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

SU 4313 is a bioactive chemical.

SR-14150 is a potent NOP/μ-opioid partial agonist with Ki of 1.39 nM and 29.9 nM, respectively.

Spastazoline is a potent and selective spastin (a microtubule-severing AAA protein) inhibitor, with an IC50 of 99 nM for Human spastin. Spastazoline shows no effect on ATPase activity of a recombinant human VPS4.

SNG-1153 is a synthetic modulator of ER-α36