 1990
)
0.56
" We tried oral etretinate for 4 years at a initial dosage of 30 mg per day for the possible prevention of new skin cancers."( [A case of xeroderma pigmentosum treated by oral etretinate].
Chang, HR; Hashimoto, Y; Iizuka, H; Ikenaga, M; Matsumoto, M; Ohkuma, N, 1990
)
0.89
" Steady state trough concentrations of acitretin in nonpregnant animals following etretinate multiple dosing reached their peak levels (53 ng/ml) at day 7 and declined to 16 ng/ml at day 19."( Influence of pregnancy on the pharmacokinetic disposition of two aromatic retinoids (etretinate and acitretin) in the rat. II. Single and multiple oral dosing studies.
Brouwer, KR; McNamara, PJ,
)
0.58
" Retinoids were given by gavage 3 times weekly either at low dosage (2000 IU vitamin A or 4 mg etretinate per kg body weight) or high dosage (10,000 IU vitamin A or 20 mg etretinate per kg body weight)."( Effects of oral retinoid (vitamin A and etretinate) therapy on photocarcinogenesis in hairless mice.
Kelly, GE; Meikle, WD; Sheil, AG, 1989
)
0.76
" An inverse relationship was found between the dosage of etretinate and the number of infiltrating polymorphonuclear leukocytes."( Etretinate modulates the leukotriene B4 induced intra-epidermal accumulation of polymorphonuclear leukocytes.
Lammers, AM; van de Kerkhof, PC, 1987
)
1.96
" The efficacy, safety, indications and dosage schedules for this combination therapy are discussed."( [Treatment of erythrodermic and pustulous psoriasis with a combination of methotrexate and etretinate].
Allegue Rodriguez, F; Freire Murgueytio, P; Ledo Pozueta, A; Moreno Izquierdo, R; Sendagorta Gomendio, E, 1988
)
0.5
"To evaluate the clinical-effectiveness of etretinate in the treatment of papilloma virus infections, 20 children with extensive warts were given this oral retinoid for a period not exceeding three months at a dosage of 1 mg per kg per day."( Treatment of extensive warts with etretinate: a clinical trial in 20 children.
Cerri, D; Gelmetti, C; Menni, S; Schiuma, AA, 1987
)
0.82
" The dosage was 1,5 mg/kg body-weight."( [Etretinate therapy in solitary keratoacanthomas].
Mensing, H; Wagner, G, 1988
)
1.19
" The drug was given 75 mg/day for 1 month before dosage was reduced to 50 mg/day."( Failure of etretinate in epidermodysplasia verruciformis.
Kowalzick, L; Mensing, H, 1986
)
0.66
" These data indicate that chronic dosing of etretinate with milk or a high fat meal compared with fasting conditions will result in higher concentrations of etretinate, which may ultimately lead to higher metabolite concentrations."( Effect of meals on the kinetics of etretinate.
Blumenthal, HP; Buggé, CJ; Colburn, WA; Gibson, DM; Rodriguez, LC,
)
0.67
" Maintenance or intermittent dosing usually results in a prolongation of remission."( Clinical pharmacokinetics of the retinoids.
Colburn, WA; Lucek, RW,
)
0.13
" A single 100 mg dose was initially given, followed 2 days later by approximately 170 days of multiple dosing with 25 mg one, two, three, or four times a day depending on the subject's response and tolerance."( Etretinate kinetics during chronic dosing in severe psoriasis.
Buggé, C; Colburn, W; Cunningham, WJ; Franz, T; Massarella, J; Rodriguez, L; Vane, F, 1985
)
1.71
" Striking features were the low dosage required to control the disease (as little as 10 mg per week) and the eventual transition of the clinical features to those of psoriasis vulgaris."( Generalized pustular psoriasis in a child.
van de Kerkhof, PC, 1985
)
0.27
" The dosage corresponded to that applied in psoriasis."( [Therapeutic results with the aromatic retinoid (Tigason) in Sharp syndrome and progressive scleroderma].
Bräuninger, W; Uhlmann, A, 1985
)
0.27
" 16 patients, 13 suffering from severe psoriasis and 3 from congenital disorders of keratinization previously treated with etretinate, received Ro 12-7554 at a mean daily dosage of 12."( Pilot study of a new retinoid, Ro 12-7554, in psoriasis and in some congenital disorders of keratinization.
Bounameaux, Y; Ott, F, 1983
)
0.47
" Reduction of the oral prednisone dosage provoked a severe exacerbation, with erythroderma associated with massive pustule formation."( Subcorneal pustular dermatosis with vesiculo-bullous eruption. Demonstration of subcorneal IgA deposits and a leukocyte chemotactic factor.
Iwase, Y; Iwatsuki, K; Tagami, H; Yamada, M, 1983
)
0.27
" Furthermore, the dose-response curve to Con A changed toward normal and the suppressor cell activity regulating Con A responses tended to increase."( Cell-mediated immunity in Darier's disease: effect of systemic retinoid therapy.
