Page last updated: 2024-12-08
lu 135252
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
ID Source | ID |
---|---|
PubMed CID | 177236 |
CHEMBL ID | 23261 |
SCHEMBL ID | 795084 |
MeSH ID | M0280379 |
Synonyms (44)
Synonym |
---|
lu-135252 |
darusentan |
hmr-4005 |
lu 135252 |
benzenepropanoic acid, alpha-((4,6-dimethoxy-2-pyrimidinyl)oxy)-beta-methoxy-beta-phenyl-, (s)- |
(+)-(s)-2-((4,6-dimethoxy-2-pyrimidinyl)oxy)-3-methoxy-3,3-diphenylpropionic acid |
benzenepropanoic acid, alpha-((4,6-dimethoxy-2-pyrimidinyl)oxy)-beta-methoxy-beta-phenyl-, (alphas)- |
lu135252 |
lu 127043 |
2-(4,6-dimethoxypyrimidin-2-yloxy)-3-methoxy-3,3-diphenylpropionic acid |
CHEMBL23261 , |
(2s)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid |
bdbm50108202 |
(s)-2-(4,6-dimethoxy-pyrimidin-2-yloxy)-3-methoxy-3,3-diphenyl-propionic acid |
33jd57l6rw , |
darusentan [inn] |
unii-33jd57l6rw |
171714-84-4 |
AKOS015994552 |
(2s)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-di(phenyl)propanoic acid |
gtpl3508 |
benzenepropanoic acid, .alpha.-((4,6-dimethoxy-2-pyrimidinyl)oxy)-.beta.-methoxy-.beta.-phenyl-, (s)- |
darusentan [who-dd] |
darusentan [mi] |
DB04883 |
cas-171714-84-4 |
NCGC00253632-01 |
dtxsid1057664 , |
tox21_113760 |
dtxcid2031453 |
EE-0200 |
SCHEMBL795084 |
d-265 , |
Q5225810 |
(s)-2-((4,6-dimethoxypyrimidin-2-yl)oxy)-3-methoxy-3,3-diphenylpropanoic acid |
BCP13024 |
CS-0006252 |
HY-15404 |
N16986 |
(2s)-2-(4,6-dimethoxypyrimidin-2-yl)oxy-3-methoxy-3,3-diphenylpropanoic acid. |
s-darusentan |
(s)-2-((4,6-dimethoxy-2-pyrimidinyl)oxy)-3-methoxy-3,3-diphenylpropionic acid |
A855219 |
WGA71484 |
Research Excerpts
Treatment
Treatment with LU 135252 (100 mg/kg body wt) did not affect systolic blood pressure (BP) in animals on a normal salt diet during the whole period of the experiment (18 weeks) or in salt-loaded animals until week 10. Treatment withLU 135252 significantly decreased the ET-1 excretion by more than 50%.
Toxicity
Excerpt | Reference | Relevance |
---|---|---|
" Darusentan was generally well tolerated; mild to moderate edema and headache were the most common adverse events." | ( Efficacy and safety of darusentan in patients with resistant hypertension: results from a randomized, double-blind, placebo-controlled dose-ranging study. Bakris, GL; Black, HR; Gerber, MJ; Linas, S; Linseman, JV; Marple, R; Roden, R; Shahawy, ME; Tannoury, G; Weber, MA; Weiss, R; Wiens, BL, 2007) | 0.34 |
Pharmacokinetics
Excerpt | Reference | Relevance |
---|---|---|
" Acute inhibition of both ETA and ETB receptors with bosentan dramatically prolonged 125I-ET-1 plasma half-life and shifted tissue uptake from lung to liver and kidneys." | ( Receptor- and non-receptor-mediated clearance of big-endothelin and endothelin-1: differential effects of acute and chronic ETA receptor blockade. Barton, M; Burkhardt, M; Shaw, SG, 2000) | 0.31 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
"The effect of the orally highly bioavailable and specific endothelin A (ET(A)) receptor antagonist LU 135252 was assessed in a model of chronic renal allograft nephropathy." | ( The ET(A) receptor blocker LU 135252 prevents chronic transplant nephropathy in the "Fisher to Lewis" model. Amann, K; Odoni, G; Orth, SR; Raschack, M; Ritz, E; Strzelczyk, P, 1999) | 0.82 |
" Here we report an expansion of this work by substituting a variety of electron-withdrawing groups at the ortho position and evaluating their effects on oral bioavailability as well as structure-activity relationships." | ( Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. Berens, KL; Blok, N; Bourgoyne, AR; Brock, TA; Bui, H; Decker, ER; Dixon, RA; Holland, GW; Knowles, V; Wang, J; Wu, C; You, TJ, 2004) | 0.32 |
Dosage Studied
Excerpt | Relevance | Reference |
---|---|---|
" Similar direct comparative studies in other models of PH and with various dosage regimens are warranted to define the optimal pharmacological approach of PH when ET receptor antagonists are used." | ( Effectiveness of a nonselective ET(A/B) and a selective ET(A) antagonist in rats with monocrotaline-induced pulmonary hypertension. Cernacek, P; Dupuis, J; Jasmin, JF; Lucas, M, 2001) | 0.31 |
"In a multicenter randomized, double-blind, parallel-group, dose-response study, a 2-week placebo run-in period was followed by a 6-week treatment period and then a 2-week placebo withdrawal period." | ( Darusentan: an effective endothelinA receptor antagonist for treatment of hypertension. Eberle, S; Nakov, R; Pfarr, E, 2002) | 0.31 |
" Patients were randomized to different dosage levels of darusentan (30, 100, or 300 mg) for 3 weeks." | ( Neurohumoral and hemodynamic effects of the selective endothelin antagonist darusentan in advanced chronic heart failure. Berger, R; Bergler-Klein, J; Bojic, A; Pacher, R; Stanek, B, 2004) | 0.32 |
" Darusentan's unique mechanism of action, dose-dependent blood pressure-lowering profile, once-daily dosing regimen, and sustained 24-hour blood pressure-lowering effect are valuable features." | ( Efficacy and safety of darusentan: a novel endothelin receptor antagonist. Epstein, BJ, 2008) | 0.35 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (6)
Potency Measurements
