HQY426 is a specific, orally bioavailable inhibitor of pre-messenger RNA endonuclease cleavage and polyadenylation specificity factor 3 (CPSF3) with binding IC50 of 0.32 uM, exhibits potent antitumor activity.

HQY436 is a specific, orally bioavailable inhibitor of pre-messenger RNA endonuclease cleavage and polyadenylation specificity factor 3 (CPSF3) with binding IC50 of 0.15 uM, exhibits potent antitumor activity.

HsClpP activator ZK53 is a potent, selective activator of mitochondrial caseinolytic protease P (HsClpP) with EC50 of 0.22 uM in FI-based protease activity assays, inactive toward bacterial ClpP proteins.

HTL0041178 is a potent GPR52 agonist with EC50 of 27.5 nM (human or rat GPR52).

HTS13286 is a selective AQP9 inhibitor with IC50 of 1.5 uM (inhibition of CHO-AQP9 cell water permeability).

HYGIC is a small molecule that simultaneously induces hypocotyl elongation and thickening via the ethylene signaling pathway activated by endogenous ethylene.

I194496 (I 194496) is a novel potent, selective inhibitor of cystathionine γ-lyase (CSE) inhibitor with IC50 of 0.79 uM.

IBS007125 is a small molecule inhibitor of c-Maf, inhibits multiple myeloma proliferation by targeting cMaf transcriptional activity.

IDE-397 (GSK-4362676, GSK-676) is a potent, selective small molecule methionine adenosyltransferase 2a (MAT2A) inhibitor, displays broad anti-tumor activity across a panel of MTAP-deleted patient-derived xenografts.

IGGi-11 is a first-in-class small molecule inhibitor of non-canonical activation of heterotrimeric G-protein signaling, binds to G-protein α-subunits (Gαi, Gαi3 ITC Kd=4 uM), specifically disrupts their engagement with GIV/Girdin.

IGGi-11me is a specific, cell-active small molecule inhibitor of GIV-dependent G-protein cell signaling, binds to G-protein α-subunits, specifically disrupts their engagement with GIV/Girdin.

IMB0901 is a small molecule myostatin (MSTN) inhibitor that inhibits the MSTN promoter activity, the MSTN signaling pathway, and the MSTN positive feedback regulation.

INH-12 is a selective small-molecule HSD17B12 inhibitor with 70% inhibition of HSD17B12 activity to transform estrone (E1) into estradiol (E2) at 1 uM, reduces the replication of Flaviviridae viruses (HCV, DENV and ZIKV).

InhiTinib is a small molecule that inhibit interferon (IFN)-gamma production (IC50=52.44 nM) and proliferation of primary CD3+ T cells without inducing cell death.

INI-60 (Inhibitor of Nuclear Import-60) is a novel small molecule inhibitor of Kpnβ1-mediated nuclear import with anti-cancer activity.

IOI-214 is a potent inhibitor of LPS-induced inflammatory cytokine production, prevent HF diet-induced NAFLD/MAFLD in vivo.

hPEBP4 inhibitor IOI-42 is a small molecule inhibitor of anti-apoptotic protein hPEBP4, potentiates TNF-α-mediated growth inhibition of MCF-7 breast cancer cells.

IPA (Inhibitor of Priming Activity) is a small-molecule compound that binds Sec18 (Kd=3.84 uM) and blocks SNARE activation, inhibits vacuole fusion at the SNARE priming stage with IC50 of 50 uM.

IP-DNQ (Isopentyl-deoxynboquinone) is a small molecule that selectively kills pancreatic ductal adenocarcinoma cells in an NQO1-dependent manner.

Ipfencarbazone is a substance being developed for the control of weeds such as watergrass in rice, herbicide agent.

IPHBA is a small-molecule inhibitor that suppresses EPAS1-driven IL-31 induction, selectively inhibits TCR-mediated IL-31 induction in murine CD4+ T cells with IC50 of 10.6 uM.

Ironomycin (Ironomycin AM5) is a lysosomal iron-targeting small molecule that reduces the mitochondrial iron load, resulting in the potent disruption of mitochondrial metabolism.

iSB09 is a potent, selective small moelcule abscisic acid (ABA) receptor agonist with HAB1 IC50 value of 316 nM (combined with the engineered CsPYL1 ABA receptor CsPYL15m).