Eskola, J; Jansén, CT; Soppi, AM; Soppi, E, 1982
)
0.26
" During multiple dosing of etretinate, a very slow terminal elimination phase is observed which is not detected after single-dose administration."( Pharmacokinetics of the retinoids isotretinoin and etretinate. A comparative review.
Brazzell, RK; Colburn, WA, 1982
)
0.81
" A comparison of the dose-response curves for induction of terata following treatment with etretinate or all-trans-retinoic acid revealed that etretinate was twice as potent as a teratogen in the hamster as all-trans-retinoic acid."( Teratogenic dose-response relationships of etretinate in the golden hamster.
Ferm, VH; Willhite, CC; Williams, KJ, 1984
)
0.75
" Isotretinoin also showed a small but significant reduction in tibial breaking strain, but with a shallow dose-response curve in the range of 50-150 mg/kg."( Evaluation of hypervitaminosis A in the rat by measurement of tibial bone breaking strain.
Cashin, CH; Lewis, EJ, 1984
)
0.27
" Methotrexate dosing was tapered, and the patient continued to do well on etretinate alone."( Treatment of generalized pustular psoriasis with etretinate (Ro 10-9359) and methotrexate.
Roenigk, HH; Rosenbaum, MM, 1984
)
0.75
" It is concluded that the combination of the aromatic retinoid (Ro 10-9359) given in low dosage orally with corticosteroids topically is as effective as therapy with the retinoid in high dosage alone, but with markedly less side-effects."( Combined treatment of psoriasis with a new aromatic retinoid (Tigason) in low dosage orally and triamcinolone acetonide cream topically: a double-blind trial.
Herrmann, WA; Polano, MK; Tijssen, JG; van der Rhee, HJ; Waterman, AH, 1980
)
0.26
"Retinoids given in a high dosage are able to reduce or prevent the growth of experimental skin tumors in animals."( [Antitumor effect of retinoids (author's transl)].
Berger, H; Mahrle, G, 1982
)
0.26
" The most effective results were obtained with a schedule entailing initial treatment for a 2-week period with AR only, followed on the 15th day by the adjunction of classic PUVA therapy with progressive daily decrease of AR dosage (schedule C)."( Treatment of psoriasis by oral PUVA therapy combined with aromatic retinoid (Ro 10-9359; Tigason).
Berretti, B; Grupper, C, 1981
)
0.26
" Because of the side effects the dosage must be fixed individually."( Treatment of dyskeratosis follicularis Darier with the retinoic acid derivative Ro 10-9359 (Tigason).
Christiansen, JV; Holm, P; Møller, R; Reymann, F; Schmidt, H, 1981
)
0.26
"The effect of oral aromatic retinoid Ro 10-9359 in a high dosage (25 mg/kg/day) on guinea pig epidermis was investigated by light and electron microscopy."( Epidermal changes induced by oral excess of aromatic retinoid in guinea pigs.
Mahrle, G; Orfanos, CE; Tsambaos, D, 1980
)
0.26
" Information collected included demographic data, dosage of etretinate taken, response and side effects, clinical follow-up, and relapse."( Etretinate therapy for psoriasis and other keratinizing disorders: a 10-year retrospective study in Singapore.
Goh, CL; Shahidullah, M; Tham, SN, 1993
)
1.97
" A 53-year-old patient suffering from MF was treated with intramuscular administration of INF-alpha at a dosage of 9 x 10(6) IU daily; skin lesions poorly responded to the treatment."( Interferon-alpha (INF-alpha) and etretinate in the treatment of mycosis fungoides.
Harada, S; Kaneko, T; Matsuyama, T; Nakanishi, H; Torii, H, 1994
)
0.57
" Planned dosing was 10 mg 3 times daily for the first month, 25 mg twice daily for the second and third months, and 10 mg twice daily thereafter."( Etretinate augments interferon beta-1b effects on suppressor cells in multiple sclerosis.
Arnason, BG; Jensen, MW; Pliskin, N; Qu, ZX; White, D, 2001
)
1.75
" Whether pulse therapy or administration of retinoid restricted to the day of interferon beta dosing will also augment suppressor function, while being better tolerated, remains to be determined."( Etretinate augments interferon beta-1b effects on suppressor cells in multiple sclerosis.
Arnason, BG; Jensen, MW; Pliskin, N; Qu, ZX; White, D, 2001
)
1.75
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
keratolytic drugA drug that softens, separates, and causes desquamation of the cornified epithelium or horny layer of skin. Keratolytic drugs are used to expose mycelia of infecting fungi or to treat corns, warts, and certain other skin diseases.
[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 (3)

ClassDescription
retinoidOxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof.
enoate esterAn alpha,beta-unsaturated carboxylic ester of general formula R(1)R(2)C=CR(3)-C(=O)OR(4) (R(4) =/= H) in which the ester C=O function is conjugated to a C=C double bond at the alpha,beta position.
ethyl esterAny carboxylic ester resulting from the formal condensation of the carboxy group of a carboxylic acid with ethanol.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (43)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency19.85253.189029.884159.4836AID1224846; AID1224894
RAR-related orphan receptor gammaMus musculus (house mouse)Potency9.84550.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency16.93010.173734.304761.8120AID1346859
USP1 protein, partialHomo sapiens (human)Potency6.30960.031637.5844354.8130AID504865
SMAD family member 3Homo sapiens (human)Potency16.93010.173734.304761.8120AID1346859
TDP1 proteinHomo sapiens (human)Potency26.16790.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency31.61800.000714.592883.7951AID1259392
AR proteinHomo sapiens (human)Potency27.92880.000221.22318,912.5098AID743035; AID743036; AID743042; AID743054; AID743063
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency20.86630.000657.913322,387.1992AID1259377; AID1259378
progesterone receptorHomo sapiens (human)Potency23.71010.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency30.90080.01237.983543.2770AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency18.99590.000214.376460.0339AID720691
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency0.53080.003041.611522,387.1992AID1159553
retinoid X nuclear receptor alphaHomo sapiens (human)Potency18.99590.000817.505159.3239AID1159527
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency30.64300.001530.607315,848.9004AID1224848; AID1224849; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency31.66790.375827.485161.6524AID743217; AID743220
pregnane X nuclear receptorHomo sapiens (human)Potency21.13170.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency8.69720.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743075; AID743080; AID743091
GVesicular stomatitis virusPotency7.76190.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency24.54540.00108.379861.1304AID1645840
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency28.22410.001024.504861.6448AID743212; AID743215
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency19.43670.001019.414170.9645AID743094; AID743191
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency28.70170.023723.228263.5986AID743222; AID743223
aryl hydrocarbon receptorHomo sapiens (human)Potency21.97430.000723.06741,258.9301AID743085; AID743122
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency26.60320.001723.839378.1014AID743083
activating transcription factor 6Homo sapiens (human)Potency10.75310.143427.612159.8106AID1159516; AID1159519
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency6.740019.739145.978464.9432AID1159509
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency6.31910.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency28.59860.042027.378961.6448AID743210; AID743228
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency23.70830.000627.21521,122.0200AID743202
gemininHomo sapiens (human)Potency26.60860.004611.374133.4983AID624296
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency10.18150.005612.367736.1254AID624032
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency5.30800.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency7.76190.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency7.76190.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency21.13170.002319.595674.0614AID651631; AID720552
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency5.30800.001551.739315,848.9004AID1259244
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency7.76190.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency7.76190.01238.964839.8107AID1645842
[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)133.00000.20005.677410.0000AID1473741
Bile salt export pumpHomo sapiens (human)IC50 (µMol)133.00000.11007.190310.0000AID1473738
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (209)

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)
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)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (72)

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)
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)
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (45)

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)
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)
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (85)

Assay IDTitleYearJournalArticle
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
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.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical 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.
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.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
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.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID130178In vivo anti-papilloma activity against chemically induced skin papillomas in mice at dose of 20(mg/kg)/day1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
Fluorinated retinoic acids and their analogues. 2. Synthesis and biological activity of aromatic 4-fluoro analogues.
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.
AID1130653Toxicity in mouse assessed as hypervitaminosis dose compound treated ip daily monday through friday in first week and monday through thursday in second week measured after 1 day of last injection1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Fluorinated retinoic acids and their analogues. 1. Synthesis and Biological activity of (4-methoxy-2,3,6-trimethylphenyl)nonatetraenoic acid analogues.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
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.
AID334311Induction of morphological transformation of rat ASK cells into astrocytes after 1 hr by light microscopy
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1130654Antipapilloma activity against Hart Swiss albino mouse assessed as decrease in chemically-induced papillomas compound treated ip for 5 days/week for 2 weeks1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Fluorinated retinoic acids and their analogues. 1. Synthesis and Biological activity of (4-methoxy-2,3,6-trimethylphenyl)nonatetraenoic acid analogues.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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]
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]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID130177In vivo anti-papilloma activity against chemically induced skin papillomas in mice at dose of 10 mg/kg/day1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
Fluorinated retinoic acids and their analogues. 2. Synthesis and biological activity of aromatic 4-fluoro analogues.
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.
AID114326Antipapilloma activity was determined after intraperitoneal administration in mice1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Retinoids at the threshold: their biological significance and therapeutic potential.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID199192Inhibition of [3H]-retinoic acid binding to murine retinoic acid receptor RAR alpha; NA means not applicable2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Inhibition of papilloma formation by analogues of 7,8-dihydroretinoic acid.
AID1130658Antipapilloma activity against Hart Swiss albino mouse assessed as decrease in chemically-induced papillomas at 40 mg/kg, ip for 5 days/week for 2 weeks1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Fluorinated retinoic acids and their analogues. 1. Synthesis and Biological activity of (4-methoxy-2,3,6-trimethylphenyl)nonatetraenoic acid analogues.
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
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1130659Antipapilloma activity against Hart Swiss albino mouse assessed as decrease in chemically-induced papillomas at 20 mg/kg, ip for 5 days/week for 2 weeks1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Fluorinated retinoic acids and their analogues. 1. Synthesis and Biological activity of (4-methoxy-2,3,6-trimethylphenyl)nonatetraenoic acid analogues.
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]
AID44377Antitumor activity in CD-1 female mouse skin Papilloma assay2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Inhibition of papilloma formation by analogues of 7,8-dihydroretinoic acid.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID52209Inhibition of [3H]-retinoic acid binding to Cellular retinoic acid-binding protein (CRABP) from chick embryo skin; NA means not applicable2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Inhibition of papilloma formation by analogues of 7,8-dihydroretinoic acid.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
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]
AID109743Lowest daily intraperitoneal dose causing hypervitaminosis A symptoms was determined in a 2-week period in mice1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Retinoids at the threshold: their biological significance and therapeutic potential.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID130088Hypervitaminosis dose determined as a measure of toxicity1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
Fluorinated retinoic acids and their analogues. 2. Synthesis and biological activity of aromatic 4-fluoro analogues.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1130657Antipapilloma activity against Hart Swiss albino mouse assessed as decrease in chemically-induced papillomas at 80 mg/kg, ip for 5 days/week for 2 weeks1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Fluorinated retinoic acids and their analogues. 1. Synthesis and Biological activity of (4-methoxy-2,3,6-trimethylphenyl)nonatetraenoic acid analogues.
AID1130660Antipapilloma activity against Hart Swiss albino mouse assessed as decrease in chemically-induced papillomas at 10 mg/kg, ip for 5 days/week for 2 weeks1979Journal of medicinal chemistry, Sep, Volume: 22, Issue:9
Fluorinated retinoic acids and their analogues. 1. Synthesis and Biological activity of (4-methoxy-2,3,6-trimethylphenyl)nonatetraenoic acid analogues.
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.
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]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID130181In vivo anti-papilloma activity against chemically induced skin papillomas in mice at dose of 80(mg/kg)/day1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
Fluorinated retinoic acids and their analogues. 2. Synthesis and biological activity of aromatic 4-fluoro analogues.
AID235613Therapeutic index calculated as the ratio of hypervitaminosis A dose to the ED50 dose1982Journal of medicinal chemistry, Nov, Volume: 25, Issue:11
Retinoids at the threshold: their biological significance and therapeutic potential.
AID130179In vivo anti-papilloma activity against chemically induced skin papillomas in mice at dose of 40 mg/kg/day1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
Fluorinated retinoic acids and their analogues. 2. Synthesis and biological activity of aromatic 4-fluoro analogues.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (1,300)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990824 (63.38)18.7374
1990's351 (27.00)18.2507
2000's73 (5.62)29.6817
2010's41 (3.15)24.3611
2020's11 (0.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 47.58

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

MetricThis Compound (vs All)
Research Demand Index47.58 (24.57)
Research Supply Index7.32 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index78.11 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (47.58)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials133 (9.69%)5.53%
Reviews106 (7.72%)6.00%
Case Studies530 (38.60%)4.05%
Observational0 (0.00%)0.25%
Other604 (43.99%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]