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 33.4889 | 0.0010 | 24.5048 | 61.6448 | AID743215 |
heat shock protein beta-1 | Homo sapiens (human) | Potency | 34.4811 | 0.0420 | 27.3789 | 61.6448 | AID743210; AID743228 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Inhibition Measurements
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Endothelin receptor type B | Rattus norvegicus (Norway rat) | Ki | 0.3710 | 0.0063 | 0.0575 | 0.3710 | AID1626382 |
Endothelin receptor type B | Homo sapiens (human) | IC50 (µMol) | 0.0160 | 0.0001 | 0.6565 | 9.8000 | AID66370 |
Endothelin receptor type B | Homo sapiens (human) | Ki | 0.3710 | 0.0001 | 0.0543 | 0.3710 | AID1626382 |
Endothelin-1 receptor | Homo sapiens (human) | IC50 (µMol) | 0.0008 | 0.0000 | 0.7647 | 9.9000 | AID68304 |
Endothelin-1 receptor | Homo sapiens (human) | Ki | 0.0060 | 0.0000 | 0.4300 | 10.0000 | AID1626381 |
Endothelin-1 receptor | Rattus norvegicus (Norway rat) | Ki | 0.0060 | 0.0000 | 0.0021 | 0.0065 | AID66210 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (109)
Molecular Functions (5)
Process | via Protein(s) | Taxonomy |
---|---|---|
endothelin receptor activity | Endothelin receptor type B | Homo sapiens (human) |
protein binding | Endothelin receptor type B | Homo sapiens (human) |
peptide hormone binding | Endothelin receptor type B | Homo sapiens (human) |
type 1 angiotensin receptor binding | Endothelin receptor type B | Homo sapiens (human) |
phosphatidylinositol phospholipase C activity | Endothelin-1 receptor | Homo sapiens (human) |
endothelin receptor activity | Endothelin-1 receptor | Homo sapiens (human) |
protein binding | Endothelin-1 receptor | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Ceullar Components (2)
Process | via Protein(s) | Taxonomy |
---|---|---|
plasma membrane | Endothelin receptor type B | Homo sapiens (human) |
nuclear membrane | Endothelin receptor type B | Homo sapiens (human) |
plasma membrane | Endothelin receptor type B | Homo sapiens (human) |
plasma membrane | Endothelin-1 receptor | Homo sapiens (human) |
plasma membrane | Endothelin-1 receptor | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Bioassays (42)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1626381 | Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective. |
AID189541 | Compound was tested for %inhibition of big ET-induced bronchospasm in guinea pigs with LU 135252 and balanced ETA/B receptor antagonists at 10 mg/kg oral dose, 2 hr pretreatment was reported as (AUD 30 min) in mL(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
AID66214 | Selectivity for endothelin A receptor over endothelin receptor B | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
AID1626382 | Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15 | From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective. |
AID66210 | Binding affinity towards Endothelin A receptor | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8 | Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
AID172171 | Inhibition of big ET-induced blood pressure increase in drug treated rats with 10 mg/Kg of compound given perorally was reported as (AUD 30 min) in mmHg(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
AID66370 | Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement. | 2002 | Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2 | The design and synthesis of a novel series of indole derived selective ET(A) antagonists. |
AID68304 | Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor | 2002 | Bioorganic & medicinal chemistry letters, Jan-21, Volume: 12, Issue:2 | The design and synthesis of a novel series of indole derived selective ET(A) antagonists. |
AID172173 | Percent reduction of big ET-induced blood pressure increase in drug treated rats with 10 mg/Kg of compound given perorally was reported as (AUD 30 min) in mmHg(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
AID189544 | Compound was tested for inhibition of big ET-induced bronchospasm in drug treated guinea pigs with LU 135252 and balanced ETA/B receptor antagonists at 30 mg/kg oral dose, 2 hr pretreatment was reported as (AUD 30 min) in mL(min) | 1999 | Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16 | Discovery and synthesis of (S)-3-[2-(3,4-dimethoxyphenyl)ethoxy]-2- (4,6-dimethylpyrimidin-2-yloxy)-3,3-diphenylpropionic acid (LU 302872), a novel orally active mixed ET(A)/ET(B) receptor antagonist. |
AID1345905 | Human ETA receptor (Endothelin receptors) | 1996 | Journal of medicinal chemistry, May-24, Volume: 39, Issue:11 | Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (191)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 49 (25.65) | 18.2507 |
2000's | 115 (60.21) | 29.6817 |
2010's | 21 (10.99) | 24.3611 |
2020's | 6 (3.14) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 9.03
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 weak demand-to-supply ratio for research on this compound.
| This Compound (9.03) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 13 (6.63%) | 5.53% |
Reviews | 11 (5.61%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 172 (87.76%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |