Page last updated: 2024-11-04

naftopidil

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Naftopidil is a selective inhibitor of Rho-associated protein kinase (ROCK) that has shown potential therapeutic applications in various conditions. It was initially synthesized in the 1980s and has since been studied extensively for its diverse biological activities. Naftopidil inhibits ROCK by binding to its catalytic domain, leading to the downstream inhibition of Rho signaling pathways. This inhibition has been shown to be beneficial in a wide range of conditions, including hypertension, atherosclerosis, fibrosis, and cancer. Its anti-proliferative and anti-inflammatory effects have made it a promising candidate for the treatment of several cancers, particularly those associated with abnormal Rho signaling. Additionally, naftopidil has been investigated for its potential therapeutic role in neurological disorders such as stroke and Alzheimer's disease, as it has demonstrated neuroprotective effects by inhibiting neuronal apoptosis and promoting angiogenesis. The significant therapeutic potential of naftopidil has fueled ongoing research to further elucidate its mechanisms of action and explore its applications in various clinical settings.'

Cross-References

ID SourceID
PubMed CID4418
CHEMBL ID142635
CHEBI ID31891
SCHEMBL ID113215
MeSH IDM0177287

Synonyms (115)

Synonym
naftopidil hydrochloride hydrate
HMS3393B09
AB00489961-18
AB00489961-19
BRD-A01787639-300-03-7
bm-15275
naftopidil
flivas
avishot
kt-611
LOPAC0_000941
BPBIO1_001111
BSPBIO_001009
PRESTWICK2_000975
PRESTWICK3_000975
4-(2-methoxyphenyl)-alpha-((1-naphthalenyloxy)methyl)-1-pioerazineethanol
brn 0629965
naftopidilum [latin]
(+-)-1-(4-(2-methoxyphenyl)piperazinyl)-3-(1-naphthyloxy)propan-2-ol
(rs)-1-(4-(2-methoxyphenyl)-1-piperazinyl)-3-(1-naphthyloxy)-2-propanol
1-pioerazineethanol, 4-(2-methoxyphenyl)-alpha-((1-naphthalenyloxy)methyl)-
(+-)-4-(o-methoxyphenyl)-alpha-((1-naphthyloxy)methyl)-1-piperazineethanol
naftopidil [inn]
AB00514643
MLS001424117
MLS000759459
smr000466346
naftopidil (jp17/inn)
flivas (tn)
57149-07-2
D01674
NCGC00024672-04
PRESTWICK1_000975
PRESTWICK0_000975
SPBIO_002920
NCGC00024672-03
HMS2051B09
HMS2089G07
1-[4-(2-methoxyphenyl)piperazinyl]-3-(1-naphthyloxy)propan-2-ol
N0832
NCGC00015718-09
nsc-759293
CHEMBL142635 ,
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol
AKOS002279617
NCGC00015718-06
1-[4-(2-methoxyphenyl)-1-piperazinyl]-3-(1-naphthalenyloxy)-2-propanol
A831328
unii-r9phw59sfn
nsc 759293
r9phw59sfn ,
naftopidilum
pharmakon1600-01506024
nsc759293
dtxcid3025176
tox21_110205
dtxsid5045176 ,
cas-57149-07-2
CCG-205022
CCG-100935
NCGC00015718-10
NCGC00015718-08
NCGC00015718-05
NCGC00015718-04
BCP9000976
FT-0630696
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(naphthalen-1-yloxy)propan-2-ol
STL372645
S2126 ,
AKOS016328058
naftopidil [mart.]
naftopidil [jan]
naftopidil [who-dd]
naftopidil [mi]
(+/-)-4-(o-methoxyphenyl)-.alpha.-((1-naphthyloxy)methyl)-1-piperazineethanol
HY-B0391
SCHEMBL113215
NC00185
4-(2-methoxyphenyl)-alpha-[(1-naphthalenyloxy)methyl]-1-piperazineethanol
BBL028454
NCGC00015718-12
tox21_110205_1
FE-0209
REGID_FOR_CID_4418
mfcd00242741
1-[4-(2-methoxyphenyl)piperazino]-3-(1-naphthoxy)propan-2-ol;hydrochloride
cid_4418
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxypropan-2-ol;hydrochloride
bdbm50773
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-naphthalen-1-yloxy-propan-2-ol;hydrochloride
1-[4-(2-methoxyphenyl)-1-piperazinyl]-3-(1-naphthalenyloxy)-2-propanol;hydrochloride
cid_6603044
1-(4-(2-methoxyphenyl)piperazin-1-yl)-3-(naphthalen-1-yloxy)propan-2-ol
AB00489961_21
AB00489961_20
HMS3655H21
CHEBI:31891
SBI-0050915.P002
SW196570-4
DB12092
1-(4-(2-methoxyphenyl)piperazin-1-yl)-
3-(naphthalen-1-yloxy)propan-2-ol
BCP21786
bm-15275; kt-611; bm 15275; kt 611; bm15275; kt611
Z31369389
naftopidil (flivas)
naftopidil,(s)
Q6958243
BRD-A01787639-300-04-5
SB19321
SDCCGSBI-0050915.P003
NCGC00015718-25
HMS3884P07
BN164631
EN300-6492981

Research Excerpts

Overview

Naftopidil is a tubulin-binding drug with fewer adverse events, implying the usefulness of this drug in clinical applications when combined with DTX. It has been used to treat lower urinary tract symptoms of benign prostatic hyperplasia.

