NV930 is a small molecule inhibitor of tRNA-specific 2′-O-methyltransferase (FTSJ1), exerts readthrough activity in vitro and in vivo.

NVS1.1 is a potent readthrough promoter, promotes the rapid and specific degradation of eukaryotic release factor 1 (eRF1) and restores functional full-length proteins in cystic fibrosis and Hurler disease models.

Opabactin is an abscisic acid (ABA) mimic and agonist Arabidopsis subfamily III/II ABA receptors with nanomolar potency (7 nM).

Ophiopogonin-D (OP-D) is one of steroidal saponins isolated from the root of the Chinese medicinal plant Ophiopogon japonicas, possesses anti-inflammatory and anti-oxidant properties.

Org 214444-0 is a highly potent, selective, allosteric agonist of follicle stimulating hormone receptor (FSHR) with EC50 of 2.0/1.2 nM (human/rat FSHR) in cell-based assays.

OSM-SMI-10B (SMI-10B) is a first-in-class small molecule inhibitor binds to oncostatin M (OSM) with Kd of 13.6 uM, significantly reduces OSM-induced STAT3 phosphorylation in cancer cells.

OV329 (OV 329) is a highly potent inactivator of gamma-aminobutyric acid aminotransferase (GABA-AT) with Ki of 9.69 uM.

PAANIB-1 is a brain-penetrant PAAN/MIF nuclease inhibitor that prevents neurodegeneration that prevents neurodegeneration induced by α-syn PFF, AAV-α-syn overexpression, or MPTP intoxication in vivo.

Panx-1 blocker 15b is a large-pore channel pannexin 1 (Panx1) inhibitor with IC50 of 0.8 uM.

PAT1inh-A0030 is a potent and selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor with IC50 of 1.0 uM, shows no activity on relevant ion transporters/channels (SLC26A3, SLC26A4, SLC26A9, CFTR, TMEM16A).

PAT1inh-B01 is a small-molecule, selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor, could fully inhibit PAT1-mediated anion exchange with IC50 of 350 nM.

PCC0105003 is a small molecule microtubule affinity-regulating kinases (MARKs) inhibitor with IC50 of 3.0, 2.0, 2.67 and 2.67 nM for MARK1, 2, 3 and 4 repectively.

PCiB-1 is a small molecule inhibitor capable of inhibiting phosphatidylcholine (PC) biogenesis with IC50 of 7.0 uM, inhibits phosphatidylethanolamine (PE) transport from mitochondria to the endoplasmic reticulum (ER), induces mitochondrial division.

PCiB-2 is a small molecule inhibitor capable of inhibiting phosphatidylcholine (PC) biogenesis with IC50 of 2.0 uM, inhibits the phosphatidylethanolamine (PE) methyltransferase activity of Cho2, induces mitochondrial division.

PCiB-3 is a small molecule inhibitor capable of inhibiting phosphatidylcholine (PC) biogenesis with IC50 of 0.4 uM, inhibits the phosphatidylethanolamine (PE) methyltransferase activity of Cho2.

PDDC is the first potent, selective, orally-available, and brain-penetrable nSMase2 (neutral sphingomyelinase 2) inhibitor with pIC50 of 6.57.

PEPCKi is a small molecule inhibitor of hosphoenolpyruvate carboxykinase (PEPCK), blocks lactate utilization and impairs tumor growth in colorectal cancer.

PF-07208254 (PF 07208254) is a potent, allosteric branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor with in vitro IC50 of 110 nM and Ki of 54 nM.

PF-07247685 (PF-07247685) is a potent, allosteric branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor with in vitro IC50 of 0.86 nM, and SPR Kd of 0.68 nM.

PFKL activator NA-11 is a small-molecule, selective PFKL activator, inhibits the NOX2-dependent oxidative burst in neutrophils by activating the glycolytic enzyme phosphofructokinase-1 liver type (PFKL).

Pixatimod (PG545) is a heparan sulfate (HS) mimetic and anticancer agent and a potent inhibitor of heparanase.

PPA-904 is a specific phenothiazine photosensitizer in photodynamic therapy (PDT) research, especially topical application for cutaneous leishmaniasis in vivo.

Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.

PRG-A01 is a chemical inhibitor against SOD1 misfolding and aggregation, inhibits the neuronal cell death caused by mutant-SOD1 overexpression.

