Citalopram is marketed as a racemate mixture of the S(+)-enantiomer and R(-)-enantiomer and the active S(+)-enantiomer (Escitalopram) that possess inhibitory effects. Citalopram is an antidepressant and enhances serotoninergic neurotransmission through potent and selective inhibition of serotonin reuptake (selective serotonin reuptake inhibitor).

Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively).

RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC50s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research.

RET-IN-9 is a potent inhibitor of RET. RET kinase is a single-pass transmembrane receptor tyrosine kinase that plays an important role in the development of the kidney and enteric nervous system, and the maintenance of homeostasis in the nervous, endocrine, hematopoietic, and male reproductive systems. RET-IN-9 has the potential for the research of RET-related disease including non-small cell lung cancer and medullary thyroid cancer (extracted from patent WO2021115457A1, compound 29).

RET-IN-15 is a rearranged during transfection (RET) kinase inhibitor extracted from patent WO2021115457A1 compound 51. RET-IN-15 can be used for the research of cancer.

RET-IN-8 is a rearranged during transfection (RET) kinase inhibitor extracted from patent WO2021093720A1 compound I-1. RET-IN-8 can be used for the research of cancer.

TCO-PEG2-Sulfo-NHS ester sodium is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

DBCO-PEG6-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo.

(S)-ABBV-CLS-484 is a potent PTPN1 or PTPN2 inhibitor.

SHP2 inhibitor is an effective SHP2 allosteric inhibitors (IC50≤50 nM), blocking the activation of SHP2 by targeting the auto-inhibited conformation of SHP2 (WO2019183367A1, compound 118).

Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts.

Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases.

P-gp inhibitor 3 is an effective P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 3 inhibits the efflux function of P-gp by activating P-gp ATPase. P-gp inhibitor 3 has relatively stronger multidrug resistance (MDR) reversal ability and enhances the anti-tumor activity of Paclitaxel.

P-gp inhibitor 2 is a potent P-gp inhibitor. P-gp inhibitor 2 shows reverse Doxorubicin resistance (IC50=0.22 µM) in P-gp overexpressing human colorectal carcinoma cells (SW600 Ad300).

Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1).

TCS-OX2-29 (hydrochloride) is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1.

iNOs-IN-1 (YPW) is a potent inducible nitric oxide synthase (iNOS) inhibitor. iNOs-IN-1 can significantly inhibit the expression of IL-6 and iNOS, as well as reduce LPS-induced NO generation with dose-dependent manner in mouse macrophages. Anti-inflammatory effects.

8A8 is a potent proinflammatory factor NO inhibitor with an IC50 of 4.7 μM. 8A8 also significantly inhibits LPS-induced HaCat cell proliferation.

PD-334581 is a MEK1 inhibitor.

NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53.

Mutant p53 modulator-1 is a mutant p53 modulator. Mutant p53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B).

PK9327 is a small-molecule stabilizer targeting cavity-creating p53 cancer mutations.

Monoacylglycerol lipase inhibitor 1 is a potent monoacylglycerol lipase inhibitor (compound 13).

LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM.

Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research.

IL-17 modulator 6 (compound 61) is a potent Interleukin 17 (IL-17) modulator (pIC50=9.1). IL-17 modulator 6 has the ability to inhibit IL-17 and can be used for the treatment of inflammatory and autoimmune diseases.

GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties.

HSP70-IN-3 is a potent HSP70 inhibitor (IC50s of 1.1 and 1.9 μM in ASZ001 and C3H10T1/2, respectively). HSP70-IN-3 has anti-Hh (Hedgehog signaling) activity and anti-proliferative activity and reduces expression of the oncogenic transcription factor GLI1.

HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2).