Novel Cyclic Peptide Inhibitor of the p6/UEV Protein-Protein Interaction, disrupting the p6/UEV interaction with an IC50 of 6.17 ± 0.24 μM by binding to UEV with a Kd of 11.9 ± 2.8 μM.

Novel bicyclic peptidyl pan-Ras inhibitor, binding selectively to the GTP-bound forms of wild-type and mutant Ras isoforms (K D = 21 nM for KRasG12V-GppNHp) and being highly cell-permeable and metabolically stable (serum t1/2 > 24 h)

Natural irreversible inhibitor of acetylcholinesterase (AChE)

Novel PD-1/PD-L1 inhibitor, binding two PD-L1 and efficiently block the PD-1/PD-L1 interaction

Natural antibacterial peptide, activating the AAA+ protease ClpC/ClpP, causing cell death by uncontrolled protein degradation

Novel Effective Aminoluciferin Derivative for Deep Bioluminescence Imaging

Androgen receptor (AR) antagonist, inhibiting AR function in castrate-resistant prostate cancer (CRPC)

Novel ABA receptor agonist, preferentially activating Pyrabactin Resistance 1 (PYR1) with low nanomolar potency

Selective D1 agonist with anti-Parkinsonian activity

Novel CXCR2 selective antagonist with a low CXCR1 antagonism preference

Novel potent CXCR2 antagonist

Nonsteroidal dermatologic and anti-inflammatory agent, blocking the MEK1/2-Erk1/2 pathway, inhibiting chronic contact hypersensitivity responses (CHRs) and the rebound phenomenon following withdrawal of corticosteroid therapy without immunosuppression

Novel inhibitor of CXCL8-mediated chemotaxis through selective regulation of CXCR2-mediated signaling

Novel low-impact ampakine that can safely activate AMPA receptors without causing excito-neurotoxicity, rapidly crossing the blood-brain barrier (T max = 2 min), protecting against respiratory depression

Potent LTB4 receptor antagonist

Novel potent and substrate-competitive PTP1B and TCPTP dual inhibitor

Novel Wnt/β-Catenin Inhibitor, Preferentially Inhibiting the Growth of Breast Cancer Stem-like Cells

Potent antimalarial agent against Plasmodium falciparum 3D7

Potent antimalarial agent against Plasmodium falciparum 3D7

Novel orally efficacious antimalarial agent against P. falciparum 3D7 ( IC50: 51 nM)

Potent serine protease inhibitor, targeting the S 2 S 3 thrombin and FXa subsites

Direct thrombin inhibitor, preventing occlusive arterial and venous thrombosis in a canine model of vascular injury

Novel potent and selective inhibitor of PI5P4Ks

Inhibitor of PIM, suppressing cyclin-Dependent Kinase 2 (CDK2)

Novel potent pregnane X Receptor (PXR) agonist

Novel dual PXR and AhR agonist

Potent anti-cancer agent

Inducer of demyelination and motor dysfunction via upregulation of IGF-1

Agonist for the cannabinoid receptors, with Ki values of 59.21 nM at CB1 and 136.38 nM at CB2 and EC50 values of 11.98 nM at CB1 and 16.2 nM at CB2

5-HT1A receptor agonist