PSB-22034 is a potent, selective agonist of MAS-related Gq protein-coupled receptor X4 (MRGPRX4) with EC50 of 11.2 nM/32.0 nM in Ca2+ assay/β-arrestin assays (variant 83S), respectively.

PSB-22040 is a potent, selective agonist of MAS-related Gq protein-coupled receptor X4 (MRGPRX4) with EC50 of 19.2 nM/30.0 nM in Ca2+ assay/β-arrestin assays (variant 83S), respectively.

PSB-CB-148 is a potent, selective antagonist of GPR18.

PSB-CB-27 is a potent, selective antagonist of GPR18 with IC50 of 650 nM, shows no inhibition on GPR55 and low affinity for CB1/CB2 receptors.

PSB-KK-1415 is a selective GPR18 agonist with EC50 of 19.1 nM (hGPR18) in β-arrestin recruitment assays, shows no activity against GPR55.

PT91 is a small-molecule GPR27 (SREB1) agonist with pEC50 of 6.15 (human GPR27) in β-arrestin 2 recruitment-based firefly luciferase complementation assay, Emax=100%.

PTI-125 (Simufilam, Sumifilam) is a small molecule targeting scaffolding protein filamin A (FLNA), preferentially binds altered FLNA and restores its native conformation.

PXS-4748 (PXS4748) is a potent, selective and irreversible pan-lysyl oxidase (pan-LOX) inhibitor with IC50 of 2.0 uM and 3.2/0.6/1.4/0.2 uM for bovine (aorta) LOX and rh LOXL1/2/3/4, respectively.

PXS-5129A is the pro-drug form of PXS-5120A, a potent, selective, irreversible inhibitor of Lysyl oxidase-like 2 (LOXL2).

PXS-5505 dihydrochloride monohydrate is an orally available, small-molecule, irreversible inhibitor of all lysyl oxidases (pan-LOX) family members, with potential antifibrotic activity.

PXS-6302 (PXS6302) is a potent, irreversible pan-lysyl oxidase (pan-LOX) inhibitor with IC50 of 3.7 uM and 3.4/0.4/1.5/0.3 uM for bovine (aorta) LOX and rh LOXL1/2/3/4, respectively.

Pyrcoumin is a competitive inhibitor of dCTP pyrophosphatase 1 (dCTPP1, IC50=3.3 uM), inhibits Wnt signaling with IC50 of 8.4 uM in SuperTOPFlash reporter gene assays.

QP5038 is a potent inhibitor of glutaminyl-peptide cyclotransferase-like protein (QPCTL) with IC50 of 3.8 nM, shows promising in vitro and in vivo anti-tumor efficacies.

R805 is a small molecule modulator of gp130 receptor pro-inflammatory signaling, targets a signaling tyrosine 814 (Y814) within gp130, modulates gp130 Y814 upstream of the SRC and MAPK circuit, elicits a protective effect on tissues after injury.

RA 5557 is a brain-penetrant, selective, oral UGT8 inhibitor, inhibits galactosylceramide biosynthesis.

RBS-10 is a small molecule that shows preferential cytotoxicity against cells pan-resistant to degraders, acts as a prodrug bioactivated by the oxidoreductase enzyme NQO1.

RECTAS is a small molecule splice modulator that corrects aberrant splicing of familial dysautonomia (FD), promotes exon 20 inclusion of IKBKAP pre-mRNA and expression of IKAP.

RF03176 is a selective AQP9 inhibitor with IC50 of 1.3 uM (inhibition of CHO-AQP9 cell water permeability).

RG100204 is a novel selective, small molecule inhibitor of the neutral solute channel Aquaporin 9 (AQP9), inhibits AQP9 water permeability (IC50=110 nM) and AQP9 glycerol permeability (IC50=76 nM).

Ro 48-8071 is a potent 2,3-oxidosqualene cyclase (OSC) inhibitor with IC50 of 6.5 nM.

RPE65-61 ((±)-RPE65-61) is a selective, non-retinoid and uncompetitive inhibitor of RPE65 (a key enzyme in the visual cycle), inhibits the retinol isomerase activity of RPE65 in vitro with IC50 of 80 nM.

RPI-194 is a novel troponin activator that binds to cardiac/slow skeletal muscle troponin, binds to cardiac troponin with KD of 24 uM, stabilizing the activated complex between troponin C and the switch region of troponin I.

