Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis. CME: Clathrin mediated endocytosis

DATPT is a 12WLVSKF17 peptide-mimetic molecule. DATPT blocks the SNX9-p47phox interaction in the endosome and suppresses reactive oxygen species and inflammatory cytokine production. DATPT with anti-inflammatory and antibacterial functions has the potential for the research of sepsis.

Rha-PEG3-SMCC (compound 13) is a drug-linker conjugate for ADC with potent antitumor activity by using SMCC (a protein crosslinker), linked via the noncleavable ADC linker Rha-PEG3.

Aspochalasin M is a colorless solid. Aspochalasin M shows modest activity against HL-60 cells with an IC50 of 20.0 μM. Aspochalasin M has the potential for the research of leukemic disease.

Antalarmin (hydrochloride) is a non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome.

Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.

Estradiol 17-(β-D-Glucuronide) sodium, a metabolite of estrogen, is well known to cause intrahepatic cholestasis in humans.

Cemdomespib (KU-596) is a highly bioavailable second-generation Hsp90 modulator. Cemdomespib has shown efficacy in improving sensory deficits in models of diabetic peripheral neuropathy. Cemdomespib induces Hsp70 levels and manifest neuroprotective activity through induction of the heat shock response.

(+)-Pileamartine A is a complex alkaloid. (+)-Pileamartine A can be accessed via intramolecular Pd(0)-catalyzed alkene 1,2-aminoarylation reactions.

SOS1-IN-4 is a potent SOS1 inhibitor with an IC50 of 56 nM for KRAS-C12C/SOS1 interaction (WO2021228028 A1, example 65).

Platencin is a natural, broad spectrum Gram-positive antibiotic isolated from S. platensis. Platencin inhibits β-ketoacyl-ACP synthases II and III (FabF and FabH, respectively) with IC50s of 1.95 and 3.91 μg/ml, respectively.

Neoechinulin C, an echinulin-related indolediketopiperazine alkaloid, protects the neuronal cells against paraquat-induced damage in a Parkinson’s disease model.

PARP-1/2-IN-1 is a potent PARP-1/2 inhibitor with IC50 of 0.51 nM and 23.11 nM, respectively.

Berkeleyacetal C, a meroterpenoid compound, shows favorable activity of inhibiting nitrogen oxide (NO) production of macrophages stimulated by lipopolysaccharide (LPS). Berkeleyacetal C exerts anti-inflammatory effects via inhibiting NF-κB, ERK1/2 and IRF3 signaling pathways.

Antiviral agent 14 is an antiviral agent against the tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV). The EC50 values of Antiviral agent 14 against TMV and CMV with EC50 values of 135.5 μg/mL and 178.6 μg/mL, respectively.

SYK/JAK-IN-1 is dual SYK/JAK inhibitor with IC50s of <5 nM for SYK and JAK2, respectively.

RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual RORγt/DHODH inhibitor, with IC50s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity.

RORγt/DHODH-IN-3 (compound (S)-14d) is a dual RORγt/DHODH inhibitor, with IC50s of 0.098 μM and 0.432 μM, respectively. RORγt/DHODH-IN-3 exhibits remarkable in vivo anti-inflammatory activity.

YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). YF-452 remarkably inhibits the migration, invasion and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) with little toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase (ERK), focal adhesion kinase (FAK) and Src. YF-452 is a potential antiangiogenic drug candidate for cancer research.

Butyrolactone V is a butanolide compound. Butyrolactone V shows antiplasmodial activity against Plasmodium falciparum K1 with an IC50 of 7.9 µg/ml.

HPK1-IN-18 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-18 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 1).

ROS-ERS inducer 1 is a type II ICD (immunogenic cell death) inducer. ROS-ERS inducer 1 is a Pt(II)-N-heterocyclic carbene (Pt(II)-NHC) complex derived from 4,5-diarylimidazole. ROS-ERS inducer 1 successfully induces endoplasmic reticulum stress (ERS) accompanied by reactive oxygen species (ROS) generation and finally lead to the release of damage-associated molecular patterns (DAMPs) in HCC cells. ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin.

DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect.

Methyl 3,4,5-trimethoxy-2-(2-(nicotinamido)benzamido)benzoate is a fungal metabolite.

HPK1-IN-14 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-14 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 79) .

Kotanin is a metabolite of Aspergillus glaucus.

EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects.

TP-16 is a novel and selective EP4 antagonist with an IC50 of 2.1 nM.

Bis-PEG4-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

PfPKG-IN-1 is a imidazole-based inhibitor of Plasmodium falciparum cGMP-dependent protein kinase (PfPKG).