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Nur77 modulator 1 is an effective Nur77 binder (KD = 3.58 μM) that up-regulates Nur77 expression, mediates its sub-cellular localization, induces Nur77-dependent ER stress and autophagy, and leads to cell apoptosis, demonstrating anti-hepatoma activity.

Goodyeroside A is a natural glycoside that inhibits liver damage caused by substances such as carbon tetrachloride, and is also effective in suppressing inflammation by inhibiting the NF-κB signalling pathway.

DI-87 (TRE-515) is a novel and orally available dCK (deoxycytidine kinase) inhibitor with good in vitro activity and low protein binding. DI-87 binds to dCK and prevents the phosphorylation of deoxycytidine by dCK, which reduces the production of dNTP and cell cycle arrest (especially in S phase). When combined with thymidine, DI-87 significantly inhibits tumor growth.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

DC_C66 DC_C66 has good selectivity for CARM1, PRMT1 (IC50 = 21μM), PRMT6 (IC50 = 47μM) and PRMT5. It is a cell-permeable, selective co-activator related arginine methyltransferase 1 (CARM1) inhibitor with IC50 of 1.8 μM.

DSP-0565 exhibits anti-convulsant activity and good safety margin in various models including scPTZ, 6 Hz, MES, and amygdala kindling. DSP-0565 can be used in studies about acting as a broad-spectrum anti-epileptic drug.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK/PD characteristics and can be used to study pulmonary fibrosis.

Ibafloxacine (R835) is a fluoroquinolone antibiotic used exclusively in veterinary medicine and exhibits no bacteriostatic effect against Bartonella.

(Rac)-Acolbifene (EM-343) is the racemic form of Acolbifene. Acolbifene is a estrogen receptor antagonist. (Rac)-Acolbifene exhibits anti-estrogenic and estrogenic activities. (Rac)-Acolbifene contains a piperidine ring and exhibits good pharmacological profile,relative binding affinity (RBA)=380.

TPN171 is potent PDE5 inhibitor with subnanomolar potency for PDE5 and good selectivity over PDE6, which has the potential for the treatment of pulmonary arterial hypertension (PAH). TPN171 was proven to exert a longer lasting effect than sildenafil in animal models, providing a foundation for a once-daily oral administration for its clinical use.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

CCT367766 is a potent, PROTAC-based, third-generation, iso-functional pirin-targeted protein degradation probe (PDP) that depletes pirin expression at low concentrations.CCT367766 has an IC50 value of 490 nM for the CRBN-DDB1 complex.CCT367766 has a good affinity for recombinant pirin and CRBN. CCT367766 has a good affinity for recombinant pirin and CRBN, with Kd values of 55 nM and 120 nM, respectively. cct367766 is a potent orally active protein that reduces the expression of pirin at low concentrations.

ATPγS tetralithium salt is a good substrate for RNA-stimulated nucleotide hydrolysis and RNA unwinding activity of eIF4A.

ML400 (CID73050863) is an allosteric inhibitor of LMPTP with an EC50 of 1μM. ML400 displays good cell-based activity and rodent pharmacokinetics.

Rufigallol (AI3-00865) is an electron-deficient disk-shaped molecule with six hydroxyl groups and is a good unit for inducing the formation of DLC from non-planar AIE molecules, an anthraquinone derivative.Rufigallol induces the acquisition of DLC properties, while the introduction of TPE groups gives the molecular structure good fluorescence in the aggregated state.The remarkable synergistic in vitro antimalarial effect, in vivo with vitamin C and ketones was synergistic and showed antimalarial activity.

CCT365623 is an orally bioavailable Lysyl Oxidase inhibitor with good anti-LOX potency, selectivity, pharmacokinetic properties, as well as anti-metastatic efficacy.

Olorofim(F-901318)is a novel selective antifungal compound targeting pyrimidine biosynthesis in mycobacteria, with inhibitory effect on Aspergillus fumigatus DHODH (IC50: 44 nM), but little inhibitory effect on human DHODH (>100 uM).Olorofim has good efficacy against a variety of pathogenic filamentous and dimorphic fungi, such as Penicillium spp, P. dermatitidis spp and Fusarium spp.

CCR2 antagonist 5 (JNJ-41443532) is a selective and orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM).JNJ-41443532 binds mCCR2 with a Ki of 9.6 µM, which can be used to study inflammatory diseases and diabetes. diseases and diabetes.

KRP-199, a highly potent and selective antagonist for the AMPA receptors, exhibits good neuroprotective effects in vivo.

KRP-199 sodium sodium is highly potent and selective for AMPA-R in vitro and exhibits good neuroprotection in vivo.

rac-CCT-250863 HCl is a selective and reversible inhibitor of NEK 2. rac-CCT-250863 HCl induces cell cycle arrest and has good anti-proliferative activity against cancer cells. rac-CCT-250863 HCl can be used in combination with Pomalidomide to induce apoptosis and can be used in combined anti-cancer studies.

Setrobuvir (ANA-598) is an orally active non-nucleoside HCV NS5B polymerase inhibitor with inhibitory effects on de novo RNA synthesis and primer extension with IC50s between 4 and 5 nM. setrobuvir shows good binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp.

Soquinolol (Soquinolol mucate) is a beta-adrenergic receptor antagonist with weak local anesthetic activity.Soquinolol has good enteral efficacy and a long duration of action.