RTI-263 (SerPheLysAsn-NH2) is a potent, selective tetrapeptide neuropeptide S receptor (NPSR, GPR154) biased agonist with EC50 of 3.02 nM for hNPSR calcium mobilization.

RU-NT-206 is a small molecule inhibitor targeting the P-stalk binding pocket of ricin toxin A subunit (RTA) with IC50 of 7 uM, inhibits catalytic activity and protects cells against ricin and Stx2 holotoxins.

RX-105 (RX105) is a small molecule inhibitor of protein interaction with glycosaminoglycans (SMIGs) with anti-inflammatory properties, binds directly to glycosaminoglycans (GAGs).

RX-207 (RX207) is a small molecule inhibitor of protein binding to glycosaminoglycans (SMIGs), inhibits protein binding to glycosaminoglycans (GAGs), inhibits inflammatory neutrophil adhesion and activity in vitro and in vivo.

S-181 (S 181) is a specific small-molecule activator (modulator) of β-glucocerebrosidase (GCase) with AC50 of 1.49 uM and a maximum activation of 780%.

S202 is a potent, selective and brain-penetrant small molecule inhibitor of ceramide galactosyltransferase (CGT) with IC50 of 15 nM in the cell-lysate assays and 3.6 nM in intact-cell assays.

S9-A13 is a highly potent and specific inhibitor of SLC26A9, potently inhibits SLC26A9-mediated Cl−/I− and Cl−/SCN− exchange activities with IC50 of 90.9 and 171.5 nM, respectively.S9-A13 does not inhibit other members of the SLC26 family and has no effects on Cl− channels such as CFTR, TMEM16A, or VRAC.S9-A13 (0-1 uM ) inhibits SLC26A9 currents in a dose-dependent manner in HEK293 cells, but shows little effects on CFTR currents in HEK293 cells at the highest concentration (5 uM).S9-A13 has a minor effect on ion transport in human airway epithelial cells and mouse trachea, despite clear expression of SLC26A9 in the apical membrane of ciliated cells.

SACLAC is an α-chloroamide ceramide analog that binds irreversibly to acid ceramidase (ASAH1), significantly reduces the viability of AML cells (EC50=3 uM) across 30 human AML cell lines.

SAN4825 is a selective small-molecule inhibitor of cardiac ADP-ribosyl cyclase (ADPR cyclase) with IC50 of 0.13 uM.

SAR439883 (SAR 439883) is a novel potent, selective, orally active PKR inhibitor with IC50 of 0.68/0.69 uM against hPKR/mPKR, respectively.

SB1501 (SB 1501) is a bioactive compound that reduces fat accumulation by elevating mitochondrial biogenesis and fatty acid oxidation via the PGC-1α-UCP1 pathway, shows anti-obesity effects in vivo.

SBI-0802936 (SBI 0802936) is an analog of SMIP004-7, inhibits NADH:ubiquinone oxidoreductase (complex I), 4-6 times more potently than SMIP004-7, acting in the same uncompetitive fashion as SMIP004-7.

SBL-105 (SBL105) is a potent, selective DHODH inhibitor with IC50 of 48.48 nM (rh DHODH).

SB-U015 is a MitoQ derivative and tumor necrosis factor receptor-associated protein 1 (TRAP1) inhibitor.

SC-919 (SC919) is a potent, selective inhibitor of IP6K (Inositol hexakisphosphate kinase) with IC50 of <5.2, <3.8 and 0.65 nM for human IP6K1/2/3, respectively.

Secdin is a small-molecule inhibitor of Arabidopsis thaliana ADP-ribosylation factor (ARF)-guanine nucleotide exchange factors (GEFs), impaires both hypocotyl and root growth in young Arabidopsis seedlings with IC50 of 4 uM.

Seletracetam (ucb 44212) is a high affinity for the synaptic vesicle protein 2A (SV2A) than levetiracetam with 10-fold, exhibits anticonvulsant properties in animal models of epilepsy.

SFI003 is novel serine/arginine-rich splicing factor 3 (SRSF3) inhibitor, inhibits the proliferation and migration of CRC cells, inhibits the proliferation of HCT-116 with IC50 of 8.78 uM.

SHR170008 is a highly potent, small molecule CD73 inhibitor with IC50 of 0.05 nM against human CD73 soluble enzyme.