JA310 is a potent, highly selective inhibitor of the mammalian sterile 20-like serine/threonine (MST) family member MST3 (STK24) with ITC KD value of 115 nM.

JBSNF-000028 (JBSNF000028) is a potent, selective, orally bioavailable substrate-analog inhibitor of nicotinamide N-methyltransferase (NNMT) with IC50 of 34 nM, 190 and 210 nM against human, monkey and mouse NNMT, respectively.

JNJ74856665 (JNJ74856665) is an orally available, potent and selective DHODH inhibitor with IC50 values in the subnanomolar range.

JNJ-54302833 (JNJ 54302833) is a potent, selective fatty acid synthase (FASN) inhibitor with IC50 of 28 nM.

JSD26 is a selective S-nitroso-coenzyme A reductase 2 (SCoR2; AKR1A1) inhibitor with Ki of 93 nM, 10-fold selectivity over AKR1B1.

JumOCA peptide (VKELLRRKRGH) is a peptide corresponding to the OCA-B N terminus, membrane-penetrating OCA-B peptide inhibitor.

JumOCA peptide Tat is a a peptide corresponding to the OCA-B N terminus, as C-terminal fusions to the HIV trans-activator of transcription (Tat) protein for membrane permeability.

JYFY-001 is a small molecule copper chelator with moderate selectivity for targeting copper, potently inhibits cancer proliferation.

JYQ-88 is a potent, selective and covalent PARK7 inhibitor with IC50 of 0.13 uM in DiFMUAc assays, 100-fold selectivity over UCHL1 (PARK5, IC50=11.1 uM), covalently modifies the active site Cys106.

K786-4469 is a small molecule inhibitor of anoctamin 1 (ANO1), suppresses cancer metastasis in vitro and in vivo.

Kakeimide is a potent GH3 inhibitor that selectively targets IAA-conjugating GH3 proteins at subnanomolar concentrations in vitro, shows auxin-like activity by inhibiting endogenous IAA catabolism.

Karyostatin 1AKaryostatin 1A is a small molecule inhibitor of importin beta with binding affinity (Kd=0.3 uM), selectively inhibits the importin α/β pathway.

KBP-066 is a potent, selective dual amylin and calcitonin receptor agonist induces an equally potent body weight loss across a broad dose range in obese rats.

KIO-100 (PP-001) is a novel potent, specific small molecule inhibitor of DHODH with IC50 of <4 nM, 150-fold higher potency than leflunomide (IC50 of 650 nM).

KL101 (KL 101) is a isoform-selective small molecule stabilizer of Cryptochrome 1 (CRY1).

A ruthenium complex anticancer agent that is useful for metastatic tumors and cis-platin resistant tumors.

A promising ruthenium anticancer compound that blocks angiogenesis, endothelial cell proliferation and migration stimulated by VEGF or NO donor agent.

KRP-6 is a potent and highly selective macrophage migration inhibitory factor (MIF) ketonase inhibitor with IC50 of 4.31 uM, significantly reduces MIF-induced neutrophil migration.

KS10076 is a metal chelator with potent anti-cancer cytotoxicity, destabilizes STAT3 by elevating ROS, shows remarkable cytotoxic efficacy in 100 cancer cell lines of different types with IC50 of <1 uM.

KVS0001 is a specific and bioavailable small molecule inhibitor of SMG1 kinase, disrupts nonsense mediated decay (NMD).

KZR-8445 (KZR8445) is a cyclic depsipeptide, client-selective Sec61 inhibitor with IC50 of 100 nM, targets the Sec61 translocon and selectively modulate Sec61-mediated protein biogenesis.

L6H21 is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor with binding KD value of 33.3 uM, blocks the formation of the LPS-TLR4/MD-2 complex.

LI-2242 is a potent pan-IP6K inhibitor with IC50 of with IC50 of 31, 42 and 8.1 nM for IP6K1, IP6K2 and IP6K3, respectively.

LP-403812 is a specific small molecule inhibitor of mammalian proline transporter (PROT), inhibits PROT-mediated proline uptake with IC50 of 0.1 uM on both recombinant human and mouse PROT.

