LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.

Telotristat ethyl (LX1606) is a novel, orally-delivered inhibitor of tryptophan hydroxylase that reduces serotonin production.

BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay.

Pramipexole dihydrochloride hydrate is a selective dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the resear

Dexketoprofen works by blocking the action of a substance in the body called cyclo-oxygenase. It belongs to a class of medicines called non-steroidal anti-inflammatory drugs (NSAIDs).

Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer.

Tretinoin(Retinoic acid） is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ

Dopamine D2 and 5-HT1A partial agonist in development as a potential treatment for schizophrenia and other psychotic indications; Pharmacoloy profile makes it an atypical antipsychotic and a new approach for the treatment of schizophrenia.

BIO-013077-01 is a pyrazole TGF-β inhibitor[1].A wide range of cellular functions such as cell proliferation, differentiation, adhesion, migration, and apoptosis are regulated by TGF-β superfamily members. The TGF-βs include the three major TGF-β isoforms, TGF-β1, TGF-β2, and TGF-β3 which are expressed in mammals. TGF-β transduces signals through a complex of two related but structurally and functionally distinct serine/threonine kinase receptors, termed type 1 and type II. Deregulation of TGF-β signaling has been also implicated in various human diseases including cancer, pancreatic diseases, and hematological malignancies[1].

Lvguidingan is a potent anticonvulsant agent. Lvguidingan also has sedative-hypnotic, tranquilizing, and muscle-relaxing actions. Lvguidingan can be used as antiepileptic agent.

GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M-1 s-1 against E.coli GGT and huma

Ifenprodil tartrate is a NMDA receptor antagonist, specifically targets GluN1 and GluN2B subunits, also inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors..

An angiotensin II analog that is an agonist of AT1 angiotensin receptor..

Bremelanotide acetate is an analogue of the naturally occurring peptide alpha-MSH.

Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research .

Ornipressin is a vasoconstrictor, haemostatic and renal agent.

GAK inhibitor 12r is a higghly potent, selective inhibitor of cyclin G-associated kinase (GAK) with Kd of 89 nM; targets only 8 other kinases with greater than 90% inhibition in a diverse panel of 468 kinases

Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.

GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively.

AZD6280 is a potent, α2/3 functionally selective, partial GABAA receptor modulator with pKi of 7.7.

ATN-224 is a choline salt of tetrathiomolybdate and an inhibitor of superoxide dismutase 1 (SOD1; IC50s = 2.91 and 3.51 µM in human and mouse blood cells, respectively, in vitro).

Etelcalcetide (AMG 416) is a novel, long-acting selective peptide agonist of the calcium sensing receptor, activates calcium sensing receptor on parathyroid glands reducing PTH synthesis and secretion.

SR 8278 is the first synthetic antagonist of the nuclear heme receptor Rev-ErbA, inhibits the REV-ERBα transcriptional repression activity with EC50 of 0.47 uM in HEK293 cells..

A small-molecule IAP antagonist that binds to select baculovirus IAP repeat (BIR) domains resulting in dramatic induction of auto-ubiquitination activity and rapid proteasomal degradation of c-IAPs.

Chlorotoxin is a 36-amino acid peptide found in the venom of the deathstalker scorpion (Leiurus quinquestriatus).

Corticotropin-releasing hormone (CRH) is a peptide hormone involved in the stress response..

Ganirelix is a gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC,sub>50 = 3.6 nM; pA2 = 9.3).

Aviptadil (INN) is an analog of vasoactive intestinal polypeptide (VIP) for the treatment of erectile dysfunction,showed potent activity against COVID-19(SARS-COV-2).

Lixisenatide is a GLP-1 agonist for the treatment of diabetes type II.

VcMMAE is an antibody-drug conjugate (ADC) with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

Glucagon is a peptide hormone, exhibits therapeutic potential for metabolic disease.

Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor).

Smurf1-IN-A01 is an inhibitor of negatively regulatory factor Smurf1 for promoting bone formation.

S-2765 is specific to activated factor X (FXa),short peptide covalently bound to pNA (4-nitroaniline).

FOY 251 is a metabolite of Camostat and a pollen protease inhibitor for prevention and control of allergy.

SNS-314 is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively.

Cilengitide (EMD 121974; NSC 707544) is a potent integrin inhibitor for αvβ3 and αvβ5 integrin with IC50 of 4.1 nM and 79 nM, respectively; ~10-fold selectivity against gpIIbIIIa.

Semax is a synthetic peptide analog of adrenocorticotropic hormone

Elamipretide (SS-31, MTP-131, Bendavia) is a novel cell-permeable antioxidant tetrapeptide (D-Arg-dimethylTyr-Lys-Phe-NH2) that targets inner mitochondrial membrane and prevents oxidative damage of neuronal cells and other cell type.

