Biotin modification of SBP1.SBP1(spike-binding peptide 1) is a first-in-class peptide binder to the SARS-CoV-2 spike protein. SBP1 specifically binds SARS-CoV-2-RBD with low nanomolar affinity. SBP1 to the RBD was determined to be 47 nM with the average Kon = 4.69*104M-1S-1 and Koff=2.2*10-3.The interaction between SBP1 and the RBD of SARS-CoV-2 spike protein was validated by bio-layer interferometry. The KD, derived from protein association and dissociation kinetics, was found to be 47 nM after averaging the fitting values at different protein concentrations. The amino acid sequence of SBP1 is entirely derived from human ACE2 and should be recognized as endogenous by the human immune system. This feature could be highly beneficial in later stages of pre-clinical development.

SIS17 is a potent and selective HDAC 11 inhibitor with an IC50 value of 0.83 μM. SIS17, is active in cells and inhibited the demyristoylation of a known HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.

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

MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.

Furin inhibitor I is a selective, irreversible, and cell-permeable competitive inhibitor of proprotein convertases, including furin/SPC1 (Ki = ~1 nM), SPC2/PC2 (Ki = 0.36 nM), SPC3/PC1/PC3 (Ki = 2.0 nM), SPC4/PACE4 (Ki = 3.6 nM), SPC6/PC5/PC6, and SPC7/LP

JA2120 (NSC81474) is a potent inhibitor of PARG with IC50 of 25.7 μM.

JA2-3 (NSC29192) is a potent dose-dependent inhibitor of PARG with IC50 of 0.1 mM.

GDC-0575, also known as ARRY-575 and RG7741, is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. Chk1 inhibitor GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.

GSK-2807 (GSK 2807, GSK2807) is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki of 14 nM.

GSK2643943A is a potent USP20 inhibitor with IC50 = 160 nM.

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

Akt Inhibitor IV is n Inhibitor of Akt protein kinase

WAY-181187 is a potent and selective 5-HT6 receptor agonist. WAY-181187 possesses high affinity binding (2.2 and 4.8 nM, respectively) at the human 5-HT6 receptor and profile as full receptor agonists (WAY-181187: EC50=6.6 nM, Emax=93%).

VXc-486 is active against drug-resistant isolates, has bactericidal activity, and kills intracellular and dormant M. tuberculosis bacteria in a low-oxygen environment.

VU6012962 (VU-6012962) is a potent, orally bioavailable and CNS penetrant mGlu7 negative allosteric modulator with IC50 of 0.35 uM.

VCMMAE-(PEG)4-DBCO is made by MMAE conjugated to DBCO-(PEG)4-vc-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.

Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.

UK-371804 is a potent and selective uPA inhibitor with excellent enzyme potency (Ki 10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

UAMC00039 dihydrochloride is a potent inhibitor of dipeptidyl peptidase II (DPP-II) (IC50 = 0.48 nM).

U 19963 is a bioactive compound.

The intermediate of ARS-853.ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.

The first small molecule ligand for the VEGF-A receptor neuropilin 1 (NRP1).

TGF-β receptor inhibitor