Philanthotoxin 74 dihydrochloride (PhTx 74) is an AMPAR antagonist; inhibits GluR3 and GluR1 with IC50s of 263 and 296 nM, respectively.

MCB-613 is a novel and potent stimulator of p160 steroid receptor coactivators (SRCs). It is a Pan-SRCs stimulator.

The first in a class, potent and highly selective, direct renin inhibitor with IC50 of 0.6 nM.

Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect.

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

Pimavanserin, also known as ACP-103, is a non-dopaminergic atypical antipsychotic for the treatment of Parkinson's disease psychosis and schizophrenia. Pimavanserin has a unique mechanism of action relative to other antipsychotics, behaving as a selective inverse agonist of the serotonin 5-HT2A receptor, with 40-fold selectivity for this site over the 5-HT2C receptor and no significant affinity or activity at the 5-HT2B receptor or dopamine receptors. It was approved by the FDA to treat hallucinations and delusions associated with psychosis experienced by some people with Parkinson's disease on April 29, 2016.

CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice.

NKTP-3 is a potent, selective, biostable, and cell-permeable cyclic d-peptide that targets NRP1 and KRASG12D with binding affinity of 116.28 nM and 50.34 nM, respectively. NKTP-3 shows good biostability and a strong cellular uptake ability and further demonstrated its antitumor effect on lung cancer with the KRASG12D mutation in vitro and in vivo.

IDP-410 is a novel therapeutic peptide that target directly N-MYC protein. IDP-410 peptide acts by reducing the interaction of N-MYC with its partner MAX and favoring the degradation of the protein.

DCC-3014(Vimseltinib) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively.

INCB086550 is an orally available, small molecule inhibitor of PD-L1 with potential immune checkpoint inhibitory and antineoplastic activities. In vitro, INCB086550 selectively and potently blocked the PD-L1/PD-1 interaction, induced PD-L1 dimerization and internalization, and induced stimulation-dependent cytokine production in primary human immune cells. In vivo, INCB086550 reduced tumor growth in CD34+ humanized mice and induced T-cell activation gene signatures, consistent with PD-L1/PD-1 pathway blockade. Preliminary data from an ongoing phase I study confirmed PD-L1/PD-1 blockade in peripheral blood cells, with increased immune activation and tumor growth control.

TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration.

Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily[1].

RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.

BAY 6035 is a potent and selective SMYD3 inhibitor.

NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets.

TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.

KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2

ACT-541468 is a dual orexin receptor antagonist.

Sodium channel blocker. Suppresses tetrodotoxin (TTX)-resistant Na+ currents approximately twice as selectively as TTX-sensitive currents. Antinociceptive; displays analgesic effects in animal models of inflammatory and neuropathic pain.

EB-42486 is a novel, potent, and highly selective G2019S-LRRK2 inhibitor (IC50 < 0.2 nM).

ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.