γ-Glu-Phe (γ-Glutamylphenylalanine) is synthesized by Bacillus amyloliquefaciens (GBA) and Aspergillus oryzae (GAO). γ-Glu-Phe or the post-enzymatic reaction mixture enhances the umami intensity of commercial soy sauce and model chicken broth.

Diphenyleneiodonium chloride (DPI) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor.

E3 ligase Ligand 4 is a ligand of E3 ligase, used in PROTAC technology.

3-acetyl-11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense).

Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM.

A non-selective group I/group II metabotropic glutamate receptor (mGluR) antagonist.

Israpafant (Y24180) is a specific antagonist of PAF receptor that inhibits PAF-induced rabbit platelet aggregation in vitro (IC50=3.84 nM), with little effect on adenosine diphosphate- or arachidonic acid-induced aggregation.

Akt Inhibitor IV is n Inhibitor of Akt protein kinase

(–)-Isoxanthohumol is an enantiomer of isoxanthohumol. It is found in similar amounts as (+)-isoxanthohumol in beer, where xanthohumol is converted to isoxanthohumol during the brewing process.

AMG-510 is a specific covalent inhibitor of K-RAS(G12C) with potential antineoplastic activity.

An endogenous pentapeptide with morphine-like activity that exhibits strong hepatoprotective effects..

An ionophore antibiotic derived from S. hygroscopicus that acts as a potassium ionophore promoting K+/H+ exchange across mitochondrial membranes.

An irreversible inhibitor of carnitine palmitoyltransferase-1 (CPT-1) that inhibits fatty acid β-oxidation in rat liver with IC50 of 5-20 nM.

An orally available, brain penetrant p75NTR ligand that blocks p75-mediated cell death, also increases proliferation and survival of hippocampal neural progenitors.

MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.

BAY-293 (BAY293, BAY 293) is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM.

BI 882370 is a highly potent, selective, orally active RAF inhibitor with IC50 of 0.4, 0.8 and 0.6 nM for BRAF V600E, BRAF WT and CRAF, respectively.

CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2.

CID-25014542 is novel inhibitor of Raf kinases.

DBCO-Biotin is a Click Chemistry intermidate used for antibody-drug conjugates..

Isopimpinellin has chemopreventive effects, it effectively inhibits mouse COH activity (IC50 values 19-40 microM).Isopimpinellin is a new inhibitor against the Leishmania APRT enzyme.

Secoisolariciresinol diglucoside(SDG) is a phytoestrogen, estrogens and phytoestrogen from soy have been reported to have mild hypotensive effects, and SDG is a long-acting hypotensive agent, and that the hypotensive effect is mediated through the guanyla

Corynoline is a reversible and noncompetitive inhibitor of acetylcholinesterase(AChE) with the IC50 value of 30.6 microM, which exhibits the potent anti-inflammatory and/or immunosuppressive activity, the potent inhibitory activity of corynoline for the I

Gynostemma Extract

COH000 is an inhibitor of Ubiquitin-like 1-activating enzyme (SUMO-activating enzyme), with an IC50 of 0.2 μM for SUMOylation in vitro.

WAY-316606, a specific antagonist of SFRP1, functions as an inhibitor of canonical Wnt/β-catenin signalling in the human hair bulb.

Inhibitor of reverse transcriptase and RNA polymerase; immunosuppressive agent; intercalates in DNA.

IRE1 RNase inhibitor 8866 (MKC8866, MKC-8866) is a spectific small molecule inhibitor of mammalian IRE1 RNase activity, prevents the recombinant IRE1 protein from cleaving the synthetic XBP1 RNA probe.

JG-98 is an allosteric Hsp70 inhibitor, displays >3-fold more active, greater stability than MKT-077 against the breast cancer cell lines MDA-MB-231 and MCF-7 (EC50 of 0.4 uM and 0.7 uM, respectively).

JHU-083 is a Glutamine antagonist, a DON prodrug.

LB42708 is an orally active farnesyltransferase (FTase) inhibitor with IC50 of 0.8, 1.2, and 2.0 nM toward H-ras, N-ras, and K-ras, respectively

RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .

Lurbinectedin (PM01183) is a new DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.

TC-O 9311 is an activator of GPR139.

Regadenoson is the first selective A2A receptor agonist that is approved by the FDA and is currently used clinically.

STING agonist-3, compound 3, is a selective and non-nucleotide small-molecule STING agonist, which has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

Suramin sodium salt (BAY-205, NF-060) is an antitrypansomal drug that also possesses antitumor activity.

CC-930(Tanzisertib) is a selective and potent JNK1/JNK2/JNK3(IC50=61/7/6 nM) inhibitor and is currently under clinical development for fibrotic and infammatory indications.

TC-2153 is a specific, small moelcule inhibitor of neuron-specific tyrosine phosphatase STEP with IC50 of 24.6 nM.

Topiroxostat(FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.

UU-T02 is a novel potent, selective small-molecule inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM.

Vorapaxar is an antagonist of the protease activated receptor-1 (PAR-1), the principal platelet thrombin receptor.

Get 73 has been investigated for the treatment of Alcohol Dependence.

NDI-091143 is a novel ATP-citrate lyase inhibitor.

A 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for design of protein tyrosine phosphatase-1B (PTP1B) inhibitor.

Shield-1 is a cell-permeable FKBP ligand that is designed to protect an otherwise unstable protein domain from degradation; binds tightly to FKBP, induces rapid and processive degradation of the LID domain.

A metabolite of Flurazepam Controlled substance (depressant).

A potent and highly selective CaMKII inhibitor with IC50 of 63 nM.

A potent and selective dopamine reuptake inhibitor with IC50 of 3.7 nM.

A potent SHIP2 inhibitor that enhances in vitro insulin signaling through the Akt pathway more efficiently than AS1949490, and ameliorates abnormal glucose metabolism in diabetic (db/db) mice.

A prodrug of Brivanib, which is a dual inhibitor of VEGFR2 and FGFR1 with IC50 of 25 nM and 148 nM respectively.

A specific and membrane-permeable inhibitor of the InsP3Kinase activity of ITPKA (inositol-1,4,5-trisphosphate-3-kinase A) with IC50 of 20 uM.

XL228 is a protein kinase inhibitor targeting IGF1R, the Aurora kinases, FGFR1-3, ABL and SRC family kinases.

Acivicin is a glutamine analog that irreversibly inhibits glutamine-dependent amidotransferases involved in nucleotide and amino acid biosynthesis (Kis = 10 and 560 μM for anthranilate synthase and glutamate synthase, respectively).

APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.

AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.

BAM 7 is a direct and selective activator of proapoptotic Bax with EC50 of 3.3 μM.

b-AP15(NSC687852) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.

BCI-215 (BCI215) is a potent, tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor.

Camostat mesylate is a synthetic, orally bioavailable is a serine protease inhibitor. Used for the treatment of chronic pancreatitis. It attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity.

EED226 is a potent and selective PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED.

ELR510444 is a novel orally available small molecule inhibitor of HIF activity.

KY-04031 is a PAK4 inhibitor with IC50 of 0.79 uM, a basic building block in designing novel imidazo[4,5-b]pyridine-based PAK4 inhibitors..

GW 791343 hydrochloride is a P2X7 allosteric modulator.

Palomid 529 (P529) is a novel potent inhibitor of both the mTORC1 and mTORC2 complexes with a GI50 of <35 μM in the NCI-60 cell lines panel; reduces phosphorylation of pAktS473, pGSK3βS9, and pS6 but no effect observed on pMAPK or pAktT308.

Talnetant (SB 223412) is a potent and selective NK3 receptor antagonist(ki=1.4 nM, hNK-3-CHO); 100-fold selective for the hNK-3 versus hNK-2 receptor, with no affinity for the hNK-1 at concentrations up to 100 uM.

GSK650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively.

FKBP12 PROTAC dTAG-13 (dTAG-13) is an in vivo-active heterobifunctional adation tag (dTAG) small molecule that engage FKBP12F36V and CRBN, selectively degrade FKBP12F36V in a CRBN-dependent manner in cells.

FKBP12 PROTAC dTAG-7 (dTAG-7) is a cell-permeable heterobifunctional adation tag (dTAG) small molecule that engage FKBP12F36V and CRBN, selectively degrade FKBP12F36V in a CRBN-dependent manner in cells.

A peptide corresponding partly to the amino terminus of the Aα chain and Bβ chain of fibrin.

ACT-389949 is a novel potent and selective formyl peptide receptor type 2 (FPR2)/Lipoxin A4 receptor (ALX) agonist with EC50 of 3 nM, shows potential for the treatment of inflammatory disorders..

ADH-503, reduced myeloid cell recruitment and altered the phenotypes of myeloid cells within the tumor. ADH-503 treatment increased responses to chemotherapy or radiation and also rendered normally resistant tumors sensitive to checkpoint blockade, as T c

BK-1361(BK1361, cyclo-RLsKDK) is a cyclic peptide with RLsKDK (s=D-serine) that functions as a potent, selective inhibitor of ADAM8 with IC50 of 120 nM.

Tretazicar (CB 1954), an antitumor prodrug, is highly selective against the Walker 256 rat tumour line. Tretazicar is enzymatically activated to generate a bifunctional agent, which can form DNA-DNA interstrand cross-links. Tretazicar in rat cells involve

cFMS Receptor Inhibitor II is a cell-permeable anilinoquinoline compound that acts as a strong, active site-targeting inhibitor of MCSF receptor/cFMS.

