Novel potent and selective covalent inhibitor of Bruton’s tyrosine kinase (BTK), targeting a noncatalytic cysteine residue (Cys481) for covalent bond formation

Novel potent inhibitor of Bruton’s tyrosine kinase (BTK)

The first small-molecule inhibitor with significant selectivity among the KCa2 channel subtypes

Novel inhibitor of alpha2beta1 integrin, decreasing average platelet adhesion in individuals with the C/T807T genotype but not in those harboring C807C

Novel unique Na V modulator, acting as a conspicuous outlier, eliminating fast but not slow inactivation

Novel effective reversible and noncovalent inhibitor of DprE1.

Negative control for BTZO-1

Ligand of the Imidazoline(2) binding site (I 2 BS), showing very good affinity for the I 2 BS (K i of 1.4 nM; K d = 1.3 nM), good selectivity compared with the α 2 -adrenoceptor (909-fold)

Potent and selective agonist of μ-opioid receptor (MOR) with relatively low affinity for the δ-opioid receptor and the κ-opioid receptor

Direct-acting vasodilator with anti-tachycardiac effect

Bulgecin A is an inhibitor of binuclear metallo-beta-lactamases and Lytic transglycosolase.

Potent inducer of anemia

Natural inhibitor of microRNA-21, reducing growth of cancer cells

Novel 11β-HSD1 inhibitor

Selective 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) inhibitor

Novel BB2 receptor antagonist. attenuating the feeding responses evoked by exogenous gastrin releasing peptide-29

Highly selective inhibitor of AChE

Novel Gemini vitamin D analog, targeting CD44-STAT3 signaling and inhibiting breast cancer invasion

Novel promising spectroscopic probe for inositol 5-phosphatase(s)

Novel potent and selective PTP-1B inhibitor

β-Hairpin Octapeptide, acting as a potent mouse melanocortin-4 receptor (mMC4R) antagonist

Natural inhibitor of BACE1

Novel sensitizer of BRAF wild-type melanoma cells to vemurafenib, significantly reducing melanoma cell viability, with limited toxicity for normal human fibroblasts

Novel broad-spectrum intracellular targeting antibacterial agent, interacting with the 70S ribosome of E. coli and inhibiting its protein synthesis, demonstrating superior clearance of bacteria from the spleen, liver, and kidneys of mice, infected with S.

Novel broad-spectrum intracellular targeting antibacterial agent, interacting with the 70S ribosome of E. coli and inhibiting its protein synthesis, demonstrating superior clearance of bacteria from the spleen, liver, and kidneys of mice, infected with S.

FPP analogue, bearing an alkyne group to allow for post-prenylation protein labeling

Novel multi-functional resveratrol derivative for the treatment of atrial fibrillation

Novel selective activator for TREK, against other two-pore domain K (K2P) channels

First-In-Class Inhibitor of the Interaction between Bacterial RNA Polymerase and Sigma Initiation Factor, Affecting the Viability and Toxin Release of Streptococcus pneumoniae

The first C3b-binding complement inhibitor, inhibiting the formation of the membrane attack complex (MAC) by preventing cleavage of C5

Inducer of mast cell degranulation

Novel potent inhibitor of botulinum neurotoxin serotype E (BoNT/E)

Novel covalent cross-linker to the SARS-CoV-2 frameshifting element (FSE), directly targeting engagement of the SARS-CoV-2 FSE in cells, dose dependently reducing frameshifting in cells expressing the SARS-CoV-2 FSE, with no significant effect on frameshi

Selective inhibitor of hCA IX and hCA XII

Potent and selective inhibitor of cathepsin B

Novel specific inhibitor of cathepsin L, effectively inhibiting degradation of LC3-II and GABARAP

Novel selective CaBdf1 BD1 inhibitor

Novel inhibitor of CaBdf1 BD1 with low-micromolar affinity and three- to fivefold selectivity relative to human Brd4 BD1

Novel selective CaBdf1 BD2 inhibitor

Potent, selective class B inhibitor of calcium-activated chloride channels (CaCCs)

Novel photocaged ERK1/2 inhibitor as a light-controlled anticancer agent

Potent agonist at thyroid hormone receptor (TR)

Effective inhibitor of the carbonic anhydrase (CA) from Trypanosoma cruzi (TcCA)

Novel inhibitor of p110

Cell permeable derivative of calcein, becoming fluorescent on hydrolysis

Dual inhibitor of fibroblast growth factors (FGF) and vascular endothelial growth factor (VEGF) ; Anti-angiogenic

Ionophore highly selective for Ca , potentiating responses to NMDA but not quisqualate