Metablok (LSALT peptide) is a specific DPEP1-binding peptide and nonenzymatic dipeptidase-1 (DPEP-1) inhibitor.

A manufactured form of the thyroid hormone thyroxine (T4) that typically used to treat hypothyroidism.

LX-6171 is a small molecule proline transporter (SLC6A7) inhibitor with potential for treating cognitive and other disorders.

Macrocyclic peptide D4-2 is a macrocyclic peptide consisting of 15 amino acids that binds to the ectodomain of mouse SIRPα (Kd=10 nM, IgV-B6 SIRPα) and efficiently blocks CD47-SIRPα interaction in an allosteric manner (IC50=0.18 uM).

MASM7 is a small molecule activator of mitochondrial fusion via mitofusins (MFN1 and MFN2), concentration-responsively increases mitochondrial aspect ratio (Mito AR) in MEFs with EC50 of 75 nM, directly and specifically modulates MFN1/2 fusogenic activity

MCI-100 is a small molecule that displays greater potency than sulindac to protect RPE cells against oxidative damage, with lacked significant COX inhibitory activity, MCI-100 is more active than sulindac in protecting cells against oxidative damage.

MEISi-1 (MEIS inhibitor 1) is a specific small molecule inhibitor of MEIS1 (Meis1), significantly inhibits MEIS1 protein activity in MEIS-luc reporter assays at 0.1 uM, modulates hematopoietic stem cell (HSC) activity.

Melatonin Biotin is compound conjuncted melatonin with biotin..

A cholesterol depleting agent that shows antitumor activity both in vitro and in vivo.

MIDI (Mitochondrial division inhibitor) is a potent, covalent mitochondrial fission inhibitor, interacts with DRP1-C367 to block mitochondrial fission.

Mito-C is a specific chemical compound targeting NEETs proteins, induces mitochondrial network fragmentation and represses dengue viral replication.

MitoCKi (Creatine kinase inhibitor CKi-26) is a selective, covalent inhibitor of creatine kinases (CKs), inhibits recombinant creatine kinase B (CKB) phosphotransfer activity with IC50 of 185 nM, depletes creatine phosphagen energetics in cells.

Mito-LND (Mito-lonidamine) is a tumor-selective inhibitor of oxidative phosphorylation with IC50 of 1.2 and 2.4 uM for mitochondrial complexes I and II, respectively, impacts the activity of mitochondrial complexes, ROS generation and peroxiredoxin oxidat

ML181 (CYM50557) is a potent and selective GPR7 (Neuropeptides B/W receptor 1, NPBW1) antagonist probe with IC50 of 270 nM for inhibition of NPW-induced GPR7 activation.

MLS000544460 (EYA2i) is a specific, allosteric inhibitor of Eya2 phosphatase with IC50 of 4.1 uM, KD of 2.0 uM, does not bind Eya3 ED, Eya1 and Eya4 ED.

MM0299 (MM 0299) is a potent, selective inhibitor of lanosterol synthase (LSS, competition EC50=1.97 nM) with anti-proliferative activity, inhibits Mut6 cell growth (IC50=18.2 nM) and induces the synthesis of 24(S),25-epoxycholesterol (EPC).

MM0299 analog 13 (MM 0299 derivative 13) is a potent, selective, orally bioavailable, brain-penetrant inhibitor of lanosterol synthase (LSS, competition EC50=28.7 nM) with anti-proliferative activity.

MN132.0262 is a small molecule, dual inhibitor of A3G (APOBEC3G, IC50=20 uM).

MN256.0102 is a small-molecule APOBEC3G DNA cytosine deaminase inhibitor with IC50 of 3.9 uM.

MN256.0105 is a small-molecule APOBEC3G DNA cytosine deaminase inhibitor with IC50 of 4.3 uM.

MO-I-1100 is a small molecule inhibitor of aspartyl-(asparaginyl)-β-hydroxylase (ASPH), inhibits the β-hydroxylase activity of ASPH about 80%, inhibits Notch signaling in HCC cancer cells.

MO-I-1182 is a small molecule inhibitor of aspartate beta-hydroxylase (ASPH), suppresses cholangiocarcinoma metastasis.

MrgX1 inhibitor 8e is a potent, allosteric modulator of MrgX1 with EC50 of 13 nM, showed improved potency and microsomal stability than ML382.