D3263 is a novel, orally bioavailable small molecule Trp-p8 agonist.

DJ101is a potent and metabolically stable tubulin inhibitor that can circumvent the drug efflux pumps responsible for multidrug resistance of existing tubulin inhibitors.

ID-8 is a DYRK inhibitor, and sustains embryonic stem cell self-renewal in long-term culture.

Ingliforib is a glycogen phosphorylase inhibitor, with IC50s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase, and has cardioprotective activity.

JBSNF-000088 (6-Methoxynicotinamide) is a small molecule nicotinamide analog that inhibits Nicotinamide N-methyltransferase (NNMT) with IC50 of 1.8, 2.8 and 5.0?μM for human, monkey and mouse NNMT, respectively.

Lodoxamide tromethamine is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.

MeO-Suc-Arg-Pro-Tyr-pNA is a synthetic colorimetric peptide substrate displaying chymotrypsin-like specificity and is used in the measurement of Kallikreins. It is succinylated at N-terminus and has a nitroanilide tag at the C-terminus.

MRT-68921 hydrochloride (MRT68921) is a potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively.

MYC inhibitor DC-34 is a potent small molecule that selectively inhibits MYC at the transcriptional level only when a G-quadruplex (G4) is present in the promoter, binds to MYC G4 with Kd of 9.4 uM.

Nepicastat (RS-25560-197, SYN-117) is a potent, selective, orally active inhibitor of dopamine-beta-hydroxylase (DBH) with IC50 of 8.5 and 9.0 nM for bovine and human DBH, respectively.

PF 3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 uM).

PXS-5153A (PXS5153A) is a potent, selective, fast-acting, dual LOXL2/LOXL3 inhibitor with IC50 of <40 nM against all mammalian species LOXL2, inhibits human LOXL3 with IC50 of 63 nM.

SB297006 is a CCR3 antagonist, which significantly inhibits proliferation and neurosphere formation in CCL11-treated neural progenitor cells.

SRA737 is a highly potent, selective, ATP-competitive inhibitor of Chk1 with IC50 of 1.3 nM.

UAMC-3203 is a novel potent, drug-like ferroptosis inhibitor with IC50 of 12 nM, inhibit erastin-induced ferroptotic cell death more potently than Ferrostatin-1.

UAMC-3203 is a novel potent, drug-like ferroptosis inhibitor with IC50 of 12 nM, inhibit erastin-induced ferroptotic cell death more potently than Ferrostatin-1.

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Yhhu-3792 is a novel small molecule that enhances the self-renewal capability of neural stem cells (NSCs) in vitro and in vivo via activating the Notch signaling pathway.

Adenosine Amine Congener is shown to be an aqueous-soluble Adenosine A1-R agonist.

NLX-101（F-15599） is a novel compound that activates serotonin 5-HT1A receptors with exceptional selectivity, having over 1000-fold higher affinity for this target over other receptors.

AGX51 is a small-molecule Id antagonist and inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduced viability.

A specific blocker of the time dependent delayed rectifier potassium current, devoid of any β-adrenoceptor blocking activity. Exhibits proarrhythmic and prohypertensive activity in vivo.

AM-6494 is a potent and orally efficacious BACE1 inhibitors with IC50 of 0.4 nM and shows biochemical IC50 BACE2/BACE1 ratio of 47.

BAY-1797 is a potent and selective P2X4 antagonist.

BAY-298 is a potent, and selective antagonists of the luteinizing hormone receptor with IC50 of 96 nM, 23 nM and 78 nM against human, rat, and cynomolgus monkey LH receptors.

CCT365623 is a potent, selective and orally bioavailable LOX inhibitor with IC50 of 0.9 μM and 1.5 μM for LOX and LOXL2.

Compound 3 (RIP2 clinical candidate) is the first RIP2 kinase inhibitor to enter clinical trials.

DBPR112 is a potent EGFR mutation inhibitor against EGFRL858R/T790M double mutations with IC50 of 48 nM and also exhibits 10-fold potency better than Osimertinib, against EGFR and HER2 exon 20 insertion mutations.

DS18561882 is a potent and isozyme-selective MTHFD2 inhibitor with GI50 of 140 nM, which also shows good oral pharmacokinetic profile.

DS54360155 is an orally potent analgesic without μ-opioid receptor agonist activity.

DS-6051b is a potent and selective ROS1 and TRK family inhibitor with IC50 of 0.207 nM, 0.622 nM and 0.980 nM against ROS1, NTRK1 and NTRK3. DS-6051b especially inhibits ROS1 G2032R and other crizotinib-resistant ROS1 mutants.