Page last updated: 2024-11-12
ly 404187
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
LY 404187: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 9928016 |
| CHEMBL ID | 435582 |
| SCHEMBL ID | 2134262 |
| MeSH ID | M0393583 |
Synonyms (38)
| Synonym |
|---|
| n-[2-[4-(4-cyanophenyl)phenyl]propyl]propane-2-sulfonamide |
| propane-2-sulfonic acid [2-(4''-cyano-biphenyl-4-yl)-propyl]-amide |
| bdbm50094024 |
| (+/-) propane-2-sulfonic acid [2-(4''-cyano-biphenyl-4-yl)-propyl]-amide |
| CHEMBL435582 , |
| ly-404187 |
| SCHEMBL2134262 |
| AKOS016000577 |
| 211311-95-4 |
| ly 404187 |
| n-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonamide |
| n-2-(4-(4-cyanophenyl)phenyl)propyl 2-propanesulfonamide |
| 75W6I8W6OU , |
| 2-propanesulfonamide, n-(2-(4'-cyano(1,1'-biphenyl)-4-yl)propyl)- |
| ly404187 |
| gtpl4249 |
| n-{2-[4-(4-cyanophenyl)phenyl]propyl}propane-2-sulfonamide |
| ly-404,187 |
| n-(2-(4'-cyano-[1,1'-biphenyl]-4-yl)propyl)propane-2-sulfonamide |
| unii-75w6i8w6ou |
| n-[2-(4'-cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide |
| c19h22n2o2s |
| DTXSID00432983 |
| mfcd07364003 |
| HY-13456 |
| CS-0006907 |
| NCGC00370739-04 |
| BCP06868 |
| EX-A2611 |
| Q27083110 |
| AS-16419 |
| Q6460433 |
| 2-propanesulfonamide, n-[2-(4'-cyano[1,1'-biphenyl]-4-yl)propyl]- |
| NCGC00370739-05 |
| A879241 |
| SB83581 |
| F87232 |
| AC-36177 |
Research Excerpts
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "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
| Excerpt | Relevance | Reference |
|---|---|---|
| " Further, in C57Bl/6 mice, imipramine produced a "U-shaped" dose-response curve in the FST, whilst no evidence of a biphasic response was present in the TST at doses up to 45 mg/kg." | ( Intra- and interstrain differences in models of "behavioral despair". Bai, F; Clay, M; Li, X; Lindstrom, T; Skolnick, P, ) | 0.13 |
| "Agonistic profiles of AMPA receptor (AMPA-R) potentiators may be associated with seizure risk and bell-shaped dose-response effects." | ( Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement. Awasaki, Y; Kaku, T; Kimura, H; Kosugi, Y; Kuno, H; Kunugi, A; Sogabe, S; Suzuki, A; Suzuki, M; Suzuki, N; Tajima, Y; Toyofuku, M, 2021) | 0.62 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (4)
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Glutamate receptor 1 | Homo sapiens (human) | EC50 (µMol) | 5.6500 | 0.3800 | 4.1138 | 10.0000 | AID536773 |
| Glutamate receptor 2 | Homo sapiens (human) | EC50 (µMol) | 1.0135 | 0.1500 | 3.0560 | 7.6000 | AID270083; AID270084; AID536775; AID536782 |
| Glutamate receptor 3 | Homo sapiens (human) | EC50 (µMol) | 1.6600 | 1.6600 | 4.4067 | 7.9000 | AID536781 |
| Glutamate receptor 4 | Homo sapiens (human) | EC50 (µMol) | 0.4702 | 0.2900 | 2.8772 | 7.6000 | AID223222; AID270081; AID270082; AID536772; AID75673 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (39)
Molecular Functions (23)
Ceullar Components (37)
Bioassays (21)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID270082 | Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19 | A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives. |
| AID536781 | Inhibition of GluR3 expressed in HEK cells | 2010 | Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20 | Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. |
| AID536782 | Agonist activity at GluR2 receptor | 2010 | Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20 | Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. |
| AID536773 | Inhibition of GluR1 expressed in HEK cells | 2010 | Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20 | Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. |
| AID536775 | Inhibition of GluR2 flop expressed in HEK cells | 2010 | Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20 | Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. |
| AID536772 | Inhibition of GluR4 expressed in HEK293 cells | 2010 | Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20 | Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. |
| AID270084 | Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19 | A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives. |
| AID223222 | Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells | 2000 | Journal of medicinal chemistry, Nov-16, Volume: 43, Issue:23 | Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors. |
| AID75673 | Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors. | 2002 | Journal of medicinal chemistry, May-09, Volume: 45, Issue:10 | Design and synthesis of a novel series of 1,2-disubstituted cyclopentanes as small, potent potentiators of 2-amino-3-(3-hydroxy-5-methyl-isoxazol-4-yl)propanoic acid (AMPA) receptors. |
| AID270083 | Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19 | A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives. |
| AID536778 | Agonist activity at AMPA receptor by FLIPR assay | 2010 | Journal of medicinal chemistry, Oct-28, Volume: 53, Issue:20 | Positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor. |
| AID270081 | Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay | 2006 | Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19 | A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives. |
| 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. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 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. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine 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. |
| AID1346557 | Human GluA1 (Ionotropic glutamate receptors) | 2001 | Neuropharmacology, Jun, Volume: 40, Issue:8 | Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. |
| AID1346546 | Human GluA4 (Ionotropic glutamate receptors) | 2001 | Neuropharmacology, Jun, Volume: 40, Issue:8 | Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. |
| AID1346582 | Human GluA2 (Ionotropic glutamate receptors) | 2001 | Neuropharmacology, Jun, Volume: 40, Issue:8 | Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. |
| AID1346589 | Human GluA3 (Ionotropic glutamate receptors) | 2001 | Neuropharmacology, Jun, Volume: 40, Issue:8 | Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (31)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 18 (58.06) | 29.6817 |
| 2010's | 10 (32.26) | 24.3611 |
| 2020's | 3 (9.68) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 17.61
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.61) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (3.13%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 31 (96.88%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||