A potent small-molecule inhibitor of steroid receptor coactivator-3 (SRC-3 or AIB1) that can selectively inhibit the intrinsic transcriptional activities of SRC-3, also inhibits SRC-1 and SRC-2.

Siastatin B is a potent and effective iminosugar inhibitor of diverse glycosidase classes, namely, sialidases, β-d-glucuronidases, and N-acetyl-glucosaminidases.

SJ572946 is a small molecule BAK activator, binds to the activation groove of BAK and selectively triggers BAK activation over that of BAX in liposome and mitochondrial permeabilization assays.

SMC-21598 is a specific small molecule CCL18 antagonist, binds with high-afnity on the CCL18 protein in 1:1 stoichiometry with ITC KD value of 600 nM, blocks the binding of CCL18 with its receptor PITPNM3.

SMIP004-7 is a small molecule inhibitor of mitochondrial respiration with selective in vivo anti-cancer activity, targets drug-resistant cancer cells with stem-like features by inhibiting NADH:ubiquinone oxidoreductase (complex I).

SN34960 is a small molecule Perforin inhibitor, inhibits perforin-induced lysis of Jurkat T-lymphoma cells with IC50 of 6.65 uM, shows suboptimal physicochemical properties and toxicity toward the natural killer (NK) cells that secrete perforin in vivo.

SP-8008 is a potent, selective inhibitor of shear stress-induced platelet aggregation (SIPA) with IC50 of 1.44 uM, effectively and broadly blocks SIPA events and attenuates platelet activation and aggregation.

SPI-0324 (SPI-24) is a small molecule Spt5-Pol II complex inhibitor (SPI), selectively lowers mutant huntingtin gene (Htt) mRNA level with IC50 of 0.52 uM, without affecting WT Htt.

SPI-1477 (SPI-77) is a small molecule Spt5-Pol II complex inhibitor (SPI), selectively lowers mutant huntingtin gene (Htt) mRNA level with IC50 of 0.1 nM, without affecting WT Htt.

SPI-21 (Spt5-Pol II inhibitor 21) is a small-molecule inhibitor of Spt5-Pol II with IC50 of 25.2 uM.

SpiD7 is a spirocyclic dimer compound that activates the unfolded protein response (UPR), selectively inhibits growth and induce apoptosis of cancer cells.

A potent, small molecule nuclear receptors REV-ERBα/β agonist with IC50 of 670/800 nM, respectively.

SRP-001 is a non-opioid and non-hepatotoxic small molecule ApAP analog, induces analgesia via N-arachidonoylphenolamine (AM404) formation, and generates higher amounts of AM404 than ApAP.

SS-1-148 is a potent, selective inhibitor of human ornithine δ-aminotransferase (hOAT) with Ki of 60 uM, shows excellent selectivity over other related aminotransferases (e.g., GABA-AT).

SST0871AA1 is a small molecule Heparanase (Hpse) inhibitor with IC50 of 0.64 uM.

SST0872AA1 is a potent, small molecule Heparanase (Hpse) inhibitor with IC50 of 0.08 uM.

STF-1084 (STF1084) is a potent, cell impermeable, specific, stable, and non-toxic ENPP1 inhibitor with Ki,app of 110 nM (in vitro 32P-cGAMP TLC assay), and cellular IC50 of 340 nM.

STOCK1S-14279 (Stock 1S-14279) is a specific small-molecule SPAK kinase (STK39) inhibitor with IC50 of 0.26 uM, inhibits SPAK-regulated phosphorylation and activation of NCC and NKCC1.

Succinyl phosphonate is an α-Ketoglutarate phosphoanalogue, α-ketoglutarate dehydrogenase inhibitor, effectively inhibits α-ketoglutarate oxidative decarboxylation.

SW088799 is a small molecule glucagon release inhibitor with IC50 of 1.26 uM, with minimal impact on insulin release.

SYNTi is a small molecule PDZ domain inhibitor targeting the syndecan/syntenin protein-protein interaction with IC50 of 400 nM.

Synucleozid hydrochloride (NSC 377363) is a small molecule that targets the IRE structure and inhibits SNCA gene translation in cells, directly targets the α-synuclein mRNA 5'UTR at the designed site.

TH301 (TH 301) is a selective small molecule stabilizer of Cryptochrome 2 (CRY2). KL101 showed selectivity over CRY1, and no or only minor effects on CKIδ, CKIα and CK2 activities in vitro.