Transmembrane protease serine 2 (TMPRSS2) inhibitor for the treatment of chronic pancreatitis and postoperative gastric reflux, blocking SARS-CoV-2 replication in TMPRSS2-expressing human cells

Novel destabilizer of CAND1-Cullin1 interaction, inducing a p53-stress response pathway

Natural cannabinoid precursor

Natural cannabinoid precursor

Novel self-assembling lysine-rich cationic amphipathic peptide (CAP)

Reverse-transcriptase_inhibitor>Non-nucleoside reverse transcriptase inhibitor

Broad spectrum antibiotic used in the therapy of drug resistant tuberculosis as a second line agent

Antimuscarinic and anticholinergic, acting as an antagonist of NMDA receptor

Antioxidant, free radical scavenger and potent inhibitor of lipid peroxidation

Mixture of Meropenem and vaborbactam for adults with complicated urinary tract infections (cUTI), including a type of kidney infection, pyelonephritis, caused by specific bacteria

Analog of etomidate that interacts weakly with 11β-hydroxylase

Novel fluorescent probe targeting of G-quadruplex structures and trapping cytoplasmic RNA G-quadruplex structures in cells

Inducer of deformation in Zebrafish>Zebrafish through the AhR-mediated, CYP1A-independent pathway

Novel inhibitor of full-length GST-tagged CARM-1

Novel potent inhibitor of coactivator-associated arginine methyltransferase 1 (CARM1)

Novel, potent, long-acting, selective, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4) with hypoglycemic activity

Anthracycline antineoplastic antibiotic, intercalating into DNA and interacting with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.

Long acting ß2-adrenoreceptor agonist (LABA)

Novel orally available α4 integrin receptor inhibitor

Irreversible and nonselective Monoamine_oxidase_inhibitor>monoamine oxidase inhibitor (MAOI)

DNA minor groove alkylating agent, alkylating N3 of adenine in a consensus sequence 5'-(A/T)(A/T)A*

Novel Cas9 Inhibitor, direct binding to apo-Cas9, preventing Cas9:gRNA complex formation

The first inhibitor of fungal (1→3)-β-D-glucan synthesis

Natural potent neutrophil elastase (NE) inhibitor with an IC 50 value of 2.79 ± 0.07 μM

Novel activator of autophagy for potential treatment of cystic fibrosis

Selective inhibitor of cathepsin B endopeptidase and exopeptidase activities

Selective inhibitor of cathepsin B endopeptidase and exopeptidase activities

Novel selective reversible inhibitor of cathepsin X

Novel ligand of voltage-gated calcium channel α2δ-1 subunit (Cavα2δ-1)

Selective inhibitor of 15-hydroxy PGDH, significantly suppressing endogenous 11-oxo-ETE production with a corresponding increase in 11(R)-HETE

Isoform-selective inhibitor of histone deacetylase (HDAC1)

Novel potent CysLT2 receptor antagonist

Novel Mdm2 inhibitor, an analog of Nutlin-3

Novel Mdm2 inhibitor, an analog of Nutlin-3

Novel RAF kinase inhibitor

Novel SRC kinase inhibitor

Novel IκB kinase inhibitor

Novel Thymidine kinase (TK) inhibitor

Novel Cyclin-dependent kinase inhibitor

Novel IκB kinase inhibitor

Novel Cell_cycle>cell cycle inhibitor

Dual thymidylate synthase and dihydrofolate reductase inhibitor

Novel inhibitor of Mycobacterium marinum MelF (Rv1936), exhibiting bacteriostatic/bactericidal activity against M. marinum and M. tuberculosis in vitro

Selective sphingosine kinase 1 (SK1) inhibitor

Novel inhibitor of HIV-1 entry

Novel inhibitor of Mycobacterium marinum MelF (Rv1936), exhibiting bacteriostatic/bactericidal activity against M. marinum and M. tuberculosis in vitro

Selective inhibitor of Adenylyl Cyclase isoform-2 (AC2)

Novel inhibitor of HIV-1 gene expression

Novel potent inhibitor of filamentation and biofilm formation by the Candida albicans SC5314 strain

Novel inhibitor of Mycobacterium marinum MelF (Rv1936), exhibiting bacteriostatic/bactericidal activity against M. marinum and M. tuberculosis in vitro

Novel Protein kinase A and B inhibitor

The first clickable, photoreactive probe that inhibits both γ-secretase and PSase activities and specifically labels PS1-NTF and signal peptide peptidase (SPP)

Novel cell-permeable, potent, reversible, and substrate competitive LSD1 inhibitor, promoting the adipogenic differentiation of hESCs

Novel inhibitor of viral transcriptional elongation, blocking both HIV-1 replication and reactivation

