Page last updated: 2024-11-13
am 966
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 | 46240292 |
| CHEMBL ID | 3621966 |
| SCHEMBL ID | 2292013 |
| MeSH ID | M0552064 |
Synonyms (32)
| Synonym |
|---|
| gtpl2905 |
| am 966 |
| 2-(4-{4-[4-({[(1r)-1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-methyl-1,2-oxazol-5-yl]phenyl}phenyl)acetic acid |
| am-966 |
| am966 , |
| HY-15277 |
| unii-ceo54nh393 |
| 1228690-19-4 |
| ceo54nh393 , |
| (4'-(4-((r)-1-(2-chlorophenyl)ethoxycarbonylamino)-3-methylisoxazol-5-yl)biphenyl-4-yl)acetic acid |
| (1,1'-biphenyl)-4-acetic acid, 4'-(4-((((1r)-1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methyl-5-isoxazolyl)- |
| (4'-(4-(((((r)-1-(2-chlorophenyl)ethyl)oxy)carbonyl)amino)-3-methylisoxazol-5-yl)biphenyl-4-yl)acetic acid |
| (4'-{4-[(r)-1-(2-chloro-phenyl)-eth-oxycarbonylamino]-3-methyl-isoxazol-5-yl}-biphenyl-4-yl)-acetic acid |
| AKOS024258999 |
| SCHEMBL2292013 |
| (r)-2-(4'-(4-(((1-(2-chlorophenyl)ethoxy)carbonyl)amino)-3-methylisoxazol-5-yl)-[1,1'-biphenyl]-4-yl)acetic acid |
| CHEMBL3621966 |
| DTXSID10153758 |
| AS-74930 |
| 2-{4'-[4-({[(1r)-1-(2-chlorophenyl)ethoxy]carbonyl}amino)-3-methyl-1,2-oxazol-5-yl]-[1,1'-biphenyl]-4-yl}acetic acid |
| NCGC00378914-01 |
| NCGC00378914-02 |
| BCP16395 |
| mfcd20486575 |
| Q27074426 |
| EX-A1956 |
| [1,1'-biphenyl]-4-acetic acid, 4'-[4-[[[(1r)-1-(2-chlorophenyl)ethoxy]carbonyl]amino]-3-methyl-5-isoxazolyl]- |
| C71895 |
| A858126 |
| 2-[4-[4-[4-[[(1r)-1-(2-chlorophenyl)ethoxy]carbonylamino]-3-methyl-1,2-oxazol-5-yl]phenyl]phenyl]acetic acid |
| 2-[4-[4-[4-[[(1r)-1-(2-chlorophenyl)ethoxy]carbonylamino]-3-methyl-isoxazol-5-yl]phenyl]phenyl]acetic acid |
| AC-35886 |
Research Excerpts
Pharmacokinetics
| Excerpt | Reference | Relevance |
|---|---|---|
| " Here, we evaluated the in vitro pharmacology, pharmacokinetic, and pharmacodynamic properties of the LPA₁-selective antagonist AM095 (sodium, {4'-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-biphenyl-4-yl}-acetate) and assessed the effects of AM095 in rodent models of lung and kidney fibrosis and dermal wound healing." | ( Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Baccei, CS; Bain, G; Broadhead, AR; Chapman, C; Correa, LD; Darlington, J; Evans, JF; Hutchinson, JH; King, CD; Lee, C; Lorrain, DS; Parr, TA; Prasit, P; Roppe, JR; Santini, AM; Seiders, TJ; Stebbins, KJ; Swaney, JS; Ziff, J, 2011) | 0.37 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "These findings demonstrate that AM966 is a potent, selective, orally bioavailable LPA(1) receptor antagonist that may be beneficial in treating lung injury and fibrosis, as well as other diseases that are characterized by pathological inflammation, oedema and fibrosis." | ( A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Baccei, CS; Bundey, RA; Chapman, C; Correa, LD; Evans, JF; Fagan, P; Hutchinson, JH; Lorrain, DS; Parr, TA; Prasit, P; Prodanovich, PC; Santini, AM; Seiders, TJ; Stebbins, KJ; Swaney, JS, 2010) | 0.36 |
| " In vivo, we demonstrated that AM095: 1) had high oral bioavailability and a moderate half-life and was well tolerated at the doses tested in rats and dogs after oral and intravenous dosing, 2) dose-dependently reduced LPA-stimulated histamine release, 3) attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and 4) decreased kidney fibrosis in a mouse unilateral ureteral obstruction model." | ( Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Baccei, CS; Bain, G; Broadhead, AR; Chapman, C; Correa, LD; Darlington, J; Evans, JF; Hutchinson, JH; King, CD; Lee, C; Lorrain, DS; Parr, TA; Prasit, P; Roppe, JR; Santini, AM; Seiders, TJ; Stebbins, KJ; Swaney, JS; Ziff, J, 2011) | 0.37 |
| "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 |
|---|---|---|
| " AM966 demonstrated a good pharmacokinetic profile following oral dosing in mice." | ( A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Baccei, CS; Bundey, RA; Chapman, C; Correa, LD; Evans, JF; Fagan, P; Hutchinson, JH; Lorrain, DS; Parr, TA; Prasit, P; Prodanovich, PC; Santini, AM; Seiders, TJ; Stebbins, KJ; Swaney, JS, 2010) | 0.36 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (7)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 10.6840 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 3.0112 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 30.1116 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 3.0112 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 3.0112 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 3.0112 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 3.0112 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (45)