TH8535 (TH-8535) is a potent, selective inhibitor of 8-oxo Guanine DNA Glycosylase 1 (OGG1) with IC50 of 0.2 uM.

TMX-4084 (TMX4084) is a highly potent, selective PIP4K2C binder with KD of 7.3 nM, shows no affinity for PIP4K2B and PIP4K2A (KD>10 uM).

TMX-4102 (TMX4102) is a highly potent, selective PIP4K2C binder with KD of 0.45 nM, shows no affinity for PIP4K2B and PIP4K2A (KD>10 uM).

TOP5300 (TOP05300) is a potent, selective, orally active allosteric agonist of follicle stimulating hormone receptor (FSHR) with EC50 of 9.72 nM, 80-fold selectivity over hLHR.

TOP5668 (TOP05668) is a potent, selective, orally active allosteric agonist of follicle stimulating hormone receptor (FSHR) with EC50 of 2.2 nM, 80-fold selectivity over hLHR.

Tpm1.8/9-1 (CID 6494468) is a specific small molecule inhibitor of Tpm1.8/9, antagonizes Tpm1.8/9's effects on EMT, Wnt signaling, and resistance to chemotherapy.

Tpm1.8/9-3 (CID 18973468) is a specific small molecule inhibitor of Tpm1.8/9, antagonizes Tpm1.8/9's effects on EMT, Wnt signaling, and resistance to chemotherapy.

TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.

trans-MiM111 is a small molecule short acting mitofusin activator, increases mitochondrial motility in MFN2 T105M expressing mouse DRGs with EC50 of 3.6 nM (Emax=93).

Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive

TTFB (ZAC antagonist TTFB) is a selective antagonist (negative allosteric modulator) of Zinc-Activated Channel (ZAC) with IC50 of 3 uM.

TXX-1-10 (CB1-8) is a small chemical molecule that inhibits HPIP oncoprotein expression, suppresses breast cancer cell growth and metastasis in vitro and in vivo.

UAB126 (UAB 126) is a novel rexinoid-like small molecule that show positive effects on metabolic syndrome without the known side effects of potent rexinoids.

UbV SP.1 is potent, selective inhibitor of STAMBP isopeptidase activity with KD of 0.05/0.18 uM for STAMBP/STAMBPL1, respectively.

UbV SP.3 is potent, selective inhibitor of STAMBP isopeptidase activity with KD/IC50 of 60/9.8 nM, with significant preferential binding to STAMBP over STAMBPL1 (250 -fold selectivity).

UNC10245131 (UNC 10245131) is a potent, selective cyclic peptide inhibitor of calcium and integrin binding protein 1 (CIB1) with ITC Kd of 6.17 nM.

UNC10245351 is a N-terminal HIV Tat conjugate to UNC10245092, a CIB1 peptide inhibitor (Kd=192 nM), cell-penetrating.

UNC2383 (UNC-2383) is a small molecule that enhances the intracellular delivery and pharmacological effectiveness of antisense oligonucleotides (ONs) and splice switching oligonucleotides (SSOs).

UNC4850 (UNC-4850) is a specific small-molecule inhibitor toward CDY Chromodomain CDYL1/2 with Kd of 0.47/0.42 uM, >10-fold selectivity over CDY1, CBX5 and CBX7.

UNC5452 is a selective NIMA-related kinase 1 (Nek1) inhibitor with IC50 of 4.3 uM.

UNC-CA157 is a selective small molecule inhibitor of the archetypal UbiB member COQ8A with IC50 of 580 nM, shows clear preference for COQ8A over COQ8B.

UT-59 is a specific inhibitor of cholesterol-sensing membrane protein Scap, binds to Scap's cholesterol-binding site, blocks SREBP activation and inhibits lipid synthesis.

UTBinh-14 is a potent, highly selective inhibitor for urea transporter UT-B with IC50 of 11 nM, with over a thousand-fold selectivity over UT-A.

VJDT (TREM1 inhibitor) is a novel small molecule inhibitor of triggering receptor expressed on myeloid cell 1 (TREM1), effectively blocks TREM1 signaling.