NF-kappa B (NF-kB) inhibitor and p53 activator

Novel selective inhibitor of KDM4s, inhibiting all members of the KDM4(A-E) subfamily

Novel KDM4 inhibitor, inhibiting equally all members of the KDM4 family and exhibiting modest selectivity over other JmjC-KDMs including KDM2A and PHF8

Novel Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα -related Diseases

The first Gatekeeper RXR antagonist that does not show allosteric inhibition in permissive RXR heterodimers, binding domain (LBD) at the entrance of the ligand binding pocket (LBP), blocking access to the LBP and thus serving as a gatekeeper

FTY720 derivative

Novel inhibitor of the E2 ubiquitin-conjugating enzyme Cdc34A

Novel Cereblon modulator, promoting ZBTB16 degradation by primarily engaging distinct structural degrons on CRBN-ZnF1 zinc finger domains

PqsE inhibitor, binding to the active center inhibiting PqsE's thioesterase activity in cell-based and in vitro assays

PqsE inhibitor, binding to the active center inhibiting PqsE's thioesterase activity in cell-based and in vitro assays

Novel potent orally bioavailable Syk kinase inhibitor

Novel Cereblon modulator, promoting ZBTB16 degradation by primarily engaging distinct structural degrons on CRBN-ZnF3 zinc finger domains

Novel Indigoid Anti-tuberculosis Agent; Antimicrobial

Novel coupleable ceritinib analog with a linker, also binding multiple other kinases, including FAK1, RSK1/2, ERK1/2, CAMKK2 and FER

Novel Inhibitor of TonB Function

Novel Inhibitor of TonB Function

Potent photoprobe as Rho/MKL1/SRF transcription inhibitor

Novel inhibitor of G Protein-Coupled Receptor Kinase

Novel covalent selective GRK inhibitor, interacting with a nonconserved cysteine (Cys474)

Novel sialyltransferase inhibitor (IC 50 : 2 µM)

Novel MmpL3 inhibitor

(E/Z)-CCR-11 (Comp 12) is a selective CD38 inhibitor, with an IC50 of 20.8 μM against CD38 cyclase. (E/Z)-CCR-11 promotes increases in cellular NAD+ levels and interferon γ.

Novel CCR4 antagonist, enhancing DC activation and homing to the regional lymph node and showing potent vaccine adjuvant activity through the inhibition of regulatory T-cell recruitment

Novel dual FLT3/Aurora A inhibitor, overcoming D835Y-mediated resistance to FLT3 inhibitors in acute myeloid leukaemia cells

Inactive analogue of pictilisib to be used as the negative control

Highly Selective Oral Checkpoint Kinase 1 (CHK1) Inhibitor

Novel inhibitor of BCL6

Novel inhibitor of the efflux function of ABCG2, selectively reversing ABCG2-mediated MDR in cancer cells in vitro and in vivo

Novel potent covalent BRD4 degrader, degrading BRD4 in a proteasome- and RNF4-dependent manner without inhibiting RNF4 autoubiquitination activity

Novel MC1R agonist

Novel Caspase-1 inhibitor

Novel telomerase inhibitor

Retinoic acid receptor beta (RARbeta) agonist, overcoming inhibition of axonal outgrowth via phosphoinositide 3-kinase signalling in the injured adult spinal cord.

Novel CD22 glycan ligand, targeting CD22-expressing B cells, uptaking and enhancing siRNA gene expression knockdown via formation of CD22 glycan ligand-conjugated siRNA

Novel CD33 pre-mRNA splicing modulator, increasing exon 2 skipping in cellular mRNA pools

Novel agonist for the vitamin D receptor (VDR)

Novel agonist for the vitamin D receptor (VDR)

Novel agonist for the vitamin D receptor (VDR)

Novel selective cdDHQD inhibitor

Novel potent and selective CDK12 inhibitor

Potent, ATP-binding site-targeting Cdk4/D1 inhibitor

Novel potent CDK6 degrader

Novel potent and balanced dual CDK6/PIM1 inhibitor, showing high kinase selectivity and displaying stronger potency in reducing the burden of AML than palbociclib and SMI-4a in vivo

Novel potent CDK8 inhibitor

Novel potent and selective dual inhibitor of CDK8 and CDK19

Potent dual inhibitor of CDK8/19, suppressing phosphorylated STAT1 in various cancer cells

Novel potent and selective inhibitor of CDK8, also modulating CDK19

Novel inhibitor of CDK8

Novel highly potent, selective, permeable CDK8 inhibitor

Novel potent and highly selective CDK8 inhibitor, with no apparent potential for time-dependent CYP3A4 inhibition