MS0621 (UNC0621, MS 0621) is a small-molecule modulator of EWSR1::FLI1-mediated chromatin, reverses EWSR1::FLI1-mediated chromatin accessibility, persistently and selectively inhibits cell proliferation in Ewing sarcoma cell lines (SK-N-MC, IC50=128 nM).

msR4M-L1 is a chemokine-selective CXCR4 ectodomain mimic that selectively binds to MIF (KD<40 nM) but not CXCL12 (>140-fold selectivity).

MY-9B is a selective, allosteric and covalent inhibitor of sterile alpha toll/interleukin receptor motif containing-1 (SARM1) with IC50 of 1.2 uM, site-specifically and stereoselectively modify cysteine-311 (C311) in the noncatalytic, autoregulatory armad

Nalacina is a small molecule that partially mimicks the effects of auxin and potent inhibitor of indole-3-acetic acid (IAA) conjugation mediated by group II GH3 (Gretchen Hagen 3) in vascular plants, inhibits Gretchen Hagen 3 (GH3) acyl acid amido synthet

NCGC00108248 is small molecule inhibitor of Mir155 reporter, dose-dependently inhibits Mir155 reporter expression with EC50 of 2.2 uM.

NCGC00378430 (Compound 8430) is a novel small molecule compound that reduces the SIX1/EYA2 interaction in vitro with IC50 of 52 uM in the Alphascreen assay.

NCGC00507974 is a small molecule inhibitor of Mir155 reporter, dose-dependently inhibits Mir155 reporter expression with EC50 of 1.2 uM.

NCI-41356 is a small molecular inhibitor of αB-crystallin (CRYAB, HSPB5), significantly reducesthe interaction between CRYAB and VEGF165.

NCP26 is a potent, ATP-competitive prolyl-tRNA synthetase (ProRS, PRS) inhibitor, inhibits recombinant human ProRS in the presence of 100 μM proline with KD of 0.35 nM in TR-FRET assays.

NERx 329 (RPAi 329, NERx329) is a novel potent, specific inhibitor of replication protein A (RPA), demonstrated potent RPA inhibitory activity in vitro, in vivo, and in cellular assays.

Ninerafaxstat 3HCl (CV-8972) is a small molecule compound that promotes glucose oxidation, decreases fatty acid oxidation and improve overall mitochondrial respiration, inhibits the growth and proliferation of cancer cells.

NIO-1 (Novel inhibitor of OCT1) is a novel small molecule inhibitor of Octamer transcription factor OCT1, inhibits OCT1 activation with IC50 of 0.11 uM.

Nizubaglustat is a potent, selective inhibitor of glucosylceramide synthase (GCS) with IC50 of 25 nM, inhibits acid glucosylceramidase (GBA1) and neutral glucosylceramidase (GBA2) with IC50 of 200 and 0.08 nM, respectively.

NOX-6-18 is a potent, selective GPR132 antagonist with IC50 of 17 nM.

NOX-6-7 is a potent, selective GPR132 agonist with EC50 of 44 nM.

NPD389 is a potent, selective, fast-binding uncompetitive inhibitor of NADP+-dependent malic enzyme 2 (ME2) with IC50 of 4.63 uM, NPD389 is a mixed-type competitive inhibitor for the substrate L-malate and an uncompetitive inhibitor for the other substrat

NSC 773097 is a RITA analog that produces hyperselective cytotoxicity while maintaining antitumor efficacy (A498 cell IC50=130 nM).

NSC33353 (NSC 33353) is a small molecule inhibitor with potent anti-tumor activity against TNBC cells, enhances TNBC sensitivity to doxorubicin.

NUP-17d-52A (Plek2 inhibitor) is a specific small molecule inhibitor of Pleckstrin-2 (Plek2), binds to Plek2-DEP domain with high affinity (Kd=160 nM).

NV848 is a small molecule inhibitor of tRNA-specific 2′-O-methyltransferase (FTSJ1), exerts readthrough activity in vitro and in vivo.

NV914 is a small molecule inhibitor of tRNA-specific 2′-O-methyltransferase (FTSJ1), exerts readthrough activity in vitro and in vivo.

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.