Balovaptan (RG7314) is an orally available, selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.

A potent GIRK2 inhibitor that inhibits GIRK2-mediated flux with an IC50 of 0.35 uM.

Alintegimod (7HP349) is a small molecule activator of the integrins αLβ2 (LFA-1) and α4β1 (VLA-4). 7HP349 directly activates integrin cell adhesion receptors crucial for the generation of an immune response.

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal effect on widetype TEAD1, TEAD1 C359S and TEAD3 C371A mutants, demonstrated selective cellular engagement with Cys371 of TEAD3.DC-TEAD3in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD (1–4) reporter assays with IC50 of 1.15 uM in cellular assays.DC-TEAD3in03 reduced the growth rate of zebrafish caudal fins when administered to zebrafish juveniles.In the Hippo signaling pathway, the transcription factor TEA domains (TEADs) family proteins (TEAD1‒4) are the most important terminal regulators, which play an important role in development, cell proliferation, cell differentiation, tissue homeostasis, and regeneration.

IBG1 is a PROTAC-like degrader, which comprises JQ1 tethered to E7820. IBG1 selectively degraded BRD2 and BRD4 but not BRD3. IBG1 results in potent BRD4 degradation with DC50 of 0.15 nM and pronounces growth inhibition in various cancer cell lines.

IBG4 is a PROTAC-like degrader. IBG4 shows high specificity for BRD4 and does not efficiently degrade BRD2.

LNK01003(Example 4) is a selective and potent JAK inhibitor.

GSK 3011724A (DG-167, GSK-3011724A) is a potent, specific inhibitor of β-ketoacyl-ACP synthase (KasA, Kd=9 nM), shows anti-tubercular activity (MIC H37Rv=0.8 uM); shows much weaker apparent dissociation constant for both Pks10 and Pks (Kd=1.4 uM); inhibits mycolic acid biosynthesis and shows negligible activity against a panel of unrelated proteins and 18 Gram-positive and Gram-negative bacterial species.

Compound 181 is a selective and highly potent stabilizer of the 14-3-3σ/ERα complex. Compound 181 shows potency comparable to the natural product Fusicoccin-A.

RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction.

PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.