Page last updated: 2024-12-10

idoxifene

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Description

idoxifene: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3034011
CHEMBL ID6318
CHEBI ID188870
SCHEMBL ID19216
MeSH IDM0193895

Synonyms (39)

Synonym
BIDD:ER0017
pyrrolidine, 1-(2-(4-(1-(4-iodophenyl)-2-phenyl-1-butenyl)phenoxy)ethyl-, (e)-
sb 223030
cb 7432
pyrrolidine, 1-(2-(4-(1-(4-iodophenyl)-2-phenyl-1-butenyl)phenoxy)ethyl)-, (e)-
1-(2-(p-((e)-beta-ethyl-alpha-(p-iodophenyl)styryl)phenoxy)ethyl)pyrrolidine
c28h30ino
(e)-1-(2-(4-(1-(4-iodophenyl)-2-phenyl-1-butenyl)phenoxy)ethyl)pyrrolidine
pyrrolidino-4-iodotamoxifen
iodoxifene
cb-7432
sb-223030
116057-75-1
D04496
idoxifene (usan/inn)
idoxifene
CHEMBL6318
1-[2-[4-[(e)-1-(4-iodophenyl)-2-phenylbut-1-enyl]phenoxy]ethyl]pyrrolidine
CHEBI:188870
AKOS016013971
unii-456uxe9867
456uxe9867 ,
idoxifene [usan:inn:ban]
idoxifene [mart.]
idoxifene [inn]
1-(2-(p-((e)-.beta.-ethyl-.alpha.-(p-iodophenyl)styryl)phenoxy)ethyl)pyrrolidine
idoxifene [mi]
idoxifene [usan]
SCHEMBL19216
DTXSID5043926
(e)-1-(2-(4-(1-(4-iodophenyl)-2-phenylbut-1-en-1-yl)phenoxy)ethyl)pyrrolidine
CS-7245
HY-U00178
Q5989541
(e)-1-(2-(4-(1-(4-iodophenyl)-2-phenylbut-1-enyl)phenoxy)ethyl)pyrrolidine
bdbm50219403
trans-1-(4-iodophenyl)-1-(4-(2'-pyrrolidinoethoxy)phenyl)-2-phenylbutene
MS-29693
A854422

Research Excerpts

Overview

Idoxifene is a novel selective oestrogen receptor modulator (SERM) It has greater antiestrogenic but lower estrogenic activity than tamoxifen. It is effective in patients with advanced breast cancer.

ExcerptReferenceRelevance
"Idoxifene is a novel selective estrogen receptor modulator (SERM) that, in preclinical models, has greater antiestrogenic but lower estrogenic activity than tamoxifen."( Idoxifene versus tamoxifen: a randomized comparison in postmenopausal patients with metastatic breast cancer.
Arpino, G; Bardou, VJ; Clark, GM; Doval Dinesh, C; Elledge, RM; Nair Krishnan, M, 2003
)
2.48
"Idoxifene is a novel selective oestrogen receptor modulator (SERM) which had greater binding affinity for the oestrogen receptor (ER) and reduced agonist activity compared with tamoxifen in preclinical studies. "( A cancer research (UK) randomized phase II study of idoxifene in patients with locally advanced/metastatic breast cancer resistant to tamoxifen.
Brampton, M; Canney, P; Coleman, RE; Coombes, RC; Dowsett, M; Earl, HM; Evans, TR; Grimshaw, R; Gumbrell, LA; Halbert, GW; Haviland, J; Haynes, BP; Howell, A; Jarman, M; Johnston, SR; Jones, A; Nutley, B; Powles, TJ; Rea, DW; Smith, IE; Soukop, M; Twelves, CJ, 2004
)
2.02
"Idoxifene is a selective estrogen receptor modulator similar to tamoxifen but is no longer in pharmaceutical development due to adverse genitourinary effects in the clinic. "( Histologic changes in ovary, uterus, vagina, and mammary gland of mature beagle dogs treated with the SERM idoxifene.
Portelli, ST; Rehm, S; Solleveld, HA; Wier, PJ, 2007
)
2
"Idoxifene is a more potent antioestrogen and is effective in patients with advanced breast cancer."( Idoxifene is equipotent to tamoxifen in inhibiting mammary carcinogenesis but forms lower levels of hepatic DNA adducts.
Bliss, J; Coombes, RC; Hewer, A; Jarman, M; Pace, P; Phillips, D, 1997
)
2.46
"Idoxifene is an agonist through the estrogen response element (ERE) and exhibits similar postreceptor effects to estrogen in bone-forming osteoblasts."( Idoxifene: a novel selective estrogen receptor modulator prevents bone loss and lowers cholesterol levels in ovariectomized rats and decreases uterine weight in intact rats.
Bradbeer, JN; Gowen, M; Hoffman, SJ; Nadeau, DP; Nuttall, ME; Rehm, S; Stroup, GB; Zhao, H, 1998
)
2.46
"Idoxifene is a novel selective estrogen receptor modulator that has shown beneficial effects on bone turnover and lipid metabolism in clinical studies. "( Sonographic assessment of the endometrium in osteopenic postmenopausal women treated with idoxifene.
Fleischer, AC; Jensen, C; Kravitz, B; MacDonald, B; Wheeler, JE; Yeh, IT, 1999
)
1.97
"Idoxifene is a novel selective estrogen (E2) receptor (ER) modulator that is currently in clinical development for the treatment of breast cancer. "( Idoxifene antagonizes estradiol-dependent MCF-7 breast cancer xenograft growth through sustained induction of apoptosis.
Boeddinghaus, IM; Dowsett, M; Grimshaw, R; Hardcastle, IR; Haynes, BP; Jarman, M; Johnston, SR; Riddler, S; Rowlands, M, 1999
)
3.19
"Idoxifene is a novel selective estrogen receptor modulator. "( Antiproliferative effects of idoxifene in a placebo-controlled trial in primary human breast cancer.
Dixon, JM; Dowsett, M; Harvey, E; Hills, M; Horgan, K; Salter, J, 2000
)
2.04
"Idoxifene acts as an oestrogen agonist in osteoblastic cells via an ER/ERE-mediated mechanism."( The selective oestrogen receptor modulators idoxifene and raloxifene have fundamentally different cell-specific oestrogen-response element (ERE)-dependent/independent mechanisms in vitro.
Fisher, PW; Gowen, M; Nuttall, ME; Suva, LJ, 2000
)
1.29
"Idoxifene (ID) is a tissue-selective estrogen receptor modulator (SERM). "( Selective estrogen receptor modulator idoxifene inhibits smooth muscle cell proliferation, enhances reendothelialization, and inhibits neointimal formation in vivo after vascular injury.
Chen, J; Gossett, KA; Gu, JL; Li, X; Louden, CS; Ma, XL; Narayanan, PK; Ohlstein, EH; Storer, B; Vickery-Clark, L; Willette, R; Yue, TL, 2000
)
2.02
"Idoxifene is a tissue-specific selective estrogen receptor modulator. "( Effects of idoxifene and estradiol on NF-kappaB activation in cultured rat hepatocytes undergoing oxidative stress.
Honda, H; Inoue, H; Ito, S; Itonaga, M; Lu, G; Nomura, M; Okamura, Y; Omoya, T; Shimizu, I; Zhou, Y, 2001
)
2.14

Effects

ExcerptReferenceRelevance
"Idoxifene has an antiproliferative effect in ER-positive but not ER-negative breast cancers, and no significant effect on apoptosis in the short-term."( Antiproliferative effects of idoxifene in a placebo-controlled trial in primary human breast cancer.
Dixon, JM; Dowsett, M; Harvey, E; Hills, M; Horgan, K; Salter, J, 2000
)
1.32
"Idoxifene has an antiproliferative effect in ER-positive but not ER-negative breast cancers, and no significant effect on apoptosis in the short-term."( Antiproliferative effects of idoxifene in a placebo-controlled trial in primary human breast cancer.
Dixon, JM; Dowsett, M; Harvey, E; Hills, M; Horgan, K; Salter, J, 2000
)
1.32

Actions

ExcerptReferenceRelevance
"Idoxifene could inhibit HSC activation."( Inhibitory effects of idoxifene on hepatic fibrosis in rats.
Chen, HS; Sha, BX; Shi, JH; Wang, X; Yin, DM; Zhou, YJ, 2005
)
1.36

Treatment

Treatment with idoxifene and estradiol inhibited IkappaB-alpha degradation and NF-kappaB activation through the attenuation of hepatocyte oxidative bursts and decreased extracellular levels of LDH and MDA. IdOxifene treatment had no effect on plasma estradio concentration but reduced SAO/R-induced hemoconcentration.

