AVN-101 is a potent 5-HT7 receptor antagonist.

UK-101 is a potent and selective inhibitor of the immunoproteasome LMP2, inhibiting β1i (LMP2), β1c (LMP2), and β5 (LMP2), with IC50s of 104 nM, 15 μM, and 1 μM. UK-101 has a 144-fold and 10-fold higher affinity for β1i than for the distribution of β1c and β5 subunits. UK-101 induces apoptosis and can be used to study prostate cancer related diseases.

KHS101 is a novel inhibitor of transforming acidic coiled-coil protein 3 (TACC3). It is a selective inducer of neuronal differentiation.

UFP-101 acetate is a selective and competitive antagonist of the NOP receptor (pKi = 10.24) with >3000-fold selectivity over δ, μ, and κ opioid receptors.

KYN-101 is a potent, selective synthetic antagonist of aryl hydrocarbon receptor (AHR) with IC50 of 22 nM in human HepG2 DRE-luciferase reporter assay and 23 nM in murine Hepa1 Cyp-luc assay.KYN-101 reverses IDO/TDO-mediated tumor progression and improves the efficacy of PD-1 blockade in B16 IDO tumor-bearing mice, as well as CT26 colorectal cancer model expressing endogenous high levels of IDO.

XY101 is a selective, metabolically stable and orally available agonist of RORγ inverse(IC50 of 30 nM and a Kd of 380 nM).

GlyH-101 is a cell-permeable glycinyl hydrazone compound that blocks CFTR with Ki of 1.4 uM.

ULK-101 is a potent and selective ULK1 inhibitor ( IC50s: 8.3/30 nM for ULK1/ULK2). It can suppress autophagy.

Retrocyclin-101 is an antimicrobial peptide with activity against bacterial and viral pathogens [1].

Anticancer Agent 101, a tetracaine derivative, exhibits anti-cancer activity [1].

PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET. It impedes RET function, promoting autophagic breakdown of FLT3, and suppresses the PI3K and Ras/ERK pathways, contributing to its anti-leukemic effects. The compound's antitumor efficacy is demonstrated in both a mouse MV4-11 flank xenograft model (doses of 3 and 10 mg/kg; po) and an allogeneic xenograft mouse model (dose of 40 mg/kg; po) [1].

OY-101, an orally active compound, serves as a potent and specific inhibitor of P-glycoprotein (P-gp). It has the capability to sensitize drug-resistant tumors and counteract tumor multidrug resistance efficiently. Compared to Tetrandrine [1], OY-101 demonstrates enhanced water-solubility, cytotoxicity, and reversal activity.

PHI-101, an orally active FLT3 inhibitor, effectively overcomes resistance associated with numerous drug-resistant mutations. It potently suppresses both single activating FLT3 mutations (ITD or TKD mutants) and inhibits double (ITD/D835Y or ITD/F691L) as well as triple (ITD/D835Y/F691L) resistance mutations. This compound shows promise for investigation in the context of relapsed or refractory acute myeloid leukemia (AML) [1].

EVT-101 is a GluN2B antagonist, binding at the same GluN1/GluN2B dimer interface as ifenprodil but adopting a remarkably different binding mode involving a distinct subcavity and receptor interactions.

(R)-(-)-Gossypol acetic acid (AT101 acetate) , the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID. Phase 2.

PKUMDL-LC-101-D04 is a potent allosteric activator of glutathione peroxidase 4 (GPX4), a regulator of iron death. GPX4 activity was increased to 150% of control levels when used at a concentration of 20 μM in a cell-free assay, and at a concentration of 61 μM in wild-type, but not Gpx4-/-, mouse embryonic fibroblast (MEF) extracts.PKUMDL-LC-101-D04 (200 μM) reduced cholesterol peroxide-induced MEF death.

RG-101 is a hepatocyte-targeted N-acetylgalactosamine conjugated oligonucleotide that functions as an antagonist for miR-122, an essential host factor in the replication of the hepatitis C virus (HCV).

KHS101 is a TACC3 inhibitor and can selectively induce a neuronal differentiation phenotype.

ORP-101 is a new chemical entity designed with intent to create a large stable molecule and to confer partial μ agonist and full κ-antagonist receptor pharmacology.

AQ-101 is a inhibitor of MDM2, which induces MDM2 protein degradation through a self-ubiquitination and proteasome-mediated mechanism.

INU-101 is an 11β-HSD1 inhibitor. In KKAy mice, ob/ob mice, and ZDF rats, oral administration of INU-101 led to enhanced insulin sensitivity and the lowering of the fasting level of glucose in the blood. INU-101 therefore shows promise as a potential treatment for type 2 diabetes and metabolic syndrome.

Antibacterial agent 101 exhibited antibacterial and antifungal effects (MIC=4-32 μg/mL).

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

Thr101, also known as NOX Inhibitor VII, is a dose-dependent inhibitor of HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9. Thr101 is also a NOX inhibitor.

VH 101, acid, a functionalized von-Hippel-Lindau (VHL) protein ligand, facilitates PROTAC research and development. It comprises an E3 ligase ligand and an alkyl linker featuring a terminal amine for easy conjugation to target protein ligands [1].

UWA-101 hydrochloride is a selective, non-cytotoxic inhibitor of DAT/SERT, demonstrating EC50 values of 3.6 µM for DAT and 2.3 µM for SERT inhibition. It mitigates motor disorders and other side effects associated with dopaminergic agent use (e.g., L-DOPA) without exhibiting psychotropic effects. This compound is utilized in research focused on neurodegenerative conditions like Parkinson's disease [1] [2].

FOBISIN101 is a novel inhibitor of all 14-3-3 isoforms in 14-3-3 PPIs.