ExcerptReferenceRelevance
"Naftopidil is a tubulin-binding drug with fewer adverse events, implying the usefulness of this drug in clinical applications when combined with DTX."( Additive naftopidil treatment synergizes docetaxel-induced apoptosis in human prostate cancer cells.
Arima, K; Ishii, K; Kajiwara, S; Kanda, H; Kato, M; Matsuoka, I; Miki, M; Sasaki, T; Shiraishi, T; Sugimura, Y, 2018
)
1.62
"Naftopidil is an alpha-blocker (AB) that has a high affinity for the A1d receptor that may have advantages in treating LUTS in this setting."( Naftopidil for the treatment of lower urinary tract symptoms compatible with benign prostatic hyperplasia.
Dahm, P; Gandhi, S; Hwang, EC; Imamura, M; Jung, JH; Kim, MH; Pang, R, 2018
)
2.64
"Naftopidil (NAF) is a chiral compound with two enantiomers (R(+)-NAF and S(-)-NAF) and is used as a racemic mixture in clinical practice. "( Identification of human cytochrome P450 isozymes involved in the metabolism of naftopidil enantiomers in vitro.
Fu, X; Huang, J; Liu, X; Yuan, M; Zhang, X; Zhu, L, 2014
)
2.07
"Naftopidil is a subtype-selective α"( Combination treatment with naftopidil increases the efficacy of radiotherapy in PC-3 human prostate cancer cells.
Arima, K; Ishii, K; Iwamoto, Y; Kajiwara, S; Kanda, H; Kato, M; Miki, M; Shiraishi, T; Sugimura, Y, 2017
)
1.47
"Naftopidil is a specific alpha1D-adrenergic receptor antagonist. "( Efficacy of selective alpha1D-blocker naftopidil as medical expulsive therapy for distal ureteral stones.
Ge, W; He, L; Lv, J; Sun, X, 2009
)
2.07
"Naftopidil is an α(1D) and α(1A) subtype-selective α(1)-adrenoceptor antagonist that has been used to treat lower urinary tract symptoms of benign prostatic hyperplasia. "( Naftopidil inhibits 5-hydroxytryptamine-induced bladder contraction in rats.
Ikegaki, I; Kasahara, K; Kuriyama, H; Sakai, T; Tomita, K, 2013
)
3.28

Effects

Naftopidil has novel effects in patients with BPH whose main complaints are storage and voiding symptoms. It has similar sexual adverse events compared to tamsulosin but has fewer compared to silodosin.

ExcerptReferenceRelevance
"Naftopidil has similar sexual adverse events compared to tamsulosin but has fewer compared to silodosin."( Naftopidil for the treatment of lower urinary tract symptoms compatible with benign prostatic hyperplasia.
Dahm, P; Gandhi, S; Hwang, EC; Imamura, M; Jung, JH; Kim, MH; Pang, R, 2018
)
2.64
"Naftopidil has novel effects in patients with BPH whose main complaints are storage and voiding symptoms, especially that of nocturia of >or=3 times, as well as in patients with a low compliance bladder and detrusor overactivity, who did not respond to tamsulosin."( Effect of naftopidil on nocturia after failure of tamsulosin.
Oh-oka, H, 2008
)
2.19
"Naftopidil appears to have been effective in this short-term treatment of BPH."( Single-blind, randomized controlled study of the clinical and urodynamic effects of an alpha-blocker (naftopidil) and phytotherapy (eviprostat) in the treatment of benign prostatic hyperplasia.
Kamai, T; Sakakibara, R; Tsujii, T; Uchiyama, T; Yamanishi, T; Yasuda, K; Yoshida, K, 2004
)
1.98

Actions

ExcerptReferenceRelevance
"Naftopidil may inhibit the micturition reflex via 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT3 receptors in the spinal cord. "( Action of naftopidil on spinal serotonergic neurotransmission for inhibition of the micturition reflex in rats.
Ashitomi, K; Hattori, T; Kadekawa, K; Nishijima, S; Sugaya, K; Ueda, T; Yamamoto, H, 2017
)
2.3

Treatment

Naftopidil treatment decreased mean systolic BP by 18.7 mm Hg for the HT 50 mg group. Treatment reduced the upregulation of mRNA levels of ischemia and fibrosis markers at the early phase of SCI, and ameliorated the decrease of bladder compliance.

ExcerptReferenceRelevance
"Naftopidil treatment decreased mean systolic BP by 18.7 mm Hg for the HT 50 mg group (p<0.001) and by 18.3 mm Hg for the HT 75 mg group (p<0.001) and mean diastolic BP by 17.5 mm Hg for the HT 50 mg group (p<0.001) and by 14.7 mm Hg for the HT 75 mg group (p=0.022). "( Clinical Efficacy and Safety of Naftopidil Treatment for Patients with Benign Prostatic Hyperplasia and Hypertension: A Prospective, Open-Label Study.
Chung, MS; Lee, SH; Yoon, BI, 2017
)
2.18
"Naftopidil treatment reduced the upregulation of mRNA levels of ischemia and fibrosis markers at the early phase of SCI, and ameliorated the decrease of bladder compliance and voiding efficiency, and the increase of urethral pressure and collagen concentration in the bladder wall at the late phase of SCI. "( Effects of an alpha1A/D-adrenoceptor antagonist, naftopidil, and a phosphodiesterase type 5 inhibitor, tadalafil, on urinary bladder remodeling in rats with spinal cord injury.
Kadekawa, K; Kawamorita, N; Majima, T; Mori, K; Okada, H; Sugaya, K; Tyagi, P; Yoshimura, N; Yoshizawa, T, 2017
)
2.15
"In naftopidil-treated PrSC, total interleukin-6 protein was significantly reduced with increased suppression of cell proliferation."( Naftopidil, a selective {alpha}1-adrenoceptor antagonist, suppresses human prostate tumor growth by altering interactions between tumor cells and stroma.
Arima, K; Hori, Y; Ishii, K; Iwamoto, Y; Kanda, H; Kise, H; Nishikawa, K; Soga, N; Sugimura, Y, 2011
)
2.33
"Treatment with naftopidil and celecoxib appears to be beneficial in distal ureter stone clearance, shortened the expulsion time, and could be used reliably and successfully to reduce the frequency and intensity of the pain episodes particularly."( Comparative evaluation of efficacy of use of naftopidil and/or celecoxib for medical treatment of distal ureteral stones.
Lv, JL; Tang, QL, 2014
)
1
"Treatment with naftopidil and tolterodine appears to be beneficial in intramural ureteral stones clearance, particularly in the intramural ureter with symptoms of vesical irritability."( Naftopidil and tolterodine in the medical expulsive therapy for intramural ureteral stones: a prospective randomized study.
De Liu, F; Hui, JH; Lu, JL; Tang, QL, 2012
)
2.16

Toxicity

The alphalA/D blocker naftopidil is both effective and safe in the treatment of BPH patients with OAB symptoms. A little lower adverse effect rate was observed with naftipidil compared with tamsulosin.

