Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction.

A potent, selective, and orally bioavailable ghrelin receptor (GHSR) inverse agonist with binding pKi of 8.36.

TVB-3664 is a FASN inhibitor which significantly reduces tubulin palmitoylation and mRNA expression.

YUN35454, also known as LMPTP INHIBITOR 1 is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A. LMPTP is a key promoter of insulin resistance and that LMPTP inhibitors would be beneficial for treating type 2 diabetes. YUN35454 was first reported in Nature Chemical Biology (2017), 13(6), 624-632.

KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).

Melphalan(Sarcolysin; L-PAM) is a chemotherapy drug belonging to the class of nitrogen mustard alkylating agents; attaches the alkyl group to the guanine base of DNA.

IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

PS-1145 has been shown to be an IKK (IKB kinase) inhibitor.

Tipifarnib S enantiomer is a potent and selective inhibitor of FTase (farnesyltransferase).

A novel, potent, and selective inhibitor of Late sodium current (late INa) for treatment of long QT-3 syndrome (LQT-3), hypertrophic cardiomyopathy (HCM), and ventricular tachycardia–ventricular fibrillation (VT–VF).

UU-T03 is the ethyl ester derivative of UU-T02, which is a potent, selective inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; exhibits growth inhibition of SW480 cells with IC50 of 10.77 uM; downregulates the transcription of AXIN2, LGR5, cyclin D1, and c-Myc in dose-dependent manners in SW480 cells.

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.

PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.

Tamoxifen(ICI-46474) is an antagonist of the estrogen receptor in breast tissue via its active metabolite, hydroxytamoxifen.

GSK3039294 is a Serum amyloid P component inhibitor.

LDC1267 is a highly selective TAM(Tyro3, Axl and Mer) kinase inhibitor with IC50 of <5 nM/8 nM/29 nM for Tyro3,Axl and Mer respectively.

Gemcabene (PD-72953, PD72953) is a first-in-class lipid-lowering agent and activator of PARP.

VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.

MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors.

NSC 23766 is a specific inhibitor of the binding and activation of RAC GTPase with IC50 of ~50 μM; does not inhibit the closely related targets, Cdc42 or RhoA.

IACS-13909 is a specific and potent allosteric inhibitor of SHP2 that suppresses the signaling of RTK/MAPK pathway and overcomes multiple mechanisms underlying osimertinib resistance. IACS-13909 potently impedes the proliferation of tumors with a broad spectrum of RTKs as the oncogenic driver. Importantly, in NSCLC models with acquired resistance to osimertinib, IACS-13909 administered as a single agent or in combination with osimertinib potently reduces tumor cell proliferation in vitro and in vivo. Together, our findings provide preclinical evidence for using a SHP2 inhibitor as a therapeutic strategy in acquired EGFR inhibitor-resistant NSCLC.

GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.

Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.

AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.

Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM.

BIX01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3. BIX01294 suppresses osteoclast differentiation on mouse macrophage-like Raw264.7 cells. BIX01294 enhances the cardiac potential of bone marrow cells.

Fasudil, a Rho-kinase inhibitor, has been shown to reduce portal venous pressure in cirrhotic rats.

Fostemsavir Tris (BMS-663068 (Tris)) is the phosphonooxymethyl prodrug of BMS-626529. Fostemsavir Tris (BMS-663068 (Tris)) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.

Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs.