N-desethyl Amodiaquine is a primary metabolite of the antimalarial compound aminodiaquine, produced by the action of cytochrome P450 isoform 2C8. N-desethyl Amodiaquine is highly active against P. falciparum and can synergize with amodiaquine.

Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a drug-linker conjugate for ADC.

SU0268 is a potent and selective OGG1 inhibitor. DNA glycosylases involved in the first step of the DNA base excision repair pathway are promising targets in cancer therapy. There is evidence that reduction of their activities may enhance cell killing in malignant tumors.

MAT2A inhibitor 2 is a methionine adenosyltransferase 2A (MAT2A) inhibitor.

nor-NOHA, also known as N-​Hydroxy-​nor-​L-​Arginine, is an Arginase inhibitor. nor-NOHA induces apoptosis in leukemic cells specifically under hypoxic conditions but CRISPR/Cas9 excludes arginase 2 (ARG2) as the functional target. Nor-NOHA can induce cell apoptosis and inhibit the ability of invasion and migration of HepG2 cells by inhibiting Arg1, which is related with the increase of iNOS expression and the high concentration of NO.

ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.

Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.

Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6).

Ziftomenib is a menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).

Mesdopetam (IRL790) is an orally active and low toxicity dopamine D3 receptor antagonist. Mesdopetam can be used for the research of Parkinson's disease (PD).

Emraclidine is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases.

BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects.

Sivopixant (S-600918) is a potent and selective P2X3 receptor antagonist (P2X3 IC50=4.2 nM; P2X2/3 IC50=1100 nM). Sivopixant shows strong analgesic effect.

Enavogliflozin (DWP-16001), an antidiabetic agent, is an orally active, best-in-class and selective sodium-glucose cotransporter-2 (SGLT-2) inhibitor.

Vocacapsaicin (CA-008), a prodrug of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin can provide meaningful and long-lasting pain relief.

Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases.

Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM).

Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.

Tinlarebant (LBS-008) is an orally active non-retinoid RBP4 (retinol-binding protein 4) antagonist. Tinlarebant can be used for the research of the Stargardt disease.

Utreloxastat is a compound used for the research of the disorders including α-synucleinopathies, tauopathies, Amyotrophic lateral sclerosis (ALS), traumatic brain injury, and ischemic-reperfusion related injuries (patent WO2020081879A2, example A1).

Sebetralstat is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases.

2-Bromohexadecanoic acid (2-BP, 2-bromopalmitate) is a nonmetabolisable analogue of palmitate and acts as a palmitoylation inhibitor. 2-Bromohexadecanoic acid can directly and irreversibly inhibit the palmitoyltransferase activity of all DHHC (Asp-His-His-Cys) proteins.