ExcerptReferenceRelevance
" Data on all randomized patients were included in the safety analyses for adverse effects and changes in blood pressure."( Comparison of tamsulosin and naftopidil for efficacy and safety in the treatment of benign prostatic hyperplasia: a randomized controlled trial.
Gotoh, M; Kamihira, O; Kinukawa, T; Ohshima, S; Ono, Y; Origasa, H, 2005
)
0.62
" The adverse effects were comparable, with no significant differences in systolic and diastolic blood pressure after treatment in both groups."( Comparison of tamsulosin and naftopidil for efficacy and safety in the treatment of benign prostatic hyperplasia: a randomized controlled trial.
Gotoh, M; Kamihira, O; Kinukawa, T; Ohshima, S; Ono, Y; Origasa, H, 2005
)
0.62
"This study suggests that naftopidil is as effective and safe as tamsulosin."( Comparison of tamsulosin and naftopidil for efficacy and safety in the treatment of benign prostatic hyperplasia: a randomized controlled trial.
Gotoh, M; Kamihira, O; Kinukawa, T; Ohshima, S; Ono, Y; Origasa, H, 2005
)
0.92
"35%) experienced the adverse event of dizziness."( [Effectiveness and safety of naftopidil for benign prostatic hyperplasia patients with overactive bladder symptoms].
Gao, JP; Ge, JP; Gong, J; Ma, HQ; Shang, XJ; Wang, D; Wei, W; Xu, S; Zhang, ZY, 2008
)
0.64
"The alphalA/D blocker naftopidil is both effective and safe in the treatment of BPH patients with OAB symptoms."( [Effectiveness and safety of naftopidil for benign prostatic hyperplasia patients with overactive bladder symptoms].
Gao, JP; Ge, JP; Gong, J; Ma, HQ; Shang, XJ; Wang, D; Wei, W; Xu, S; Zhang, ZY, 2008
)
0.95
" α(1) Blockers generally lead to more adverse effects compared with placebo, and those caused by terazosin were more frequent than others."( The efficacy and safety of alpha-1 blockers for benign prostatic hyperplasia: an overview of 15 systematic reviews.
Liu, Y; Mao, C; Qin, X; Yang, K; Yang, Z; Yuan, J, 2013
)
0.39
" The adverse effects caused by α(1) blockers are generally mild and well-tolerated."( The efficacy and safety of alpha-1 blockers for benign prostatic hyperplasia: an overview of 15 systematic reviews.
Liu, Y; Mao, C; Qin, X; Yang, K; Yang, Z; Yuan, J, 2013
)
0.39
" Adverse events (AEs), obstructive/irritative subscores, quality of life (QoL) score, maximum urinary flow rate (Qmax), and benefit, satisfaction with treatment, and willingness to continue treatment (BSW) questionnaire were also analyzed."( Clinical Efficacy and Safety of Naftopidil Treatment for Patients with Benign Prostatic Hyperplasia and Hypertension: A Prospective, Open-Label Study.
Chung, MS; Lee, SH; Yoon, BI, 2017
)
0.74

Pharmacokinetics

ExcerptReferenceRelevance
"99) h, Tmax was (1."( [Pharmacokinetics of high-dosage naftopidil capsules in dogs].
Ding, JS; Jiang, XH, 2001
)
0.59
" These data reveal the stereoselective pharmacokinetic profiles of the two enantiomers in rats."( Enantiospecific determination of naftopidil by RRLC-MS/MS reveals stereoselective pharmacokinetics and tissue distributions in rats.
Guo, J; Huang, B; Huang, J; Liu, X; Luo, C; Rong, Y; Yuan, M; Zhang, X; Zhu, L, 2015
)
0.7

Bioavailability

Naftopidil bioadhesive sustained-release capsule. Study their pharmacokinetics and relative bioavailability in the dog.

ExcerptReferenceRelevance
" The absolute bioavailability of the parent compound amounted to 9% in rats and indicates a high first pass effect to in part pharmacodynamically effective metabolites, as was shown in a previous paper."( Pharmacokinetic fate of the novel antihypertensive drug naftopidil.
Borbe, HO; Locher, M; Niebch, G; Peter, G, 1991
)
0.53
" Mean values for the absolute bioavailability in patients with hepatic dysfunction were significantly higher (mean 75%, median 53%, range 13."( Pharmacokinetics of naftopidil, a novel anti-hypertensive drug, in patients with hepatic dysfunction.
Abrams, SM; Alstead, EM; Farthing, MJ; Haug, G; Hermann, R; Johnston, A; Molz, KH; Niebch, G; Ruus, P; Turner, P, 1994
)
0.61
"To prepare naftopidil bioadhesive sustained-release capsule and study their pharmacokinetics and relative bioavailability in the dog."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
0.99
" The naftopidil concentrations in plasma were determined by a newly developed HPLC method and the pharmacokinetic parameters as well as the relative bioavailability were measured."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
1.11
" The bioadhesive formulations and the non-bioadhesive one were not bioequivalent, the relative bioavailability of the two bioadhesive sustained-release capsules were respectively 150% +/- 14% and 154% +/- 23% when compared with the non-bioadhesive capsule."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
0.6
"It is much improving bioavailability of naftopidil by using bioadhesion."( [Improving bioavailability of naftopidil by using bioadhesion in dogs].
Ding, JS; Jiang, XH; Yuan, M, 2001
)
0.87
" The absorbed fraction(F) and in vivo absorption rate (A) of the NAF sustained-release tablet in the dog at different time were calculated by W-N method and deconvolution method, respectively."( [The study of the in vivo-in vitro correlation of the naftopidil sustained-release tablet in dog].
Ding, J; Jia, Y; Jiang, X, 2006
)
0.58
" This study aimed to investigate the pharmacokinetics, bioavailability and tissue distributions of NAF enantiomers in rats after intragastric administration of the individual enantiomers."( Enantiospecific determination of naftopidil by RRLC-MS/MS reveals stereoselective pharmacokinetics and tissue distributions in rats.
Guo, J; Huang, B; Huang, J; Liu, X; Luo, C; Rong, Y; Yuan, M; Zhang, X; Zhu, L, 2015
)
0.7
" It was previously shown that bioavailability of S(-)-NAF (14."( Poor and enantioselective bioavailability of naftopidil enantiomers is due to extensive and stereoselective metabolism in rat liver.
Cai, Y; Fu, X; Guo, J; Guo, Y; Huang, B; Huang, J; Li, A; Liu, X; Rong, Y; Wu, B; Xiao, Q; Yuan, M; Zhang, X; Zhu, L, 2017
)
0.71
" We hypothesized that the dissolution rate and oral bioavailability of NAF would increase through hydrogen bonding between NAF and weak acids/hydrophilic polymers."( Naftopidil-fumaric acid interaction in a solid dispersion system: Improving the dissolution rate and oral absorption of naftopidil in rats.
Byeon, JC; Choi, JS; Park, JS, 2019
)
1.96
"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

Naftopidil shifted the dose-response curve of methoxamine at equipotent hypotensive doses to the same extent to the right as does prazosin. Both drugs barely affected the response to norepinephrine.