CXD101 is a novel class I-selective HDACi (HDAC1 (IC50 : 63nM), HDAC2 (IC50 :570nM), HDAC3 (IC50 :550nM)). CXD101(CXD-101) has no activity against HDAC class II

Complement component C3 plays a particularly versatile role in this process by keeping the cascade alert, acting as a point of convergence of activation pathways, fueling the amplification of the complement response, exerting direct effector functions, and helping to coordinate downstream immune responses[3]. In C3-/- mice alcohol-induced liver steatosis is absent or strongly reduced after chronic or acute alcohol exposure. This suggests that the complement system and its component C3 contribute to the development of alcohol-induced fatty liver and its consequences[4].AMY-101 TFA (Cp40 TFA) is a peptidic inhibitor of the central complement component C3 (KD: 0.5 nM). It shows a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation[5].a daily subcutaneous dose of AMY-101 (4 mg/kg bodyweight) was protective against NHP periodontitis, suggesting that patients treated for systemic disorders (e.g., paroxysmal nocturnal hemoglobinuria) can additionally benefit in terms of improved periodontal condition[6].Plasma concentrations of both C3 and Cp40 were measured periodically and complete saturation of plasma C3 was confirmed. No differences in hematological, biochemical, or immunological parameters were identified in the blood or tissues of animals treated with Cp40 when compared to those injected with vehicle alone. Further, skin wounds showed no signs of infection in those treated with Cp40.Cp40 treatment was associated with a trend toward accelerated wound healing when compared with the control group. In addition, a biodistribution study in a rhesus monkey indicated that the distribution of Cp40 in the body is associated with the presence of C3, concentrating in organs that accumulate blood and produce C3[7].

CAL-101 (Idelalisib) is a selective inhibitor of p110δ(IC50 : 2.5 nM; in cell-free assays); shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

UCPH-101 is an inhibitor of excitatory amino acid transporter subtype 1 (EAAT1) with an IC50 of 0.66 μM.

Antitumor agent-101 is a selective, covalent inhibitor targeting lysine methyltransferases G9a/GLP, demonstrating IC50 values of 8.5 nM for G9a and 5.5 nM for GLP. It exhibits antitumor efficacy in the PANC-1 xenograft model [1].

EVT-101, also known as ENS-101, is an experimental medication which originated from Roche and is under development by Evotec AG for the treatment of major depressive disorder. It acts as a selective NMDA receptor subunit 2B (NR2B) antagonist.

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC6 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

LEI 101 hydrochloride is potent and selective CB2 partial agonist.

VMY-1-101 is a synthesized fluorescent CDK inhibitor. VMY-1-101 demonstrates potent CDK inhibitory activity, enhanced induction of G2/M arrest and modest apoptosis as compared to purvalanol B.

VT101 is a TEAD Auto-palmitoylation inhibitor that Selectively Inhibit Proliferation and Tumor Growth of NF2-deficient Mesothelioma. VT101 inhibited the firefly luciferase reporter dose-dependently and had no 204 effect on the Renilla luciferase reporter.

CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.

NDMC101 is an inhibitor of dipeptidyl peptidase-IV activity in human T cells and exhibits immunomodulatory effects. It also acts as a novel inhibitor of NFATc1 and NF-κB activity.

Caveolin-1 (82-101) amide (human, mouse, rat), also known as Caveolin-1 scaffolding domain peptide, mitigates aging-related detrimental alterations in various organs and inhibits tyrosine kinases [1].

Sulforhodamine 101 DHPE, a fluorescent probe, results from the conjugation of sulforhodamine 101, a red fluorescent dye with excitation/emission spectra of 586/605 nm, to the phospholipid 1,2-dipalmitoyl-sn-glycero-3-PE. It effectively integrates into phospholipid bilayers and is utilized for imaging solid supported lipid bilayers, detecting protein-ligand interactions on bilayers, and monitoring lipid probe colocalization in liposomes through resonance energy transfer (RET).

AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a multi-target drug candidate for the treatment of CNS disorders.

Functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkylC4 linker with terminal amine ready for conjugation to a target protein ligand. Part of a range of functionalized tool molecules for PROTAC R&D. PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

S101 is an inhibitor of proliferating T-cells, rescuing mice from superantigen-induced shock.

UCF 101 is a specific inhibitor of HtrA2 and reduces apoptosis in PC12 cells.

Ossirene (AS101), a potent in vitro and in vivo immunomodulator, is a novel inhibitor of IL-1beta converting enzyme.

VH 101, a thiol (compound 20), serves as a VHL ligand essential for PROTAC synthesis [1].

UFP101 is a synthetic peptide that functions as an antagonist of the nociceptin receptor, demonstrating high affinity with a Ki of 0.06 nM in CHO cells expressing the human receptor. It exhibits selectivity for the nociceptin receptor over the κ-opioid receptor, with a Ki of 204 nM in CHO cells expressing the rat receptor. The compound effectively inhibits GTPγS release from the nociceptin receptor in CHO cell membranes, with an EC50 of 1.86 nM. When administered intracerebroventricularly at a dose of 10 nmol/animal, UFP101 prolongs the latency to tail withdrawal in the tail-flick test in mice, indicating its potential as an analgesic. Additionally, at doses of 0.003, 0.03, and 0.3 mg/kg, UFP101 enhances survival in a sepsis mouse model induced by cecal ligation and puncture, suggesting potential therapeutic applications in sepsis management.

UFP-101 TFA is a potent, selective, and competitive N/OFQ peptide (NOP) receptor antagonist, boasting a pK i value of 10.24 and demonstrating over 3000-fold selectivity against δ, μ, and κ opioid receptors. It exhibits antidepressant-like effects [1] [2].

NIP-101 is a potent calcium antagonist.