A novel potent, slow tight binding LPA1 receptor antagonist with IC50 of 86 nM, Kd of 0.34 nM.

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

A potent, selective S1P3 antagonist with Ki of 0.25 nM.

A synthetic immunosuppressant that functions as a S1P1 receptor agonist.

AD 2900 (AD2900, AD-2900) is a novel potent, broad S1P receptor antagonist with IC50 of 3.8, 3.2, 6.2, 5.9 and 0.405 uM for S1P1, 2, 3, 4 and 5 respectively.

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

AM966 is a high affinity, selective, oral LPA1 (lysophosphatidic acid receptor, IC50=17 nM) antagonist, with selectivity for this receptor over the other LPA receptors.

BMS-986020 is an LPA1 antagonist.

BMS-986202 is a clinical Tyk2 inhibitor that binds to Tyk2 JH2 with IC50 of 0.19 nM and shows remarkably selectivity over other kinases including Jak family members.

Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM.

CYM-5442 is a highly-selective S1P1 (Spingosine 1-Phosphate Receptor 1) agonist.

Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1(S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.

Fingolimod(FTY720 free base) is a S1P antagonist with IC50 of 0.033 nM.

Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6.

Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6.

ONO-7300243 is a novel, potent LPA1(Lysophosphatidic Acid Receptor) antagonist with an IC50 of 160 nM.

Ozanimod (RPC1063) is a selective S1P1R modulator

Ponesimod(ACT-128800) is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.

S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2.

SAR-100842 (SAR100842) is a potent, selective, orally available antagonist of the Lysophosphatidic Acid 1 Receptor (LPA1 receptor) with IC50 of 31 nM in β-arrestin assays.

SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2.

TAK-615 (TAK615) is a potent, selective, negative allosteric modulator (NAM) of the LPA1 receptor, partially inhibits the LPA response with IC50 of 91 nM (60% at 10 uM) in calcium mobilisation assays..

CYM5541 is a selective sphingosine-1-phosphate receptor 3 (S1P3) allosteric agonist (EC50 = 72-132 nM).

Ceralifimod is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.

BAF312 is a potent and selective agonist of S1P with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively

GSK-2018682 is a sphingosine 1 phosphate receptor (S1PR)-1 agonist potentially for the treatment of multiple sclerosis.

CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R.

CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.

LPA2 antagonist 2 (H2L 5226501) is a selective LPA2 antagonist with an IC50 of 28.3 nM, which is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM).

1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant LPA species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation. 1-Oleoyl lysophosphatidic acid increases SRE-drivenβ-galactosidase activity.

H2L 5765834 is an antagonist of lysophosphatidic acid receptors LPA1, LPA3, and LPA5, with IC50s of 94, 752, and 463 nM respectively.

Vibozilimod (example 33) is a S1p1 receptor agonist (extracted from patent WO2012140020A1).

Zectivimod is a sphingosine-1-phosphate receptor agonist. Zectivimod can be used for the research of autoimmune diseases, chronic inflammatory diseases and immunoregulation disorders.

ALESIA is a specific sphingosine-1-phosphate receptor 3 (S1PR3)-G12-biased agonist and selectively induces G12 signal.ALESIA promotes nitric oxide production and oxidative stress.ALESIA selectively induces apoptosis in cancer cells because of low glucose levels.Intraperitoneal administration of ALESIA improved the survival of mice with peritoneally disseminated rhabdomyosarcoma.ALESIA (Anticancer Ligand Enhancing Starvation-induced Apoptosis) is a new anticancer compound for glucose starvation therapy.

GSK-1842799 is a potent, selective, oral bioavailable S1P1 agonist with bind affinity of 0.52 nM; displays an excellent selectivity (>3,000-fold) for S1P1 over S1P3; significantly reduces blood lymphocyte at 3 mg/kg, achieves efficacy equivalent to FTY720 in the mouse EAE model of MS.

S1P5-IN-15 is a potent, selective, orally active and brain-penetrant S1P5 antagonist with IC50 of 0.1 nM, no effect on S1P1-4.

ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.

ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively.

IMMH002 is a potent, selective and orally active S1P1 agonist, IMMH002 can be transformed to IMMH002-P in vivo, IMMH002-P activates S1P1, S1P4, and S1P5 with 12.4, 19.8 and 29.4 nM respectively.

JTE-013 (JTE013) is a potent, specific S1P2 receptor (Edg-5) antagonist with IC50 of 17 nM and 22 nM for human and rat S1P2, respectively.

NXC736 hydrochloride (SLB736) is a selective functional antagonist for type 4 sphingosine-1-phosphate receptor (S1PR4), has immunomodulatory and anti-fibrotic effects.

SLB1122168 is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM.

SLB1122168 hydrochloride is a potent, specific inhibitor of S1P transporter spinster homologue 2 (Spns2), inhibits Spns2-mediated S1P release with IC50 of 94 nM.

TP0541640 (TP 0541640) is a novel potent LPA1 antagonist with IC50 of 1.6 nM, shows potential for the treatment of lung and skin fibrosis.

UCM-14216 (UCM14216) is a potent and selective antagonist of type 2 lysophosphatidic acid receptor (LPA2) with KD value of 1.3 nM and IC50 of 1.9 uM.