Oncrasin 1 is a proapoptotic substance. Induces abnormal nuclear aggregation of PKCι and suppressing RNA transcription.

Z-944 is a potent, highly selective and oral T-type calcium channel blocker with IC50 of 50-160 nM for human Cav3.1, Cav3.2, and Cav3.3 channels.

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..

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

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.

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.

cis-Epoxysuccinic acid is a succinate receptor (SUCNR1/GPR91) agonist. cis-Epoxysuccinic acid inhibits cAMP levels with an EC50 value of 2.7 µM. cis-Epoxysuccinic acid can be used for the research of cardiovascular system.

ND-654 (ND654) is a novel potent, liver-specific acetyl-CoA carboxylase (ACC) inhibitor with IC50 of 3/8 nM for human ACC1/ACC2, 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.

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].

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

SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.

SPP-86 is a potent RET inhibitor.

Ro 60-0175 is a potent, selective 5-HT2C receptor agonist with pKi of 9, 7.5, 5.4, 5.2 and 5.6 for human 5-HT2C, 2A, 1A, 6 and 7 receptors respectively.

Bretazenil, also known as Ro 16-6028, is GABA A receptor agonist potentially for the treatment of anxiety disorders. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α1, α2, α3, α4, α5 and α6 subunit containing GABAA receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α1, α2, α3 and α5 GABAA benzodiazepine receptor complexes.

CAY10444 (BML-241) is a sphingosine-1-phosphate 3 (S1P3) antagonist. CAY10444 inhibits by 37% S1P-induced increases in Ca2+ in HeLa cells expressing S1P3 receptors[1].

NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.

Kira8 is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α’s RNase.

JT010 is a potent agonist of TRPA1 with an EC50 of 0.65 nM.

HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells.

CP-24879 hydrochloride is a D5D/D6D dual-inhibitor, showing beneficial effects against increased intracellular lipid accumulation and inflammatory injury in hepatocytes.

A novel LTA4 hydrolase (LTA4H) inhibitor that inhibits LTB4 synthesis in human neutrophils with IC50 of 0.5 uM.

A novel FTY720 analog that acts as PP2A activator, disrupts the SET/PP2A interaction devoid of immunosuppressive effects leads to the reactivation of PP2A.

AM-2232 is a drug that acts as a potent but unselective agonist for the cannabinoid receptors.

SB02024 is a novel highly potent, selective, ATP competitive, orally active inhibitor of vacuolar protein sorting 34 (Vps34) with Kd of 1 nM, >1000 times selective towards other PI3K isoenzymes; SB02024 is also highly selective at 1 uM in the DiscoveRx ScanMax panel of 468 kinases; reduces the number of GFP-2xFYVE puncta with IC50 of 14 nM, induces a dose-dependent increase in levels of NCOA4 and p62; blocks autophagy in vitro and reduces xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7; also significantly potentiates cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro.

MRS 1845 is a potent calcium channel protein inhibitor and inhibits capacitative Ca2+ influx in HL-60 cells (IC50 = 1.7 mM).

Guanabenz (WY 8678) is an α2 adrenergic receptor agonist that is used as an antihypertensive agent, also has been proposed to exert protective effects against misfolding by interfering with eIF2α-P dephosphorylation through selective disruption of a PP1-P