DL-AP-3, or AP-3 is a Potent metabotropic glutamate receptor antagonist.

Gramicidin S is an anttiboitics. Gramicidin S reduces the cell number of planktonic cells within 20-40 min at a concentration of 40-80 μg/mL. Gramicidin S kills the cells of pre-grown biofilms at concentrations of 100-200 μg/mL, such that no re-growth is possible. The translocation of the peptide into the cell interior and its complexation with intracellular nucleotides, including the alarmon ppGpp, can explain its anti-biofilm effect. The successful treatment of persistently infected root canals of two volunteers confirms the high effectiveness of GS. The broad Gramicidin S activity towards resistant, biofilm-forming E. faecalis suggests its applications for approval in root canal medication.

Meclozine is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Potent activator of SHIP-1 inducing apoptosis of the cancer cell lines in vitro in both a time and dose dependant manner

PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).

Dodecylphosphocholine is a detergent widely utilized in NMR studies of membrane proteins.

PL-SNS-032 conjugate 955 can potently degrade CDK9 in a ubiquitin-proteasome-dependent manner and is much more potent than SNS-032 against various tumor cells in vitro.

VU0652957 (VU2957, Valiglurax) is a potent, selective mGlu4 positive allosteric modulator (PAM) with EC50 of 64.6 nM in calcium mobilization human mGlu4/Gqi5 assays; showes excellent pharmacokinetics across species (low CLps, %F > 35%), an acceptable CYP profile (>30 uM vs. 3A4, 2D6 and 2C9, 12.5 uM vs. 2C19 and 1.5 uM vs. 1A2), no CYP induction or timedependent inhibition and excellent metabolite coverage across species; also shows attractive predicted human PK parameters (CLps 5-9 mL/min/kg, Vds 1-2 L/kg and t1/2 2-4 hours).

KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be us

PABK (para-azidobenzyloxycarbonyl lysine) is a site-specific small molecule-activated amino acids which could be installed into proteins in the zebrafish embryo and enable fast and tunable activation of the function of several enzymes.

non-deuterated form of VV116.VV116 is an oral drug candidate of nucleoside analog against SARS-CoV-2.

NSC112200 is a chemical inhibitor of the EZH2 deubiquitinase ZRANB1 (at 10 uM), destabilizes EZH2, promotes proteasomal degradation of EZH2 and inhibits the viability of TNBC cells.

JNJ 2408068 is a potent RSV (respiratory syncytial virus) inhibitor. JNJ2408068 significantly inhibits replication of RSV A and B subtypes in the lungs of cotton rats without any evidence of toxicity. The minimum protective dose of JNJ 2408068 appears to be approximately 0.39 mg/kg[1].

IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.

CX-4945 Sodium Salt is a water soluble CX-4945 (GLXC-04060), First-in-class Casein kinase 2 (CK2) inhibitor, sequentially attenuating the proteins in PI3K/Akt and MAPK pathways.

SP-13786(UAMC-1110) is a Novel potent and selective inhibitor of fibroblast activation protein (FAP), displaying low nanomolar inhibitory potency and high selectivity against the related dipeptidyl peptidases (DPPs) DPPIV, DPP9, DPPII, and prolyl oligopeptidase (PREP)

VX-150 (EOS-62073), a NaV1.8 blocker, is currently in a phase II clinical trial for the treatment of patients with acute pain. VX-150 significantly alleviates postoperative pain.

VU6015929 is a selective discoidin domain receptor inhibitor. VU6015929 potently blocks collagen-induced DDR1 activation and collagen-IV production, suggesting DDR1 inhibition as an exciting target for antifibrotic therapy.

MRT68921 is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.

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

VX-765 is a novel Caspase-1 inhibitor with an IC 50 of 0.8nM being investigated for the treatment of epilepsy, currently being developed by Vertex.

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

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

PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.