ExcerptRelevanceReference
" In pithed rats, naftopidil shifted the dose-response curve of methoxamine at equipotent hypotensive doses to the same extent to the right as does prazosin, but both drugs barely affected (in contrast to phentolamine) the response to norepinephrine."( Naftopidil, a new adrenoceptor blocking agent with Ca(2+)-antagonistic properties: interaction with adrenoceptors.
Borbe, HO; Freud, P; Jakob, B; Müller-Beckmann, B; Sponer, G, 1992
)
2.07
" KT-611 at a dosage of once or twice a day was evaluated for its effects on 49 patients with benign prostatic hypertrophy."( [Effect of KT-611 (Naftopidil) on the contraction of human prostatic tissue and its use in benign prostatic obstruction].
Fukaya, Y; Itou, K; Kameoka, H; Kuma, Y; Kumakawa, K; Shiraiwa, Y; Yamaguchi, O; Yamanaka, N; Yokota, T; Yokoyama, J, 1991
)
0.61
" The dose-response curves for collagen and ADP were unaffected by either drug."( The potentiation of adrenaline-induced in vitro platelet aggregation by ADP, collagen and serotonin and its inhibition by naftopidil and doxazosin in normal human subjects.
Alarayyed, NA; Graham, BR; Prichard, BN; Smith, CC, 1995
)
0.5
"Although the anticholinergic dosage was low, the present results suggest that naftopidil monotherapy was as useful as combination therapy of naftopidil and an anticholinergic agent."( Naftopidil monotherapy vs naftopidil and an anticholinergic agent combined therapy for storage symptoms associated with benign prostatic hyperplasia: A prospective randomized controlled study.
Hanazawa, K; Honda, S; Kawachi, Y; Koizumi, K; Maruyama, O; Noto, K; Saitoh, T; Sugimura, S; Sugiyama, Y; Yamashita, R, 2006
)
2
"We examined the tolerability of dosage methods of naftopidil in the treatment of male lower urinary tract symptoms associated with benign prostatic hyperplasia (BPH/male LUTS)."( A prospective, randomized, controlled, multicenter study of naftopidil for treatment of male lower urinary tract symptoms associated with benign prostatic hyperplasia: 75 mg once daily in the evening compared to 25 mg thrice daily.
Kazama, T; Kimura, H; Nozaki, T; Okumura, A; Tsuritani, S, 2010
)
0.86
"To examine the difference in improvement of lower urinary tract symptoms between morning and evening dosing of α1 -blocker naftopidil."( Efficacy of naftopidil for nocturia in male patients with lower urinary tract symptoms: comparison of morning and evening dosing.
Adachi, T; Kuratsukuri, K; Nakamura, T; Nakatani, T; Ohmachi, T; Tamada, S; Tanaka, T; Yamaguchi, T; Yamamoto, S; Yoshimura, R, 2015
)
1
"A total of 177 male patients with nocturia were included in the present study and randomized to morning or evening dosing of naftopidil."( Efficacy of naftopidil for nocturia in male patients with lower urinary tract symptoms: comparison of morning and evening dosing.
Adachi, T; Kuratsukuri, K; Nakamura, T; Nakatani, T; Ohmachi, T; Tamada, S; Tanaka, T; Yamaguchi, T; Yamamoto, S; Yoshimura, R, 2015
)
1
" In a multivariate model, both the dosing time of naftopidil and the initial nocturia quality of life index were significantly associated with change in nocturia quality of life index."( Efficacy of naftopidil for nocturia in male patients with lower urinary tract symptoms: comparison of morning and evening dosing.
Adachi, T; Kuratsukuri, K; Nakamura, T; Nakatani, T; Ohmachi, T; Tamada, S; Tanaka, T; Yamaguchi, T; Yamamoto, S; Yoshimura, R, 2015
)
1.05
"Evening dosing of naftopidil seems to be more effective in treating nocturia in male patients with lower urinary tract symptoms."( Efficacy of naftopidil for nocturia in male patients with lower urinary tract symptoms: comparison of morning and evening dosing.
Adachi, T; Kuratsukuri, K; Nakamura, T; Nakatani, T; Ohmachi, T; Tamada, S; Tanaka, T; Yamaguchi, T; Yamamoto, S; Yoshimura, R, 2015
)
1.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
piperazines
[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 (57)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency31.62280.004023.8416100.0000AID485290
thioredoxin reductaseRattus norvegicus (Norway rat)Potency29.93490.100020.879379.4328AID588453
RAR-related orphan receptor gammaMus musculus (house mouse)Potency23.27640.006038.004119,952.5996AID1159521; AID1159523
ATAD5 protein, partialHomo sapiens (human)Potency19.46830.004110.890331.5287AID493106; AID493107
USP1 protein, partialHomo sapiens (human)Potency59.66490.031637.5844354.8130AID504865
GLS proteinHomo sapiens (human)Potency7.94330.35487.935539.8107AID624146
TDP1 proteinHomo sapiens (human)Potency22.69190.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency23.94420.000714.592883.7951AID1259369; AID1259392
Microtubule-associated protein tauHomo sapiens (human)Potency24.06820.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency28.74660.000221.22318,912.5098AID1259243; AID1259247
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency23.71010.000657.913322,387.1992AID1259378
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency5.23350.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency33.49150.000417.946075.1148AID1346795
regulator of G-protein signaling 4Homo sapiens (human)Potency0.23780.531815.435837.6858AID504845
EWS/FLI fusion proteinHomo sapiens (human)Potency14.87680.001310.157742.8575AID1259252; AID1259253; AID1259256
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency26.60320.003041.611522,387.1992AID1159552; AID1159553; AID1159555
retinoid X nuclear receptor alphaHomo sapiens (human)Potency21.94530.000817.505159.3239AID1159527; AID1159531
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency23.05350.001530.607315,848.9004AID1224841; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency29.84700.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency13.33320.005428.02631,258.9301AID1346982
estrogen nuclear receptor alphaHomo sapiens (human)Potency6.16920.000229.305416,493.5996AID1259248; AID743069
GVesicular stomatitis virusPotency1.73770.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency0.43650.00108.379861.1304AID1645840
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency50.11870.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency6.79470.035520.977089.1251AID504332
aryl hydrocarbon receptorHomo sapiens (human)Potency28.22630.000723.06741,258.9301AID743085; AID743122
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency23.91450.057821.109761.2679AID1159526
D(1A) dopamine receptorHomo sapiens (human)Potency3.66240.02245.944922.3872AID488982
chromobox protein homolog 1Homo sapiens (human)Potency39.81070.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency3.16230.01789.637444.6684AID588834
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency31.03990.000323.4451159.6830AID743065; AID743067
heat shock protein beta-1Homo sapiens (human)Potency21.13000.042027.378961.6448AID743210
mitogen-activated protein kinase 1Homo sapiens (human)Potency8.91250.039816.784239.8107AID1454
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency24.22780.00378.618923.2809AID2660; AID2667; AID2668
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency9.43840.000627.21521,122.0200AID743202
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency36.12540.005612.367736.1254AID624032
M-phase phosphoprotein 8Homo sapiens (human)Potency37.68580.177824.735279.4328AID488949
lamin isoform A-delta10Homo sapiens (human)Potency0.89130.891312.067628.1838AID1487
Interferon betaHomo sapiens (human)Potency1.73770.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.73770.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency29.84930.002319.595674.0614AID651631
D(1A) dopamine receptorSus scrofa (pig)Potency23.28090.00378.108123.2809AID2667
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency3.54810.009610.525035.4813AID1479145
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency2.51191.000010.475628.1838AID1457
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.73770.01238.964839.8107AID1645842
Ataxin-2Homo sapiens (human)Potency31.62280.011912.222168.7989AID588378
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.73770.01238.964839.8107AID1645842
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)10.00000.11007.190310.0000AID1449628
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki1.00000.00000.667310.0000AID40413
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.05520.00020.75688.8970AID1266203; AID1391654
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.00120.00000.360910.0000AID1374287
Alpha-1A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.55500.00020.56145.4000AID1266201; AID1391652
Alpha-1A adrenergic receptorHomo sapiens (human)Ki0.00370.00000.272610.0000AID1374285
Alpha-1B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.63400.00020.65268.3300AID1266202; AID1391653
Alpha-1B adrenergic receptorHomo sapiens (human)Ki0.02000.00000.471310.0000AID1374286
Beta-2 adrenergic receptorCanis lupus familiaris (dog)Ki1.00000.14001.61333.7000AID41479
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
voltage-dependent T-type calcium channel subunit alpha-1H isoform aHomo sapiens (human)EC50 (µMol)3.72000.43404.827513.3000AID489005
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)Kd0.17780.00020.52667.5858AID1374280
Alpha-1D adrenergic receptorRattus norvegicus (Norway rat)Kd0.07750.00020.89627.5858AID1374281; AID1544676
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)Kd0.03310.00020.51397.5858AID1374279
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (237)

Processvia Protein(s)Taxonomy
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)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressureAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrineAlpha-1A adrenergic receptorHomo sapiens (human)
apoptotic processAlpha-1A adrenergic receptorHomo sapiens (human)
smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
activation of phospholipase C activityAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1A adrenergic receptorHomo sapiens (human)
adult heart developmentAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of cell population proliferationAlpha-1A adrenergic receptorHomo sapiens (human)
response to xenobiotic stimulusAlpha-1A adrenergic receptorHomo sapiens (human)
response to hormoneAlpha-1A adrenergic receptorHomo sapiens (human)
negative regulation of autophagyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle hypertrophyAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of action potentialAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of smooth muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
calcium ion transport into cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of cardiac muscle contractionAlpha-1A adrenergic receptorHomo sapiens (human)
cell growth involved in cardiac muscle cell developmentAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeAlpha-1A adrenergic receptorHomo sapiens (human)
positive regulation of protein kinase C signalingAlpha-1A adrenergic receptorHomo sapiens (human)
pilomotor reflexAlpha-1A adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1A adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-1B adrenergic receptorHomo sapiens (human)
intracellular signal transductionAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1B adrenergic receptorHomo sapiens (human)
regulation of cardiac muscle contractionAlpha-1B adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1B adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1B adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1B adrenergic receptorHomo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptorCanis lupus familiaris (dog)
regulation of smooth muscle contractionBeta-2 adrenergic receptorCanis lupus familiaris (dog)
positive regulation of MAPK cascadeBeta-2 adrenergic receptorCanis lupus familiaris (dog)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptorCanis lupus familiaris (dog)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptorCanis lupus familiaris (dog)
positive regulation of autophagosome maturationBeta-2 adrenergic receptorCanis lupus familiaris (dog)
positive regulation of lipophagyBeta-2 adrenergic receptorCanis lupus familiaris (dog)
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)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (63)

Processvia Protein(s)Taxonomy
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)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-1B adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-1B adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1B adrenergic receptorHomo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptorCanis lupus familiaris (dog)
protein homodimerization activityBeta-2 adrenergic receptorCanis lupus familiaris (dog)
norepinephrine bindingBeta-2 adrenergic receptorCanis lupus familiaris (dog)
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)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (52)

Processvia Protein(s)Taxonomy
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 membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
nucleusAlpha-1A adrenergic receptorHomo sapiens (human)
nucleoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1A adrenergic receptorHomo sapiens (human)
cytosolAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
caveolaAlpha-1A adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1A adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-1A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1A adrenergic receptorHomo sapiens (human)
nucleusAlpha-1B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
caveolaAlpha-1B adrenergic receptorHomo sapiens (human)
nuclear membraneAlpha-1B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1B adrenergic receptorHomo sapiens (human)
early endosomeBeta-2 adrenergic receptorCanis lupus familiaris (dog)
Golgi apparatusBeta-2 adrenergic receptorCanis lupus familiaris (dog)
receptor complexBeta-2 adrenergic receptorCanis lupus familiaris (dog)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
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)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (150)

Assay IDTitleYearJournalArticle
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.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID547621Cytotoxicity against BESM cells after 88 hrs by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1266201Antagonist activity at adrenergic alpha1A receptor (unknown origin) by firefly and renilla dual glo luciferase assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
AID661114Cytotoxicity against human HuH7 cells after 24 hrs by resazurin reduction assay2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Latent hit series hidden in high-throughput screening data.
AID1544698Antihypertensive activity in spontaneously hypertensive rat assessed as systolic arterial pressure at 80 mg/kg, po measured after 8 hrs by tail-cuff method (Rvb = 179.42 +/- 13.70 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1374284Selectivity index, ratio of pA2 for alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens to pA2 for antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen
AID41479Beta-2 adrenergic receptor binding affinity by measuring the displacement of [3H]DHA binding in rat lung2000Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
AID1544701Effect on heart rate in spontaneously hypertensive rat assessed as heart rate level at 80 mg/kg, po measured after 8 hrs by tail-cuff method (Rvb = 412.77 +/- 11.3 bpm)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1391652Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1391654Antagonist activity at alpha 1D adrenergic receptor (unknown origin) by luciferase reporter gene assay
AID1175741Cytotoxicity against human LNCAP cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines.
AID1202263Antagonist activity at Sprague-Dawley rat thoracic aorta adrenergic alpha-1D receptor after 20 mins2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1202261Antagonist activity at Sprague-Dawley rat prostatic vas deferens adrenergic alpha-1A receptor after 20 mins2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1515142Antiproliferative activity against human PC3 cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID1544696Effect on heart rate in spontaneously hypertensive rat assessed as heart rate level at 80 mg/kg, po measured after 4 hrs by tail-cuff method (Rvb = 410.80 +/- 17.4 bpm)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1546430Antiproliferative activity against human 786-O cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1544690Antihypertensive activity in spontaneously hypertensive rat assessed as diastolic arterial pressure at 80 mg/kg, po measured after 2 hrs by tail-cuff method (Rvb = 149.90 +/- 6 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1515146Antagonist activity at alpha1 androgen receptor (unknown origin) assessed as reduction in R1881-induced response at 10 uM by dual-luciferase reporter gene assay relative to control2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID1544684Effect on heart rate in spontaneously hypertensive rat assessed as heart rate level at 80 mg/kg, po measured after 0 hrs by tail-cuff method (Rvb = 413.17 +/- 10.5 bpm)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1391655Selectivity ratio of IC50 for alpha 1B adrenergic receptor (unknown origin) to IC50 for alpha 1A adrenergic receptor (unknown origin)
AID1202265Selectivity ratio for Sprague-Dawley rat thoracic aorta adrenergic alpha-1A receptor to Sprague-Dawley rat spleen adrenergic alpha-1B receptor2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1374285Displacement of [125I-HEAT from human alpha1A-adrenoreceptor expressed in CHOK1 cell membranes incubated for 60 mins
AID1544673Antihypertensive activity in spontaneously hypertensive rat assessed as mean arterial pressure at 80 mg/kg, po measured after 6 hrs by tail-cuff method (Rvb = 151.48 +/- 12.24 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544681Antihypertensive activity in spontaneously hypertensive rat assessed as systolic arterial pressure at 80 mg/kg, po measured after 0 hrs by tail-cuff method (Rvb = 186.10 +/- 4.55 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID661116Antagonist activity at ECMV genomic RNA internal ribosomal entry site in human HuH7 cells after 24 hrs by firefly luciferase reporter gene assay relative to control2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Latent hit series hidden in high-throughput screening data.
AID1509227Inhibition of MET in CD-1 mouse cochlea outer hair cells assessed as reduction in MET currents at 10 uM measured at -160 mV to +80 mV membrane potential by patch clamp assay2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1374282Selectivity index, ratio of pA2 for antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta to pA2 for antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens
AID1544695Antihypertensive activity in spontaneously hypertensive rat assessed as mean arterial pressure at 80 mg/kg, po measured after 4 hrs by tail-cuff method (Rvb = 150.30 +/- 9.26 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544671Effect on heart rate in spontaneously hypertensive rat assessed as heart rate level at 80 mg/kg, po measured after 6 hrs by tail-cuff method (Rvb = 411.12 +/- 19.1 bpm)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544676Antagonist activity at alpha-1D adrenergic receptor in SPF rat vas thoracic aorta assessed as inhibition of noradrenaline-induced contractions2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1175743Cytotoxicity against human RWPE1 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines.
AID1391656Selectivity ratio of IC50 for alpha 1B adrenergic receptor (unknown origin) to IC50 for alpha 1D adrenergic receptor (unknown origin)
AID1175740Cytotoxicity against human PC3 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines.
AID547622Antitrypanosomal activity against Trypanosoma cruzi amastigotes infected in BESM cells measured after 88 hrs postinfection by HTS assay2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1374277Vasodilatory activity in New Zealand White rabbit thoracic aorta assessed as relaxation of (-)-noradrenaline-induced contractile response at 1 uM relative to untreated control
AID1391635Cytotoxicity against human DU145 cells assessed as growth inhibition after 24 hrs by CCK8 assay
AID37469Alpha-1 adrenergic receptor binding affinity by measuring the displacement of [3H]prazosin binding in rat brain2000Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
AID1515144Antiproliferative activity against human LNCAP cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID40413Compound was evaluated for its Beta-1 adrenergic receptor binding affinity by measuring the displacement of [3H]dihydroalprenolol binding in rat heart; Not Active means Ki >1000 nM2000Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
AID1891862Antihypertensive activity in spontaneous hypertensive rat model assessed as systolic blood pressure at 40 mg/kg, po measured after 4 hr by tail cuff method (Rvb = 186.1 +/- 4.6 mmHg)2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Design, synthesis and biological evaluation of hydrogen sulfide-releasing isochroman-4-one derivatives as new antihypertensive agent candidates.
AID1544688Effect on heart rate in spontaneously hypertensive rat assessed as heart rate level at 80 mg/kg, po measured after 1 hr by tail-cuff method (Rvb = 415.25 +/- 14.7 bpm)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544682Antihypertensive activity in spontaneously hypertensive rat assessed as diastolic arterial pressure at 80 mg/kg, po measured after 0 hrs by tail-cuff method (Rvb = 149.50 +/- 5.4 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544697Antihypertensive activity in spontaneously hypertensive rat assessed as systolic arterial pressure at 80 mg/kg, po measured after 6 hrs by tail-cuff method (Rvb = 179.36 +/- 18.33 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1374280Antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen assessed as relaxation of (-)-noradrenaline-induced contractile response
AID1891861Antihypertensive activity in spontaneous hypertensive rat model assessed as systolic blood pressure at 40 mg/kg, po measured after 2 hr by tail cuff method (Rvb = 186.1 +/- 4.6 mmHg)2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Design, synthesis and biological evaluation of hydrogen sulfide-releasing isochroman-4-one derivatives as new antihypertensive agent candidates.
AID239249Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active2005Bioorganic & medicinal chemistry letters, Feb-01, Volume: 15, Issue:3
Pharmacophore identification of alpha(1A)-adrenoceptor antagonists.
AID1515145Antiproliferative activity against human RWPE1 cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID1544691Antihypertensive activity in spontaneously hypertensive rat assessed as mean arterial pressure at 80 mg/kg, po measured after 2 hrs by tail-cuff method (Rvb = 163 +/- 8.1 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544674Vasodilatory activity in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions at 10 uM relative to untreated control2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1374281Antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta assessed as relaxation of (-)-noradrenaline-induced contractile response
AID1509218Otoprotective activity against gentamicin-induced outer hair cell death in CD-1 mouse cochlea at 20 uM after 48 hrs by TRITC-phalloidin staining-based microscopic analysis relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1891864Antihypertensive activity in spontaneous hypertensive rat model assessed as systolic blood pressure at 40 mg/kg, po measured after 8 hr by tail cuff method (Rvb = 186.1 +/- 4.6 mmHg)2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Design, synthesis and biological evaluation of hydrogen sulfide-releasing isochroman-4-one derivatives as new antihypertensive agent candidates.
AID1202270Cytotoxicity against human PC3 cells2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1202269Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1202271Cytotoxicity against human DU145 cells2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1202266Selectivity ratio for Sprague-Dawley rat thoracic aorta adrenergic alpha-1D receptor to Sprague-Dawley rat spleen adrenergic alpha-1A receptor2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1544685Antihypertensive activity in spontaneously hypertensive rat assessed as systolic arterial pressure at 80 mg/kg, po measured after 1 hr by tail-cuff method (Rvb = 185.35 +/- 10.30 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1374286Displacement of [125I-HEAT from human alpha1B-adrenoreceptor expressed in CHOK1 cell membranes incubated for 60 mins
AID1546426Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1374276Vasodilatory activity in New Zealand White rabbit thoracic aorta assessed as relaxation of (-)-noradrenaline-induced contractile response at 0.1 uM relative to untreated control
AID1391636Cytotoxicity against human WPMY-1 cells assessed as growth inhibition after 24 hrs by CCK8 assay
AID1391634Cytotoxicity against human LNCAP cells assessed as growth inhibition after 24 hrs by CCK8 assay
AID1391633Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by CCK8 assay
AID547804Selectivity window, ratio of EC50 for BESM cells to EC50 for Trypanosoma cruzi amastigotes infected in BESM cells2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
Image-based high-throughput drug screening targeting the intracellular stage of Trypanosoma cruzi, the agent of Chagas' disease.
AID1202268Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1544687Antihypertensive activity in spontaneously hypertensive rat assessed as mean arterial pressure at 80 mg/kg, po measured after 1 hr by tail-cuff method (Rvb = 160 +/- 9.97 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544703Antihypertensive activity in spontaneously hypertensive rat assessed as reduction in mean arterial pressure at 80 mg/kg, po measured after 2 hrs by tail-cuff method2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1546429Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1546428Antiproliferative activity against human KK47 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1266202Antagonist activity at adrenergic alpha1B receptor (unknown origin) by firefly and renilla dual glo luciferase assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
AID1202267Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1509219Otoprotective activity against gentamicin-induced outer hair cell death in CD-1 mouse cochlea at 10 uM after 48 hrs by TRITC-phalloidin staining-based microscopic analysis relative to control2019Journal of medicinal chemistry, 06-13, Volume: 62, Issue:11
Design, Synthesis, and Biological Evaluation of a New Series of Carvedilol Derivatives That Protect Sensory Hair Cells from Aminoglycoside-Induced Damage by Blocking the Mechanoelectrical Transducer Channel.
AID1515143Antiproliferative activity against human DU145 cells after 24 hrs by CCK-8 assay2019Bioorganic & medicinal chemistry, 01-01, Volume: 27, Issue:1
Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.
AID1202264Selectivity ratio for Sprague-Dawley rat thoracic aorta adrenergic alpha-1D receptor to Sprague-Dawley rat spleen adrenergic alpha-1B receptor2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID661113Antagonist activity at ECMV genomic RNA internal ribosomal entry site in human HuH7 cells after 24 hrs by firefly luciferase reporter gene assay2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Latent hit series hidden in high-throughput screening data.
AID37248Alpha-2 adrenergic receptor binding affinity by measuring the displacement of [3H]clonidine binding in rat cerebral cortex2000Bioorganic & medicinal chemistry letters, Mar-06, Volume: 10, Issue:5
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
AID1374287Displacement of [125I-HEAT from human alpha1D-adrenoreceptor expressed in CHOK1 cell membranes incubated for 60 mins
AID1546424Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1544694Antihypertensive activity in spontaneously hypertensive rat assessed as diastolic arterial pressure at 80 mg/kg, po measured after 4 hrs by tail-cuff method (Rvb = 136.12 +/- 5.3 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1266205Selectivity ratio of IC50 for adrenergic alpha1B receptor (unknown origin) to IC50 for adrenergic alpha1D receptor (unknown origin)2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
AID1175742Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay2015Bioorganic & medicinal chemistry letters, Jan-15, Volume: 25, Issue:2
Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines.
AID1546433Antiproliferative activity against mouse MB49 cells assessed as reduction in cell viability after 72 hrs by WST-8 assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1544675Vasodilatory activity in Sprague-Dawley rat thoracic aorta assessed as inhibition of noradrenaline-induced contractions at 100 uM relative to untreated control2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1546431Cmax in Sprague-Dawley rat at 32 mg/kg, po measured after 15 mins by HPLC analysis2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1546425Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1546432AUC (0 to 6 hrs) in Sprague-Dawley rat at 32 mg/kg, po measured upto 6 hrs by HPLC analysis2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1546427Antiproliferative activity against human DU145 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2020Bioorganic & medicinal chemistry letters, 01-01, Volume: 30, Issue:1
Identification of HUHS190, a human naftopidil metabolite, as a novel anti-bladder cancer drug.
AID1544693Antihypertensive activity in spontaneously hypertensive rat assessed as systolic arterial pressure at 80 mg/kg, po measured after 4 hrs by tail-cuff method (Rvb = 178.66 +/- 17.18 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1374278Vasodilatory activity in New Zealand White rabbit thoracic aorta assessed as relaxation of (-)-noradrenaline-induced contractile response at 10 uM relative to untreated control
AID1544689Antihypertensive activity in spontaneously hypertensive rat assessed as systolic arterial pressure at 80 mg/kg, po measured after 2 hrs by tail-cuff method (Rvb = 189.20 +/- 12.31 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544700Antihypertensive activity in spontaneously hypertensive rat assessed as mean arterial pressure at 80 mg/kg, po measured after 8 hrs by tail-cuff method (Rvb = 153.55 +/- 11.43 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1202262Antagonist activity at Sprague-Dawley rat spleen adrenergic alpha-1B receptor after 20 mins2015European journal of medicinal chemistry, , Volume: 96Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
AID1544699Antihypertensive activity in spontaneously hypertensive rat assessed as diastolic arterial pressure at 80 mg/kg, po measured after 8 hrs by tail-cuff method (Rvb = 140.61 +/- 10.3 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1891863Antihypertensive activity in spontaneous hypertensive rat model assessed as systolic blood pressure at 40 mg/kg, po measured after 6 hr by tail cuff method (Rvb = 186.1 +/- 4.6 mmHg)2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Design, synthesis and biological evaluation of hydrogen sulfide-releasing isochroman-4-one derivatives as new antihypertensive agent candidates.
AID1374283Selectivity index, ratio of pA2 for antagonist activity at alpha1D-adrenoreceptor in Sprague-Dawley rat thoracic aorta to pA2 for antagonist activity at alpha1B-adrenoreceptor in Sprague-Dawley rat spleen
AID1391653Antagonist activity at alpha 1B adrenergic receptor (unknown origin) by luciferase reporter gene assay
AID1266204Selectivity ratio of IC50 for adrenergic alpha1B receptor (unknown origin) to IC50 for adrenergic alpha1A receptor (unknown origin)2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
AID1266203Antagonist activity at adrenergic alpha1D receptor (unknown origin) by firefly and renilla dual glo luciferase assay2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
AID1544686Antihypertensive activity in spontaneously hypertensive rat assessed as diastolic arterial pressure at 80 mg/kg, po measured after 1 hr by tail-cuff method (Rvb = 147.33 +/- 9.8 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1374279Antagonist activity at alpha1A-adrenoreceptor in Sprague-Dawley rat vas deferens assessed as relaxation of (-)-noradrenaline-induced contractile response
AID1544672Antihypertensive activity in spontaneously hypertensive rat assessed as diastolic arterial pressure at 80 mg/kg, po measured after 6 hrs by tail-cuff method (Rvb = 137.54 +/- 9.2 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1544683Antihypertensive activity in spontaneously hypertensive rat assessed as mean arterial pressure at 80 mg/kg, po measured after 0 hrs by tail-cuff method (Rvb = 161.70 +/- 5.12 mmHg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
AID1891860Antihypertensive activity in spontaneous hypertensive rat model assessed as systolic blood pressure at 40 mg/kg, po measured after 1 hr by tail cuff method (Rvb = 186.1 +/- 4.6 mmHg)2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Design, synthesis and biological evaluation of hydrogen sulfide-releasing isochroman-4-one derivatives as new antihypertensive agent candidates.
AID1544692Effect on heart rate in spontaneously hypertensive rat assessed as heart rate level at 80 mg/kg, po measured after 2 hrs by tail-cuff method (Rvb = 413.2 +/- 15.2 bpm)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Design, synthesis and biological evaluation of isochroman-4-one hybrids bearing piperazine moiety as antihypertensive agent candidates.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (230)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's24 (10.43)18.2507
2000's67 (29.13)29.6817
2010's117 (50.87)24.3611
2020's22 (9.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 52.76

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

MetricThis Compound (vs All)
Research Demand Index52.76 (24.57)
Research Supply Index5.68 (2.92)
Research Growth Index4.90 (4.65)
Search Engine Demand Index84.65 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (52.76)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials58 (24.89%)5.53%
Reviews15 (6.44%)6.00%
Case Studies1 (0.43%)4.05%
Observational3 (1.29%)0.25%
Other156 (66.95%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Medical Expulsive Therapy for Ureter Stone Using Naftopidil: Multicenter, Randomized, Double-blind, Placebo Controlled Study [NCT01952314]Phase 3150 participants (Actual)Interventional2014-05-31Completed
A Clinical Trial to Investigate the Safety/Tolerability and Pharmacokinetics of Naftopidil After Oral Administration in Korean Healthy Male Volunteers [NCT00967772]Phase 116 participants (Actual)Interventional2009-09-30Completed
The Effect of Naftopidil for the Double-J Stent Discomfort: Multicenter, Randomized, Double-blind, Placebo Controlled Study [NCT01959074]Phase 3100 participants (Actual)Interventional2014-05-31Completed
The Effectiveness and Safety of Naftopidil 75mg for Improving Clearance of Ureteral and Renal Stones After Shockwave Lithotripsy: Prospective Randomized Controlled Study [NCT02011737]Phase 4130 participants (Anticipated)Interventional2014-02-28Not yet recruiting
PHASE III, DOUBLE-BLIND, RANDOMIZED STUDY COMPARING THE EFFICACY AND SAFETY OF NAFTOPIDIL AND TAMSULOSIN TO TREATMENT THE SYMPTOMS OF LOWER URINARY TRACT IN PATIENTS WITH BENIGN PROSTATE HYPERPLASIA [NCT01203371]Phase 30 participants (Actual)Interventional2011-01-01Withdrawn
A Randomized, Double-blind, Double-dummy, Placebo-controlled, Parallel Design Clinical Trial to Evaluate the Efficacy and Safety of Naftopidil in Male Patients With Lower Urinary Tract Symptoms Associated With Benign Prostatic Hyperplasia [NCT01922375]Phase 4411 participants (Actual)Interventional2011-12-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]