WX-02-37 is a selective, allosteric and covalent inhibitor of sterile alpha toll/interleukin receptor motif containing-1 (SARM1) with IC50 of 1.5 uM, site-specifically and stereoselectively modify cysteine-311 (C311) in the noncatalytic, autoregulatory ar

XEN 602 (XEN602) is a potent, specific divalent metal transporter 1 (DMT1) inhibitor that inhibits Mn incorporation in HEK293 cells with IC50 of 0.3 nM.

X-Neu5Ac (sodium) is a substrate for chromogenic assay of neuraminidase activity in bacterial expression systems; with a Km of 0.89 mM for neuraminidase.

XST-20 is a small molecule selectively targeting FOXM1 DNA-binding domain (DBD) with SPR Kd of 20 uM, effectively suppresses FOXM1 transcriptional activities and inhibits ovarian cancer cell proliferation.

YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).

YE6144 (YE 6144) is a specific small molecule inhibitor of transcription factor IFN regulatory factor 5 (IRF5), selectively suppresses IRF5 activity through inhibition of IRF5 phosphorylation.

YL-365 (YL365) is a highly potent, selective and competitive antagonist of GPR34.

Z839878730 (KK-LC-1 inhibitor Z8) is a small moelcuel compound targeting KK-LC-1, which is significantly highly expressed in triple-negative breast cancer tissues than in normal breast tissues.

ZHAWOC8697 is a small molecule dual inhibitor of sentrin-specific protease SENP1 and SENP2 with IC50 of 8.6 and 2.3 uM, respectively, a valuable tool for the study of SUMOylation processes.

ZINC13407541 is a small molecule antagonist for FGF23, inhibits FGF-23 signaling with IC50 of 0.45 uM.

ZINC16991592 is a selective MRGPRX2 antagonist with Ki of 189 nM.

ZYF0033 (ZYF 0033) is potent, selective, small-molecule inhibitor of HPK1 with IC50 of <10 nM based on the phosphorylation inhibition of MBP protein.

ψTnI (Peptide DWRKNIDA) is a selective, high-affinity, eight amino acid peptide inhibitor of cardiac troponin I (cTnI), directly binds to δPKC with high affinity (Kd=5 nM) and inhibits cTnI/δPKC interaction.

AdipoAI is a novel small molecule APN receptor (AdipoR, adiponectin receptor) agonist.

ALY688 (ADP 355) is an adiponectin mimetic adiponectin receptor (AdipoR) agonist, inhibits the growth of AdipoR1/AdipoR2-positive cancer cell lines (MCF-7 cell, 0.1-10 uM).

K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.

Wyeth-1 (hAMCase inhibitor 1) is a potent, selective inhibitor of human acidic mammalian chitinase (hAMCase) with IC50 of 210 nM, 20-fold selectivity over hCHIT1.

DL5050 (DL 5050) is a potent selective agonist of human constitutive androstane receptor (CAR) with EC50 of 0.37 uM in cell-based luciferase reporter assays (Emax=3.8).

DL7076 (CN06) is a small molecule dual activator of the constitutive androstane receptor (CAR, NR1I3) and nuclear factor erythroid 2-related factor 2 (Nrf2) with EC50 of 8.85 and 0.72 uM, respectively.

BVT173187 is a potent, selective, non-peptide inhibitor of formyl peptide receptor 1 (FPR1), inhibits fMLF and WKYMVM induced oxidase activity.

ICT12035 (AZ2158) is a potent, selective formylpeptide receptor-1 (FPR1) antagonist with IC50 of 30 nM in calcium mobilisation assays (100 nM fMLF).

MD102 is a potent transglutaminase 2 (TGase 2; TG2) inhibitor with IC50 of 0.35 uM, shows p53 stabilization effect and anticancer activity at RCC cell lines.

ZED1227 is a potent, selective, covalent, and orally active transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 45 nM.

LJ4827 (LJ-4827) is a potent, specific inhibitor of HASPIN, a mitotic kinase for Histone H3, with Ki value of 0.46 nM, enzyme IC50 of 0.155 nM in HASPIN kinase assay performed with Histone H3 peptide.

AG-120-X is a first-in-class small molecule inhibitor of ICOS/ICOSL interaction with IC50 of 4.68 uM in TR-FRET assay, dose-dependently blocks ICOS/ICOSL interaction in cellular assay based on co-culturing Jurkat T cells expressing ICOS and CHO-K1 cells e

C-5401331 is a small molecule T-cell immunoglobulin and mucin domain-containing protein 3 (Tim-3) inhibitor, suppresses acute myeloid leukemia (AML) cell proliferation.

