Page last updated: 2024-11-12

cs-2100

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID11977938
CHEMBL ID1951304
SCHEMBL ID3132510
MeSH IDM0573881

Synonyms (20)

Synonym
bdbm50364607
CHEMBL1951304 ,
DWVJASHDNJMDNH-UHFFFAOYSA-N ,
1-({4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl}methyl)azetidine-3-carboxylic acid
CS-2100 ,
SCHEMBL3132510
913827-99-3
1-[[4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylic acid
cs 2100
AKOS024458213
NCGC00379155-01
1-[[4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-2-thienyl]methyl]-3-azetidinecarboxylicacid
1-[[4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]thiophen-2-yl]methyl]azetidine-3-carboxylic acid
1-[[4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]-
2-thienyl]methyl]-3-azetidinecarboxylic acid
CS-0028983
HY-108493
1-[[4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]- 2-thienyl]methyl]-3-azetidinecarboxylic acid
1-({4-ethyl-5-[5-(4-phenoxyphenyl)-1,2,4-oxadiazol-3-yl]thiophen-2-yl}methyl)azetidine-3-carboxylic acid
1-((4-ETHYL-5-(5-(4-PHENOXYPHENYL)-1,2,4-OXADIAZOL-3-YL)THIOPHEN-2-YL)METHYL)AZETIDINE-3-CARBOXYLIC ACID ,

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency18.51390.01237.983543.2770AID1645841
[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)
Sphingosine 1-phosphate receptor 4Homo sapiens (human)EC50 (µMol)0.05800.00010.26263.2500AID648607
Sphingosine 1-phosphate receptor 1Homo sapiens (human)EC50 (µMol)0.00400.00000.17597.8700AID645220; AID648581; AID660636
Sphingosine 1-phosphate receptor 1Rattus norvegicus (Norway rat)EC50 (µMol)0.00150.00030.00070.0015AID648579
Sphingosine 1-phosphate receptor 3Homo sapiens (human)EC50 (µMol)20.00000.00010.30925.0000AID645221; AID648582; AID660637
Sphingosine 1-phosphate receptor 5Homo sapiens (human)EC50 (µMol)0.01700.00020.13653.1623AID648608
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (40)

Processvia Protein(s)Taxonomy
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 4Homo sapiens (human)
immune responseSphingosine 1-phosphate receptor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 4Homo sapiens (human)
activation of phospholipase C activitySphingosine 1-phosphate receptor 4Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSphingosine 1-phosphate receptor 4Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 4Homo sapiens (human)
blood vessel maturationSphingosine 1-phosphate receptor 1Homo sapiens (human)
cardiac muscle tissue growth involved in heart morphogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell adhesionSphingosine 1-phosphate receptor 1Homo sapiens (human)
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
brain developmentSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell population proliferationSphingosine 1-phosphate receptor 1Homo sapiens (human)
cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
transmission of nerve impulseSphingosine 1-phosphate receptor 1Homo sapiens (human)
lamellipodium assemblySphingosine 1-phosphate receptor 1Homo sapiens (human)
actin cytoskeleton organizationSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of cell adhesionSphingosine 1-phosphate receptor 1Homo sapiens (human)
neuron differentiationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of bone mineralizationSphingosine 1-phosphate receptor 1Homo sapiens (human)
leukocyte chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of bone resorptionSphingosine 1-phosphate receptor 1Homo sapiens (human)
endothelial cell differentiationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of smooth muscle cell proliferationSphingosine 1-phosphate receptor 1Homo sapiens (human)
positive regulation of positive chemotaxisSphingosine 1-phosphate receptor 1Homo sapiens (human)
negative regulation of stress fiber assemblySphingosine 1-phosphate receptor 1Homo sapiens (human)
heart trabecula morphogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
T cell migrationSphingosine 1-phosphate receptor 1Homo sapiens (human)
angiogenesisSphingosine 1-phosphate receptor 1Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 1Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
inflammatory responseSphingosine 1-phosphate receptor 3Homo sapiens (human)
G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationSphingosine 1-phosphate receptor 3Homo sapiens (human)
Notch signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
positive regulation of cell population proliferationSphingosine 1-phosphate receptor 3Homo sapiens (human)
anatomical structure morphogenesisSphingosine 1-phosphate receptor 3Homo sapiens (human)
regulation of interleukin-1 beta productionSphingosine 1-phosphate receptor 3Homo sapiens (human)
negative regulation of establishment of endothelial barrierSphingosine 1-phosphate receptor 3Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 3Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 3Homo sapiens (human)
sphingosine-1-phosphate receptor signaling pathwaySphingosine 1-phosphate receptor 5Homo sapiens (human)
regulation of neuron differentiationSphingosine 1-phosphate receptor 5Homo sapiens (human)
regulation of metabolic processSphingosine 1-phosphate receptor 5Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwaySphingosine 1-phosphate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
protein bindingSphingosine 1-phosphate receptor 4Homo sapiens (human)
lipid bindingSphingosine 1-phosphate receptor 4Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 4Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 4Homo sapiens (human)
G protein-coupled receptor bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 1Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 1Homo sapiens (human)
sphingolipid bindingSphingosine 1-phosphate receptor 1Homo sapiens (human)
integrin bindingSphingosine 1-phosphate receptor 3Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 3Homo sapiens (human)
lipid bindingSphingosine 1-phosphate receptor 3Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 3Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 3Homo sapiens (human)
protein bindingSphingosine 1-phosphate receptor 5Homo sapiens (human)
sphingosine-1-phosphate receptor activitySphingosine 1-phosphate receptor 5Homo sapiens (human)
G protein-coupled receptor activitySphingosine 1-phosphate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
mitochondrionSphingosine 1-phosphate receptor 4Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 4Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 4Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 4Homo sapiens (human)
nucleoplasmSphingosine 1-phosphate receptor 1Homo sapiens (human)
endosomeSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
external side of plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
intracellular membrane-bounded organelleSphingosine 1-phosphate receptor 1Homo sapiens (human)
membrane raftSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 1Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 1Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 3Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 3Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 3Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 5Homo sapiens (human)
cytoplasmSphingosine 1-phosphate receptor 5Homo sapiens (human)
plasma membraneSphingosine 1-phosphate receptor 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (47)

Assay IDTitleYearJournalArticle
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.
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.
AID1347160Primary screen NINDS Rhodamine 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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
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.
AID660666Drug metabolism in po dosed monkey plasma assessed as formation of 4-phenoxy benzoic acid2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648581Agonist activity at human S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648603Drug metabolism in po dosed rat plasma assessed as 4-PBA level2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648598AUC (0 to 72 hrs) in Lewis rat at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648599Cmax in C57BL/6J mouse at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID660661Stability of the compound in presence of enterobacteria from monkey feces contents under anaerobic condition at 3 to 30 uM after 24 hrs2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648595Cmax in Lewis rat at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648591Cmax in Lewis rat at 0.1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID660662Stability of the compound in presence of enterobacteria from rat cecal contents under anaerobic condition at 3 to 30 uM after 48 hrs2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648601Terminal half life in C57BL/6J mouse at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648593Terminal half life in Lewis rat at 0.1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID660665Drug metabolism in po dosed rat plasma assessed as formation of 4-phenoxy benzoic acid2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID660639Immunosuppressive activity in po dosed LEW rat transplanted with spleen cells of WKAH rat assessed as inhibition of enlargement of draining popliteal lymph node administered qd for 4 days2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648590Antimultiple sclerosis activity in C57BL/6J mouse assessed as reduction of experimental autoimmune encephalomyelitis score at 1 mg/kg, po qd for 23 days2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648589Antimultiple sclerosis activity in C57BL/6J mouse assessed as reduction of experimental autoimmune encephalomyelitis score at 0.3 mg/kg, po qd for 23 days2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648582Agonist activity at human S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID645222Selectivity ratio of EC50 for human S1P3 receptor to EC50 for human S1P1 receptor2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
AID648608Agonist activity at human S1P5 receptor2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID660636Agonist activity at human S1P1 receptor by [S35]GTPgammaS binding assay2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648596Tmax in Lewis rat at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648588Antiarthritic activity in po dosed Lewis rat assessed as reduction of adjuvant-induced right hind foot volume administered as qd for 18 days2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648580Agonist activity at rat S1P3 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID660663Stability of the compound in presence of enterobacteria from monkey feces contents under anaerobic condition at 3 to 30 uM after 48 hrs2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648592Tmax in Lewis rat at 0.1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648583Selectivity ratio of EC50 for human S1P3 receptor to EC50 for human S1P1 receptor2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID660660Stability of the compound in presence of enterobacteria from rat cecal contents under anaerobic condition at 3 to 30 uM after 24 hrs2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648602AUC (0 to 72 hrs) in C57BL/6J mouse at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648579Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells assessed as induction of GTPgammaS binding2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID645223Immunosuppressive activity in po dosed LEW rat model assessed as inhibition of WKAH rat spleen cells-induced popliteal lymph node swelling administered qd for 4 days measured at day 4 by host versus graft reaction analysis2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
AID648604Drug metabolism in po dosed monkey plasma assessed as 4-PBA level2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648607Agonist activity at human S1P4 receptor2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648585Immunomodulatory activity in Lewis rat assessed as decrease in peripheral blood lymphocyte numbers at 0.1 mg/kg, po after 8 hrs relative to control2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648600Tmax in C57BL/6J mouse at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648605Metabolic stability in liver microsomes assessed as 4-PBA level2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648587Immunomodulatory activity in Lewis rat assessed as decrease in peripheral blood lymphocyte numbers at 0.1 to 1 mg/kg, po after 24 to 48 hrs2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID660637Agonist activity at human S1P3 receptor by [S35]GTPgammaS binding assay2012Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9
Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.
AID648606Metabolic stability in liver microsomes assessed as degradation of 1,2,4-oxadiazole ring2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID645221Agonist activity at human S1P3 receptor assessed as stimulation of [35S]GTPgamma binding2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
AID648594AUC (0 to 72 hrs) in Lewis rat at 0.1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID648586Immunomodulatory activity in Lewis rat assessed as decrease in peripheral blood lymphocyte numbers at 1 mg/kg, po after 8 hrs relative to control2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
AID645220Agonist activity at human S1P1 receptor assessed as stimulation of [35S]GTPgamma binding2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Discovery of CS-2100, a potent, orally active and S1P3-sparing S1P1 agonist.
AID648597Terminal half life in Lewis rat at 1 mg/kg, po2012European journal of medicinal chemistry, May, Volume: 51Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's4 (66.67)24.3611
2020's2 (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: 34.42

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

MetricThis Compound (vs All)
Research Demand Index34.42 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index49.59 (26.88)
Search Engine Supply Index2.43 (0.95)

This Compound (34.42)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]