APOL1-IN-1 is a apolipoprotein L1 (APOL1) inhibitor extracted from patent WO2020131807A1 compound 87. APOL1-IN-1 can be used for the research of focal segmental glomerulosclerosis (FSGS) and non-diabetic kidney disease (NDKD)[1].

CDC801 is a potent and orally active phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α) inhibitor with IC50 of 1.1 μM and 2.5 μM, respectively.

CARM1-IN-7g is a potent, selective coactivator-associated arginine methyltransferase 1 (CARM1) with IC50 of 8.6 uM, exhibits lower or no activity against a panel of different PRMTs or HKMTs (>80-fold over PRMT1 and SET7).

A novel potent and selective TGF-βRI (ALK5) inhibitor with IC50 of 4.83 nM, dispalys >300-fold selectivity over p38α.

A potent Nrf2 activator that upregulates Nrf2 expression and resulted in translocation of Nrf2 into the nucleus..

ARD2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.

AZD0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders.

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.

WC36 is a novel nonlipidic inhibitor of the lipid-SH2 domain interaction. WC36 is effective against RAS-mutated HL-60 AML cells that shows de novo resistance to entospletinib.

D11 is a potent and selective inhibitor of protein kinase CK2 with Ki of 5 nM.

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.

Comopound X1 (Xist) binds the non-coding RNA prototype Xist, specifically the RepA motif, with Kd of 0.4 μM. X1 binding reduces the conformational space of RepA, displaces cognate interacting protein factors (PRC2 and SPEN), suppresses histone H3K27 trimethylation, and blocks initiation of X-chromosome inactivation.

Compound 16 (UNC-CA94) is a reversible inhibitor of PKN3 with IC50 of 14 nM. Compound 16 (UNC-CA94) is a potential tool compound to study the cell biology of PKN3.

S3-15 selectively interrupts soluble RANKL-RANK interaction and without interfering with the membrane RANKL-RANK interaction. S3-15 exhibits anti-osteoporotic effects without causing immunosuppression.

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.

ML901 is a specific reagent that hijacks a single aminoacyl transfer RNA (tRNA) synthetases (aaRSs) in the malaria parasite Plasmodium falciparum. ML901 inhibits the growth of the malaria parasite Plasmodium falciparum in vitro and in animals but was not toxic to human cells.

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.

N-0385 is a novel highly potent inhibitor of TMPRSS2-like proteases (IC50 = 1.9 nM) that blocks SARS-CoV-2 VOCs (B.1.1.7, P.1, B.1.351 and B.1.617.2) and is broadly protective against infection and mortality in mice. N-0385 demonstrates potent inhibition of SARS-CoV-2 infection in Calu-3 cells with EC50 of 2.8 nM and a SI of > 10E6.

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].