L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.

MTX-3937 is a small-molecule Siglec-9 inhibitor with binding KD of 3.15 uM in BLI assay, inhibits phosphorylation of Siglec-9 and downstream SHP1 and SHP2.

ARUK3001185 is a potent, selective, brain-penetrant inhibitor of Wnt-deactivating enzyme Notum carboxylesterase activity with IC50 of 6.7 nM in OPTS biochemical assay.

LP-914822 (LP914822) is a potent, selective and orally-active NOTUM with IC50 of 2 nM for human, mouse and rat Notum.

LP-935001 (LP935001) is a potent, selective and orally-active NOTUM with enzyme IC50 of 0.4 nM for both of human and mouse Notum.

AS-48 is a specific, small-molecule measles virus (MeV) entry inhibitor with IC50 of 0.6 uM agianst MV-KS.

MBZM-N-IBT is a small molecule inhibitor of Chikungunya virus (CHIKV), inhibits CHIKV infection in vitro in RAW 264.7 cells with IC50 of 22.34 uM, targets CHIKV nsP2 protease activity.

SBI-0090799 (SBI 0090799) is a selective and potent inhibitor of Zika virus (ZIKV) replication, inhibits replication of multiple ZIKV strains and in different cell systems.

UMM-766 is an orally available nucleoside analog with potent, broad-spectrum antiviral activity against multiple members of orthopoxviruses (EC50<1 uM against VACV).

USC-373 is a phosphonate prodrug of HPMPC (cidofovir) with activity against VZV and other DNA viruses.

EOS789 is a potent, pan-phosphate transporter inhibitor, inhibits phosphate uptake in a noncompetitive manner for human NaPi-IIb, PiT-1, and PiT-2 with IC50 of 6.8, 1.5 and 1.7 uM, respectively.

EOS789 tosylate is a potent, pan-phosphate transporter (NaPi-2b, PiT-1, PiT-2) inhibitor, inhibits phosphate uptake in a noncompetitive manner for human NaPi-IIb, PiT-1, and PiT-2 with IC50 of 6.8, 1.5 and 1.7 uM, respectively.

LY3358966 is a potent, selective inhibitor of the intestinal sodium-dependent phosphate cotransporter NPT2b (NaPi-2b, SLC34A2), inhibits phosphate uptake in human NPT2b expressed in CHO cells with IC50 of 32.4 nM.

TY-2136 is a next generation ROS1/TRK/ALK inhibitor with IC50 of 1.6 nM and 460.1 nM for ROS1 G2032R and TRKA G595R, respectively, inhibits ROS1/TRK/ALK mutations and overcomes drug resistance due to acquired solvent-front mutations.

1D-142 is a novel small molecule RHO family of GTPase RAC1 inhibitor, inhibits Rac1-GEF interaction and reduces Rac1-mediated TNFα-induced NF-κB nuclear translocation during cell proliferation and migration.

CS7171 is an effective, blood-brain barrier (BBB) permeable small molecule inhibitor of hippocampal Rac1 activity, rescues learning deficits in APP/PS1 mice.

GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.

JKF-034 is an effective,blood-brain barrier (BBB) permeable small molecule inhibitor of hippocampal Rac1 activity, rescues learning deficits in APP/PS1 mice.

PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.

BAY 2686013 is a selective, allosteric antagonist of human pituitary adenylate cyclase activating polypeptide receptor (hPAC1-R) with IC50 of 0.92 and 0.4 uM in cAMP HTRF and Ca2+ release assays, respectively.

PA-915 (PA915) is a small-molecule, non-peptide antagonist of the PACAP type I (PAC1) receptor, inhibits PACAP (1 nM)-induced phosphorylation of CREB in PAC1/CHO cells with IC50 of <10 pM.

Ro 25-1553 is a potent, selective VIPR2 agonist and a cyclic peptide analog of vasoactive intestinal peptide (VIP), displaces the radioligand 125I-VIP from rat forebrain membranes with IC50 of 4.98 nM.

Zenuzolac (GLS1027, VGX-1027) is a small molecule immunosuppressant and an orally available isoxazole compound, inhibits toll-like receptor 4 (TLR4) activity, has shown promise for the treatment of several neuroinflammatory disorders.