Ingliforib is a glycogen phosphorylase inhibitor, with IC50s of 52, 352 and 150 nM for liver, muscle and brain glycogen phosphorylase, and has cardioprotective activity.

JBSNF-000088 (6-Methoxynicotinamide) is a small molecule nicotinamide analog that inhibits Nicotinamide N-methyltransferase (NNMT) with IC50 of 1.8, 2.8 and 5.0?μM for human, monkey and mouse NNMT, respectively.

KY-226 (KY226) is a potent, allosteric, orally active inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 uM (human PTP1B), does not exhibit PPARγ agonist activity.

Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling.

ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity.

MRT-68921 hydrochloride (MRT68921) is a potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively.

CP-945598 HCl is a potent and selective cannabinoid type 1 receptor antagonist with Ki of 0.7 nM.

PDM 11 is a potent and selective aryl hydrocarbon receptor (AhR) antagonist.

PF 3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 uM).

Pirozadil is a hypolipidemic agent.

PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 by covalent cysteine modification, without compromising DNA binding.

PK11007 is a thiol-reactive anticancer agent that stabilizes wild type and mutant p53 through selective alkylation of two surface cysteines without interfering with its DNA binding.

PXS-5153A (PXS5153A) is a potent, selective, fast-acting, dual LOXL2/LOXL3 inhibitor with IC50 of <40 nM against all mammalian species LOXL2, inhibits human LOXL3 with IC50 of 63 nM.

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50 = 5.9 nM).

SRI-011381 is an agonist of the TGF-beta signaling pathway for treatment of Alzheimer's disease.

XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50 values of 71.1 ± 12.9 nM and 38.1 ± 6.9 nM against MST1 and MST2, respectively.

Sulfaphenazole is an inhibitor of CYP2C9 (Ki = 0.3 μM) that demonstrates at least 100-fold selectivity over other CYP450 isoforms (Kis = 63 and 29 μM for CYP2C8 and CYP2C18, respectively, and no activity at CYP1A1, CYP1A2, CYP3A4, CYP2C19).

SRT3109 is an antagonist of CXCR2, with a pIC50 of 8.2, and used in the research of chemokine mediated diseases.

PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM.

PIK-75 is a selective cell-permeable inhibitor of PI 3-kinase p110α (IC50 values are 5.8, 76 nM and 1.3 μM at PI 3-kinase p110α, PI 3-kinase p110γ and PI 3-kinase p110β respectively). Inhibits production of PIP2 and PIP3 in adipocytes, phosphorylation of

CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.

β-catenin inhibitor C2 is a novel potent selective β-catenin inhibitor with Kd of 54.96 nM, directly to ARM domain of β-catenin.β-catenin inhibitor C2 reduced viability of DLD1 and SW480 cells in dose-dependent manner with IC50 ranging between 0.8-1.3 uM, viability of HCT116 and SW48 with IC50 3.45-5.35 uM.β-catenin inhibitor C2 selectively inhibits β-catenin, lowers its cellular load and significantly reduces viability of β-catenin-driven cancer cells.

ZY12201 is a potent, selective, orally bioavailable TGR5 agonist with hTGR5 EC50 of 57 pM and mTGR EC50 of 62 pM.ZY12201 displays a favorable pharmacokinetic properties and demonstrated in-vivo glucose lowering effects in animal models (ED50 of 7.9 mg/kg and ED90 of 29.2 mg/kg).

ZJU-37 is a novel small molecule, BBB penetrant RIPK1 kinase inhibitor (IC50=366.4 nM) with higher potency than Nec-1s, prevents TNFα-induced necroptosis of Jurkat FADD−/− cells with IC50 of 185.2 nM.ZJU-37 promotes oligodendrocyte progenitor cells (OPCs) proliferation in vitro with higher efficacy than Nec-1s, enhances remyelination in vivo.ZJU-37 promotes transcription of PDGFRα and proliferation of OPCs via NF-κB.

ZH07 (Dual Mcl-1/Bfl-1 inhibitor 24) is a potent, selective dual Mcl-1 and Bfl-1 inhibitor, binds both Mcl-1 and Bfl-1 with Ki of 97 nM and 100 nM, respectively.ZH07 displays appreciable selectivity (>250-fold) over Bcl-2/Bcl-xL.ZH07 induces dose-dependent disruption of interactions between BL-Bim and endogenous Mcl-1 and Bfl-1, without affecting the complexes between BL-Bim and Bcl-2 or Bcl-xL.ZH07 demonstrates on-target cellular activity in model lymphoma cell lines.

Zevaquenabant ((S)-MRI-1867) is a peripherally restricted, orally bioavailable dual CB1 receptor/iNOS inhibitor.Zevaquenabant ((S)-MRI-1867) (3 mg/kg, p.o.) ameliorated obesity-induced kidney morphological and functional changes via decreasing kidney inflammation, fibrosis, oxidative stress, and renal injury.The hybrid CB1R/iNOS inhibitor Zevaquenabant ((S)-MRI-1867) has greater antifibrotic efficacy than inhibition of CB1R alone.(S)-MRI-1867 reduced hepatic steatosis and the rate of hepatic VLDL secretion, upregulated hepatic LDLR expression, and reduced the circulating levels of proprotein convertase subtilisin/kexin type 9 (PCSK9) in diet-induced obesity (DIO mice).

Zebularine (NSC309132, 4-Deoxyuridine) is a nucleoside analog of cytidine and inhibitor of cytidine deaminase, also inhibits DNA methylation and tumor growth both in vitro and in vivo.

ZE132 is a potent and selective small-molecule inhibitor of PD-1/PD-L1 interaction with IC50 of <0.1 nM.ZE132 effectively inhibits the PD-1/PD-L1 interactions in vitro, and has a potent affinity to PD-L1.ZE132 shows robust anti-tumour effects in vivo, better than anti-PD-1 antibody.ZE132 treatment promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression.ZE132 elicits strong inhibitory effects on the mRNA expression of TGF-β.

ZB-R-55 is a potent and selective RIPK1 inhibitor with IC50 of 5.7 nM, 10-fold more potent than GSK2982772.ZB-R-55 is a dual-mode RIPK1 inhibitors occupying both the allosteric and the ATP binding pockets.ZB-R-55 exhibits excellent kinase selectivity, good oral pharmacokinetics and good therapeutic effects in the LPS-induced sepsis model.

YX-I-1 is a small-molecule modulator of human islet amyloid polypeptide (hIAPP) assembly, specifically inhibits amyloid formation; YX-I-1 inhibits the aggregation of wt hIAPP, extending the t50 from 15.1 ± 0.2 h to 23.4 ± 1.0 h at a 1:7 molar ratio of peptide:inhibitor. YX-I-1 inhibits primary nucleation, secondary nucleation and elongation of wt hIAP. YX-A-1 is a useful chemical tools to study hIAPP aggregation.