Novel potent CDK8 inhibitor

Novel CDK8 inhibitor

Novel CDK8 inhibitor

Novel CDK8 inhibitor

Novel Potent and Selective CDK9 Degrader for Targeting Transcription Regulation in Triple-Negative Breast Cancer

Novel potent dual inhibitor of CDK9 and BET proteins with balanced activities of BRD4 (IC50 = 12.7 nM) and CDK9 (IC50 = 22.4 nM), as well as good antiproliferative activities on a small cancer cell panel

Highly specific, ATP-competitive inhibitor of CDK9/CycT1 with antiviral activity

Novel inhibitor of the cyclin-dependent kinase 9 (CDK9)

Potent and selective ATP competitiive inhibitor of cycB-CDK1, cycE-CDK2, and cycD1-CDK4

Novel potent inhibitor of cyclin-dependent kinases (CDKs) 2, 5, and 9, displaying activities across more than 60 cancer cell lines

Novel photoaffinity probe for cyclin-dependent kinase (CDK) family

Novel anti-hepatitis B virus (HBV) agent

Highly permeable non-Pglycoprotein substrate

Potent Antagonist for the Human Thyrotropin Receptor (TSHR)

Novel highly selective inhibitor of multidrug resistance protein 4 (MRP4)

First-generation cephalosporin antibiotic and interleukin 15 inhibitor, specifically interacting with interleukin 15 (IL-15) receptor subunit α (IL-15Rα) and to inhibit IL-15-dependent TNF-α and IL-17 synthesis, showing inhibitory activity against all of

Third-generation, semi-synthetic, beta-lactam cephalosporin antibiotic with antibacterial activity

Second-generation, semi-synthetic, beta-lactam cephalosporin antibiotic with antibacterial activity

Broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin antibiotic, inhibiting bacterial cell wall synthesis via inhibition of cross-linking of peptidoglycans

Third-generation broad spectrum antibiotic against both gram-positive and gram-negative microorganisms

Fourth-generation cephalosporin

Broad-spectrum fourth-generation cephalosporin antibiotic

beta-Lactamase-stable, broad-spectrum, third-generation cephalosporin antibiotic with antibacterial activity

Broad-spectrum, fifth-generation cephalosporin antibiotic, inactivating penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall

Novel modulator of cell death signal transduction pathways, reducing the cytotoxicity of anthrax lethal toxin (LT)

Novel highly selective TAF1 inhibitor

Novel potent ALK inhibitor. also inhibiting the insulin receptor

Novel potent ALK inhibitor

Prodrug of CEP-751 (KT-6587) as antitumor agent, inhibiting protein kinases

Novel potent, selective, and orally bioavailable inverse agonist of the histamine H 3 receptor (H 3 R)

Novel selective inhibitor of the nuclear enzymes poly(ADP-ribose) polymerase (PARP) 1 and 2

Natural disrupter of RNA G-quadruplexes, inhibiting G-quadruplex-dependent alternative splicing, stimulting the stomach lining and inducing vomiting

Novel small molecule prodrug for use with SEAKER cells, exhibiting enhanced anticancer activity

Novel probe for cellulose synthase trafficking, inhibiting cellulose deposition and interferes with the trafficking of cellulose synthase complexes and their associated proteins KORRIGAN1 and POM2/CSI1

Novel Probe for the High Temperature Requirement A (HTRA) Serine Proteases

Novel non-steroid reversible dual inhibitor of CYP17 and CYP11B2 against prostate cancer with fewer cardiac side effects

Potent inhibitor of TTK kinase

Novel Highly Potent, Selective, Bioavailable TTK (threonine tyrosine kinase) Inhibitor

Novel GSK3 inhibitor, inducing cell death through cyclin D1 depletion in breast cancer cells

Novel inducer of neural differentiation and growth arrest in human primary GBM-derived cells, playing a tumor-suppressive role via cAMP/CREB signaling pathway

Novel PRL-3 inhibitor, blocking the migration and invasion of metastatic cancer cells

CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells.

Novel functional Gboxin analogue that is suitable for live-cell ultraviolet crosslink conjugation and click chemistry

Novel Bruton's tyrosine kinase (BTK) inhibitor

Novel inhibitor of Wnt/β-catenin signaling; Anticancer agent promoting PKCα-mediated β-catenin phosphorylation/degradation

Non-peptide tachykinin NK1 receptor antagonist

Activator of RORalpha, inducing growth arrest in androgen-independent DU 145 prostate cancer cells

Novel HIV-1 protease inhibitor, also potently inhibiting major aspartyl peptidase 1 (May1), a secreted Cryptococcus neoformans protease

Peptoid Tat/transactivation response element inhibitor, inhibiting human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry