SCH-23390 is a dopamine D1-like receptor antagonist (with Ki values of 0.2 nM and 0.3 nM for the D1 and D5 receptor subtypes, respectively). SCH-23390 can shorten the latency period for cocaine-induced lever pressing behavior in rats. SCH-23390 can also eliminate generalized seizures caused by chemical convulsants, such as arecoline and strychnine, and is used in research on neurological disorders related to the dopamine system.

Novel, Potent and Selective Histone Methyltransferase SET7 Inhibitor

A potent, selective, allosteric CCR2 antagonist with binding IC50 of 5.1 nM.

Linopirdine (DuP 996) is an orally active, selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor with an IC50 of 2.4 μM. Linopirdine is a TRPV1 agonist. Linopirdine, a putative cognition enhancing agent, increases acetylcholine release in rat brain tissue.

SOD1-Derlin-1 inhibitor 56-59 is a cell-permeable, small molecule inhibitor of SOD1-Derlin-1 interaction, target SOD1 DBR and clearly attenuates the interactions of Derlin-1 with 122 types of SOD1mut in the cell-based co-immunoprecipitation assay.

GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca2+ release assay, respectively.

NCRW0005-F05 is a small-molecule inhibitor reported to target the Wnt/β-catenin signaling pathway with activity in vitro. It suppresses β-catenin–dependent transcription in a concentration-dependent manner, with reported IC50 values in the low micromolar range (~1–10 µM) in reporter assays. NCRW0005-F05 reduces expression of Wnt target genes such as c-Myc and cyclin D1, leading to decreased proliferation in Wnt-driven cancer cell models.

NPD4928 (NPD 4928) is a small molecule that enhances ferroptosis via inhibition of ferroptosis suppressor protein 1 (FSP1).NPD4928 enhanced the sensitivity of various cancer cells to GPX4 inhibitor RSL3.

ONT-093, also known as OC-144-093, is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy. ONT-093 could inhibit P-gp and reverse multidrug resistance at nM concentrations with no effect on paclitaxel pharmacokinetics. OC144-093 is the least non-specifically toxic Pgp inhibitor described to date, with an average cytostatic IC50 of >60 microM in 15 cell types. OC144-093 may represent an ideal candidate for use in enhancement of AED blood-brain barrier penetration.

BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab, anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer.

EDI048 (compound 1.16) is an orally active Cryptosporidium PI4K inhibitor for the research of cryptosporidiosis.

ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects.

BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 81 nM. BAY-8400 shows synergistic activity of DNA-PK inhibition when combined with DNA damage inducing cancer therapy, like targeted alpha radiation.

Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM.

KCNQ2/3 activator-1 is an activator of Kv7.2/Kv7.3 (KCNQ2/3) potassium channel. KCNQ2/3 activator-1 has the potential in relieving pain (the main problem from medical treatment) (extracted from patent WO2021113757A1, compound A).

BRD0639 is a first-in-class inhibitor of the PRMT5-substrate adaptor interaction. BRD0639 is a PRMT5 binding motif (PBM)-competitive agent that can support studies of PBM dependent PRMT5 activities.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor.

Quorum sensing modulator as a PqsR antagonist

SZU101 is a small molecule TLR7 agonist that directly activates, induces reporter activity (23-fold) in a TLR7-NF-kB reporter system expressed in HEK-293 cells TLR7 signalling.

TPN171 (TPN-171) is a highly potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 0.62 nM, 32-fold selectivity over PDE6.

Flagelin 22 TFA, a fragment of bacterial flagellin, is an effective elicitor in both plants and algae.

3'-Methoxyapiin (Graveobioside B) is a flavone. 3'-Methoxyapiin can be found in Uraria crinite and celery.

SU-10994 is a novel VEGFR inhibitor.

SW-163D-AcLysValCit-PABC-DMAE is a Drug-Linker Conjugates for ADC which consists of a natural bis-intercalator, SW-163D, conjugated via an AcLysValCitPABC-DMAE linker.

Target Protein-binding moiety 6 hydrochloride is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

Adrenomedullin (AM) (1-52), human (TFA) affects cell proliferation and angiogenesis in cancer.

Befiradol hydrochloride is a selective 5-HT1A receptor agonist.

E3 Ligase Ligand-Linker Conjugates 23 (TFA) is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

Elacestrant S enantiomer is an low activity enantiomer of elacestrant. Elacestrant (RAD1901) is a selective and orally available estrogen receptor (ERR) degrader with IC50 values of 48 and 870 nM for ERα and ERβ, respectively.

FAS-IN-1 tosylate is a potent inhibitor of fatty acid synthase (FAS) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.