T6253

Talazoparib (LT-673) is a new-type PARP inhibitor (IC50: 0.58 nM), It similarly binds to PARP1/2 (Kis: 1.2/0.85 nM).

N-Arachidonyldopamine (NADA) is a selective and potent endogenous CB1 receptor agonist (Ki: 250 nM).N-Arachidonyldopamine is also a potent and selective TRPV1 agonist with an EC50 value of ~50 nM.

TRK-IN-12 (Compound 9e), a macrocyclic derivative, is a potent TRK inhibitor, with efficacy against TRK G595R (IC 50 = 13.1 nM). It demonstrates significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC 50 = 0.080 μM) and exhibits superior inhibitory performance (IC 50 = 0.646 μM) compared to the control agent LOXO-101 in the Ba/F3-LMNA-NTRK1-G595R cell line [1].

MRS2395 is a dipivaloyl derivative and a potent antagonist of the P2Y12 receptor. MRS2395 inhibited ADP-induced platelet activation (Ki: 3.6 μM). MRS2395 enhances platelet dense granule release in response to TRAP-6.

MALT1-IN-8 is a potent inhibitor of MALT1 protease (IC50: 2 nM) that inhibits the growth of OCI-LY3 lymphoma cells (IC50: 1.16 μM) and exhibits anticancer activity.

POP-IN-2 (Compound 7k) is a potent covalent inhibitor of prolyl oligopeptidase (POP) with a Ki of 6 nM, suitable for neurodegenerative disease and cancer research.

ZINC09659342 (compound 13) is an inhibitor of the Lbc-RhoA interaction with an IC50 value of 3.6 μM.

S100P-IN-1 is a potent S100P inhibitor.S100P-IN-1 has anti-metastatic effects on pancreatic cancer (pancreatic) cells.

Antimalarial agent 7 is a potent and effective inhibitor of PfATP4, showing potential for studying human Plasmodium falciparum.

AChE-IN-15 (Compound 3d) is a reversible inhibitor of human acetylcholinesterase (huAChE) and human butyrylcholinesterase (huBChE), exhibiting IC50 values of 6.8 μM for huAChE and 16.1 μM for huBChE, and demonstrates significant antioxidant activity. The compound has potential applications in the treatment of Alzheimer's disease.