ExcerptReferenceRelevance
"Idoxifene treatment had no effect on plasma estradiol concentration but reduced SAO/R-induced hemoconcentration (+8.8 +/- 1.3 vs."( Endothelial protective and antishock effects of a selective estrogen receptor modulator in rats.
Chen, J; Christopher, TA; Gao, F; Lopez, BL; Ma, XL; Ohlstein, EH; Yue, T, 2001
)
1.03
"Treatment with idoxifene at either 1 or 2 mg/kg/day, or 17beta-estrogen at 1 mg/kg/day for 4 days significantly preserved endothelial function (P <.01 versus vehicle)."( Nitric oxide stimulatory and endothelial protective effects of idoxifene, a selective estrogen receptor modulator, in the splanchnic artery of the ovariectomized rat.
Chen, J; Christopher, TA; Disa, J; Gao, F; Gu, JL; Lopez, BL; Ma, XL; Ohlstein, EH; Yao, CL; Yue, TL, 2000
)
0.89
"Treatment with idoxifene and estradiol inhibited IkappaB-alpha degradation and NF-kappaB activation through the attenuation of hepatocyte oxidative bursts and decreased extracellular levels of LDH and MDA."( Effects of idoxifene and estradiol on NF-kappaB activation in cultured rat hepatocytes undergoing oxidative stress.
Honda, H; Inoue, H; Ito, S; Itonaga, M; Lu, G; Nomura, M; Okamura, Y; Omoya, T; Shimizu, I; Zhou, Y, 2001
)
1.04

Pharmacokinetics

ExcerptReferenceRelevance
" We conclude that 124I-labelled idoxifene combined with PET imaging would facilitate human in vivo pharmacokinetic studies of this new anticancer drug and provide an opportunity to investigate relationships between drug uptake and tumour response."( Biodistribution and kinetics of radiolabelled pyrrolidino-4-iodo-tamoxifen: prospects for pharmacokinetic studies using PET.
Carnochan, P; Eccles, S; Haynes, B; Ott, R; Potter, G; Trivedi, M; Young, H, 1994
)
0.57

Dosage Studied

Treatment with either idoxifene or estrogen (starting on day 10 of disease) of male and female Lewis rats also was effective in reducing paw inflammation in these animals. Cumulative dose-response vasorelaxation to idox ifene was 0.

ExcerptRelevanceReference
" Therapeutic treatment with either idoxifene or estrogen (starting on day 10 of disease) of male and female Lewis rats also was effective in reducing paw inflammation in these animals, although the effect was much less than that observed with the prophylactic dosing protocol."( Idoxifene, a novel selective estrogen receptor modulator, is effective in a rat model of adjuvant-induced arthritis.
Badger, AM; Blake, SM; Dodds, RA; Gowen, M; Griswold, DE; Hoffman, SJ; Rieman, DJ; Stroup, GB; Swift, BA, 1999
)
2.02
" Cumulative dose-response vasorelaxation to idoxifene (0."( Idoxifene causes endothelium-dependent, nitric oxide-mediated vasorelaxation in male rats.
Christopher, TA; Gao, E; Gao, F; Lopez, BL; Ma, XL; Ohlstein, EH; Stillwagon, JC; Yue, TL, 2002
)
2.02
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
stilbenoidAny olefinic compound characterised by a 1,2-diphenylethylene backbone.
[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 (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Estrogen receptorHomo sapiens (human)IC50 (µMol)0.00750.00000.723732.7000AID69240
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)IC50 (µMol)1.50000.40002.23759.9000AID158738
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)IC50 (µMol)1.50000.23002.510510.0000AID158738
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)IC50 (µMol)1.50000.40002.23759.9000AID158738
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)IC50 (µMol)1.50000.00002.14179.2000AID158738
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)IC50 (µMol)1.50000.23001.98149.0000AID158738
Estrogen receptor betaHomo sapiens (human)IC50 (µMol)0.00750.00010.529432.7000AID69240
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (56)