Molecular Functions (18)
Ceullar Components (22)
Bioassays (26)
| 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. |
| 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. |
| AID1347164 | 384 well plate NINDS Rhodamine confirmatory 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. |
| AID1347169 | Tertiary RLuc qRT-PCR qHTS assay 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. |
| AID1347163 | 384 well plate NINDS AMC confirmatory 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. |
| 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. |
| 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. |
| AID1347149 | Furin counterscreen 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. |
| AID1347152 | Confirmatory screen NINDS 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. |
| AID1347161 | Confirmatory 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. |
| AID1347167 | Vero cells viability 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. |
| AID1347168 | HepG2 cells viability 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. |
| AID1347157 | Confirmatory screen GU Rhodamine qHTS for Zika virus inhibitors qHTS | 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. |
| AID1347153 | Confirmatory 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. |
| 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. |
| AID1623909 | Antagonist activity at mouse TRPV2/LPAR1 expressed in LPA-stimulated HEK293T cells assessed as inhibition of 2-APB evoked currents at 10 uM dosed 3 mins after LPA stimulation by whole-cell patch clamp assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel. |
| AID1623917 | Antagonist activity at mouse TRPV2/LPAR1 expressed in LPA-stimulated HEK293T cells assessed as inhibition of 2-APB evoked currents at 1 uM dosed 3 mins after LPA stimulation by whole-cell patch clamp assay | 2019 | Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3 | Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel. |
| AID1346184 | Mouse LPA3 receptor (Lysophospholipid (LPA) receptors) | 2010 | British journal of pharmacology, Aug, Volume: 160, Issue:7 | A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. |
| AID1346114 | Human LPA1 receptor (Lysophospholipid (LPA) receptors) | 2011 | The Journal of pharmacology and experimental therapeutics, Mar, Volume: 336, Issue:3 | Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. |
| AID1346025 | Mouse LPA2 receptor (Lysophospholipid (LPA) receptors) | 2010 | British journal of pharmacology, Aug, Volume: 160, Issue:7 | A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. |
| AID1346958 | Human LPA4 receptor (Lysophospholipid (LPA) receptors) | 2010 | British journal of pharmacology, Aug, Volume: 160, Issue:7 | A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. |
| AID1346019 | Mouse LPA1 receptor (Lysophospholipid (LPA) receptors) | 2010 | British journal of pharmacology, Aug, Volume: 160, Issue:7 | A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. |
| AID1346102 | Human LPA2 receptor (Lysophospholipid (LPA) receptors) | 2010 | British journal of pharmacology, Aug, Volume: 160, Issue:7 | A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. |
| AID1346181 | Human LPA3 receptor (Lysophospholipid (LPA) receptors) | 2010 | British journal of pharmacology, Aug, Volume: 160, Issue:7 | A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. |
| AID1347158 | ZIKV-mCherry secondary 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. |
| AID1347156 | DAPI mCherry counterscreen 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (6)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 4 (66.67) | 24.3611 |
| 2020's | 2 (33.33) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 18.45
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 (18.45) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||