Processvia Protein(s)Taxonomy
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
antral ovarian follicle growthEstrogen receptorHomo sapiens (human)
epithelial cell developmentEstrogen receptorHomo sapiens (human)
chromatin remodelingEstrogen receptorHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
signal transductionEstrogen receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayEstrogen receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationEstrogen receptorHomo sapiens (human)
androgen metabolic processEstrogen receptorHomo sapiens (human)
male gonad developmentEstrogen receptorHomo sapiens (human)
negative regulation of gene expressionEstrogen receptorHomo sapiens (human)
positive regulation of phospholipase C activityEstrogen receptorHomo sapiens (human)
intracellular steroid hormone receptor signaling pathwayEstrogen receptorHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptorHomo sapiens (human)
response to estradiolEstrogen receptorHomo sapiens (human)
regulation of toll-like receptor signaling pathwayEstrogen receptorHomo sapiens (human)
negative regulation of smooth muscle cell apoptotic processEstrogen receptorHomo sapiens (human)
negative regulation of canonical NF-kappaB signal transductionEstrogen receptorHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
response to estrogenEstrogen receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
fibroblast proliferationEstrogen receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEstrogen receptorHomo sapiens (human)
stem cell differentiationEstrogen receptorHomo sapiens (human)
regulation of inflammatory responseEstrogen receptorHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
RNA polymerase II preinitiation complex assemblyEstrogen receptorHomo sapiens (human)
uterus developmentEstrogen receptorHomo sapiens (human)
vagina developmentEstrogen receptorHomo sapiens (human)
prostate epithelial cord elongationEstrogen receptorHomo sapiens (human)
prostate epithelial cord arborization involved in prostate glandular acinus morphogenesisEstrogen receptorHomo sapiens (human)
regulation of branching involved in prostate gland morphogenesisEstrogen receptorHomo sapiens (human)
mammary gland branching involved in pregnancyEstrogen receptorHomo sapiens (human)
mammary gland alveolus developmentEstrogen receptorHomo sapiens (human)
epithelial cell proliferation involved in mammary gland duct elongationEstrogen receptorHomo sapiens (human)
protein localization to chromatinEstrogen receptorHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptorHomo sapiens (human)
negative regulation of miRNA transcriptionEstrogen receptorHomo sapiens (human)
regulation of epithelial cell apoptotic processEstrogen receptorHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptorHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptorHomo sapiens (human)
regulation of smooth muscle cell apoptotic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
cGMP catabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
regulation of smooth muscle cell proliferationCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
response to amphetamineCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
locomotory behaviorCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
visual learningCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
monocyte differentiationCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cellular response to macrophage colony-stimulating factor stimulusCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
dopamine catabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
serotonin metabolic processCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cellular response to granulocyte macrophage colony-stimulating factor stimulusCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
cAMP-mediated signalingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
signal transductionEstrogen receptor betaHomo sapiens (human)
cell-cell signalingEstrogen receptor betaHomo sapiens (human)
negative regulation of cell growthEstrogen receptor betaHomo sapiens (human)
intracellular estrogen receptor signaling pathwayEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-templated transcriptionEstrogen receptor betaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityEstrogen receptor betaHomo sapiens (human)
cellular response to estradiol stimulusEstrogen receptor betaHomo sapiens (human)
regulation of transcription by RNA polymerase IIEstrogen receptor betaHomo sapiens (human)
cellular response to estrogen stimulusEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (34)

Processvia Protein(s)Taxonomy
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
TFIIB-class transcription factor bindingEstrogen receptorHomo sapiens (human)
transcription coregulator bindingEstrogen receptorHomo sapiens (human)
transcription corepressor bindingEstrogen receptorHomo sapiens (human)
transcription coactivator bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificEstrogen receptorHomo sapiens (human)
chromatin bindingEstrogen receptorHomo sapiens (human)
DNA-binding transcription factor activityEstrogen receptorHomo sapiens (human)
nuclear receptor activityEstrogen receptorHomo sapiens (human)
steroid bindingEstrogen receptorHomo sapiens (human)
protein bindingEstrogen receptorHomo sapiens (human)
calmodulin bindingEstrogen receptorHomo sapiens (human)
beta-catenin bindingEstrogen receptorHomo sapiens (human)
zinc ion bindingEstrogen receptorHomo sapiens (human)
TBP-class protein bindingEstrogen receptorHomo sapiens (human)
enzyme bindingEstrogen receptorHomo sapiens (human)
protein kinase bindingEstrogen receptorHomo sapiens (human)
nitric-oxide synthase regulator activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptorHomo sapiens (human)
nuclear estrogen receptor bindingEstrogen receptorHomo sapiens (human)
estrogen response element bindingEstrogen receptorHomo sapiens (human)
identical protein bindingEstrogen receptorHomo sapiens (human)
ATPase bindingEstrogen receptorHomo sapiens (human)
14-3-3 protein bindingEstrogen receptorHomo sapiens (human)
sequence-specific double-stranded DNA bindingEstrogen receptorHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
protein bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A Bos taurus (cattle)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
protein bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated dual specificity 3',5'-cyclic-GMP, 3',5'-cyclic-AMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
metal ion bindingCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
calmodulin-activated 3',5'-cyclic-GMP phosphodiesterase activityCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingEstrogen receptor betaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificEstrogen receptor betaHomo sapiens (human)
DNA bindingEstrogen receptor betaHomo sapiens (human)
nuclear steroid receptor activityEstrogen receptor betaHomo sapiens (human)
nuclear receptor activityEstrogen receptor betaHomo sapiens (human)
steroid bindingEstrogen receptor betaHomo sapiens (human)
protein bindingEstrogen receptor betaHomo sapiens (human)
zinc ion bindingEstrogen receptor betaHomo sapiens (human)
enzyme bindingEstrogen receptor betaHomo sapiens (human)
nuclear estrogen receptor activityEstrogen receptor betaHomo sapiens (human)
estrogen response element bindingEstrogen receptor betaHomo sapiens (human)
receptor antagonist activityEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
nucleusEstrogen receptorHomo sapiens (human)
nucleoplasmEstrogen receptorHomo sapiens (human)
transcription regulator complexEstrogen receptorHomo sapiens (human)
cytoplasmEstrogen receptorHomo sapiens (human)
Golgi apparatusEstrogen receptorHomo sapiens (human)
cytosolEstrogen receptorHomo sapiens (human)
plasma membraneEstrogen receptorHomo sapiens (human)
membraneEstrogen receptorHomo sapiens (human)
chromatinEstrogen receptorHomo sapiens (human)
euchromatinEstrogen receptorHomo sapiens (human)
protein-containing complexEstrogen receptorHomo sapiens (human)
nucleusEstrogen receptorHomo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1AHomo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BBos taurus (cattle)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1BHomo sapiens (human)
lysosomeCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
cytosolCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
neuronal cell bodyCalcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1CHomo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
nucleoplasmEstrogen receptor betaHomo sapiens (human)
mitochondrionEstrogen receptor betaHomo sapiens (human)
intracellular membrane-bounded organelleEstrogen receptor betaHomo sapiens (human)
chromatinEstrogen receptor betaHomo sapiens (human)
nucleusEstrogen receptor betaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID302179Growth inhibition of human HL60 cells after 4 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic aldehyde, cinnamyltrimethylsilane, and beta-chlorophenetole.
AID302175Antiproliferative activity against human HL60 cells assessed as cell viability at 1 ug/ml after 4 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic aldehyde, cinnamyltrimethylsilane, and beta-chlorophenetole.
AID225255Inhibition of calmodulin-dependent Phosphodiesterase1995Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2
Rationally designed analogues of tamoxifen with improved calmodulin antagonism.
AID67812Percent stimulation of alkaline phosphatase activity in Ishikawa human endometrial adenocarcinoma cells relative to moxestrol2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.
AID103394Growth inhibitory activity against MCF-7 human breast tumor cell line at a concentration of 10e-8 M in vitro.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
AID69520Receptor binding affinity(RBA) for rat uterine cytosolic estrogen receptor relative to estradiol1995Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2
Rationally designed analogues of tamoxifen with improved calmodulin antagonism.
AID104076In vitro cytotoxicity against hormone-responsive MCF-7 cell line.1995Journal of medicinal chemistry, Jan-20, Volume: 38, Issue:2
Rationally designed analogues of tamoxifen with improved calmodulin antagonism.
AID69240Displacement of [3H]17-beta-estradiol from Estrogen receptor of rabbit uterine tissue2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.
AID302176Antiproliferative activity against human HL60 cells assessed as cell viability at 5 ug/ml after 4 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic aldehyde, cinnamyltrimethylsilane, and beta-chlorophenetole.
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.
AID302177Antiproliferative activity against human HL60 cells assessed as cell viability at 10 ug/ml after 4 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic aldehyde, cinnamyltrimethylsilane, and beta-chlorophenetole.
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.
AID1646797Chaperone activity at GCase L444P GBA gene mutant in human fibroblasts derived from Gaucher patient assessed as increase in GPN-induced reduction of calcium release using Fluo-8AM based fluorescence assay2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
AID158738Inhibitory activity against calmodulin-dependent Phosphodiesterase was reported.1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Homologs of idoxifene: variation of estrogen receptor binding and calmodulin antagonism with chain length.
AID1646798Chaperone activity at GCase L444P GBA gene mutant in human fibroblasts derived from Gaucher patient assessed as increase in GPN-induced reduction of calcium release using Fluo-8AM based fluorescence assay relative to control2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Novel compounds that reverse the disease phenotype in Type 2 Gaucher disease patient-derived cells.
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.
AID103392Growth inhibitory activity against MCF-7 human breast tumor cell line at a concentration of 10e-6 M in vitro.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
AID46330Antagonistic potency against calmodulin-dependent cyclic AMP phosphodiesterase relative to Idoxifene1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Homologs of idoxifene: variation of estrogen receptor binding and calmodulin antagonism with chain length.
AID103393Growth inhibitory activity against MCF-7 human breast tumor cell line at a concentration of 10e-7 M in vitro.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
AID302174Antiproliferative activity against human HL60 cells assessed as cell viability after 4 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic aldehyde, cinnamyltrimethylsilane, and beta-chlorophenetole.
AID67813Stimulation of alkaline phosphatase activity in Ishikawa human endometrial adenocarcinoma cells2002Bioorganic & medicinal chemistry letters, Jan-07, Volume: 12, Issue:1
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.
AID69373Binding affinity towards rat uterine cytosolic Estrogen receptor was determined relative to estradiol1996Journal of medicinal chemistry, Feb-16, Volume: 39, Issue:4
Homologs of idoxifene: variation of estrogen receptor binding and calmodulin antagonism with chain length.
AID302178Antiproliferative activity against human HL60 cells assessed as cell viability at 20 ug/ml after 4 hrs by MTT assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
An expeditious synthesis of tamoxifen, a representative SERM (selective estrogen receptor modulator), via the three-component coupling reaction among aromatic aldehyde, cinnamyltrimethylsilane, and beta-chlorophenetole.
AID71122Relative binding affinity against estrogen receptors in calf uterine cytosol.1989Journal of medicinal chemistry, Dec, Volume: 32, Issue:12
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (59)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (1.69)18.7374
1990's23 (38.98)18.2507
2000's32 (54.24)29.6817
2010's2 (3.39)24.3611
2020's1 (1.69)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.32

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index21.32 (24.57)
Research Supply Index4.25 (2.92)
Research Growth Index6.27 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (21.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (13.11%)5.53%
Reviews6 (9.84%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other47 (77.05%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]