Lorotomidate (Example 16) is a GABAA receptor agonist. Lorotomidate has anaesthetic effects (ED50: i.v., 2 mg/kg in KM mice; LD50: 46.5 mg/kg in KM mice). Lorotomidate has no inhibitory effect on the secretion of corticosteroids in animals, and thus has good safety.

(R)-ACE-OH is the enantiomer of (S)-ACE-OH.

(R)-PHA533533 is an inactive enantiomer (S)-PHA533533 (active enantiomer). (S)-PHA533533 is a CDK2 inhibitor with antitumor activity.

SMU-037 is an orally active and selective ROS1 inhibitor that demonstrates potent activity (IC₅₀ = 6.8 nM) and possesses the ability to penetrate the blood-brain barrier. SMU-037 shows ~25-fold selectivity over ALK, and superior sensitivity against the G2032R mutation. SMU-037 attenuates phosphorylation of ROS1 and downstream MAPK-ERK signaling pathway, leading to cell cycle arrest and apoptosis. SMU-037 effectively suppresses tumor progression in both xenograft and intracranial mouse models. SMU-037 can be used for non-small cell lung cancer (NSCLC) research.

A-75998 is an antagonist of luteinizing hormone-releasing hormone (LHRH). A-75998 can be used in the research of diseases such as hormone-sensitive cancers and endometriosis.

MK-5932 is an orally active, selective, dissociated partial glucocorticoid receptor agonist. MK-5932 inhibits IL-6. MK-5932 induces lymphopenia. MK-5932 restores glucose levels to normal. MK-5932 shows anti-inflammatory effects.

(±)-PM 92131 is a non-nucleoside HIV-1 inhibitor. (±)-PM 92131 has an anti-HIV-1 activity with IC50s of 45.7 and 53.8 μM for HIV-1 RF strain in XTT cytoprotection and syncytium-forming assay, respectively. (±)-PM 92131 can be used for HIV infections research.

Soficitinib (Compound 20) is a selective inhibitor targeting tyrosine kinase 2 (TYK2) and Janus kinase 2 (JAK2) with an IC50 values of 0.5 nM and 1.2 nM, respectively. Soficitinib is promising for research of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis) and inflammatory diseases.

KC-11458 is a motilin agonist. KC-11458 can accelerate gastric emptying.

NKS-01 is a selective estrogen receptor modulator. NKS-01 can be used for the research of cancer, such as estrogen receptor-positive breast cancer.

Androgen receptor ligand 3 is an androgen receptor (AR) ligand. Androgen receptor ligand 3 is linked to an IAP ligand via a linker to form an ERα PROTAC degrader.

HMR-3787 is a 2-fluoroketolide and bactericide. HMR 3787 is bactericidal against 12 H. influenzae strains.

MS-153 is a glutamate transporter activator that can be used as a neuroprotective agent.

Dazodeunetant (Example 56) is a nitrogen-containing fused ring derivative. Dazodeunetant is an inhibitor of neurokinin (NK). Dazodeunetant has an IC50 0f 75.99 nM against NK3R in HEK293-NK3 (IP1). Dazodeunetant can be studied in research for menopausal hot flashes.

Asuptegravir (Compound 1) is an inhibitor of HIV integrase activity. Asuptegravir inhibits HIV in HEK293T cells (EC50 = 1.08 nM). Asuptegravir can be studied in anti-AIDs/HIV research.

CMLD009688 is a cationic amphiphilic antifungal agent. CMLD009688 selectively inhibits plant pathogenic fungi such as Fusarium graminearum. CMLD009688 interacts with biological membranes, perturbing vacuolar and mitochondrial membrane structures to induce fungal cell death. CMLD009688 is promising for research of plant fungal diseases (e.g., wheat head blight, gray mold).

WHN-11 is an amino-Artemisinin derivative with anti-cancer activity against various cancer cell lines. WHN-11 deprives the cell of ATP, activates autophagy, and causes subsequent cell death by apoptosis. WHN-11 alters cellular protein homeostasis pathways to induce mitochondrial fission and dysfunction. WHN-11's anti-cancer activity is independent of substantive ROS production. WHN-11 can be used for the study of triple-negative breast cancer (TNBC).

PBX-7016 is a Camptothecin derivative. PBX-7016 can selectively inhibit Topoisomerase 1. PBX-7016 can specifically bind and degrade the cancer protein DDX5, thereby down-regulating the expression of anti-apoptotic proteins such as Survivin, Mcl-1, and XIAP, and promoting the apoptosis of cancer cells. PBX-7016 can be used to synthesis of ADCs.

Fmoc-Gly-Thr-OH is an ADC Linker. Fmoc-Gly-Thr-OH can be used to synthesize antibody-drug conjugates (ADCs).

4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.

MKP10241 is an orally active GPR119 agonist. MKP10241 elevates cAMP levels in the GPR119 expressing cell line (EC50: 3.7 nM). MKP10241 reduces blood glucose levels and HbA1c in acute models and a chronic diabetic mouse model. MKP10241 also demonstrates excellent preclinical efficacy in acute as well as chronic rodent models of obesity, and MASH.

PF 04254644 is an orally active c-Met inhibitor. PF 04254644 inhibits mesenchymal transfer factor/hepatocyte growth factor receptor. PF 04254644 induces myocardial degeneration in rats. PF 04254644 may be used in research on cardiovascular disease and cancer.

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.

PrCP-7414 is a prolylcarboxypeptidase (PRCP) inhibitor. PrCP-7414 can block the receptor tyrosine kinase (RTK) signaling pathway mediated by PRCP and the GPCR-RTK crosstalk. PrCP-7414 can inhibit cancer cells proliferation and induce apoptosis. PrCP-7414 can be used for the research of cancer, such as triple negative breast cancer (TNBC).

CT-996 is an orally active GLP-1RA agonist, with an EC50 of 0.49 nM. CT-996 reduces the β-arrestin recruitment and GLP-1R internalization. CT-996 suppresses postprandial blood glucose following a mixed meal tolerance test (MMTT) in mice expressing the human GLP-1 receptor and enhances glucose stimulated insulin secretion (GSIS) during an intravenous glucose challenge in obese monkeys. CT-996 can be used for the study of type 2 diabetes (T2D) and obesity.

E3 Ligase Ligand-linker Conjugate 190 is a E3 ligase ligand-linker conjugate, used for the synthesis of BP-198.

E3 ligase Ligand 66 is an E3 ligase ligand that can be used to recruit IAP proteins. E3 ligase Ligand 66 can be linked to SARS-CoV-2 Mpro ligand 1 through a linker to form PROTAC BP-198.

Arachidonic acid leelamide, a Leelamine analog, is a pyruvate dehydrogenase kinase (PDK) inhibitor. Arachidonic acid leelamide can be used for the study of breast cancer.

Galeterone (TOK-001) hydrochloride is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone hydrochloride also functions as a CYP17 inhibitor (IC50 = 47 nM). Galeterone hydrochloride induces cell apoptosis. Galeterone hydrochloride inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone hydrochloride can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research[1][2].

ABJ-879 is an Epothilone derivative. ABJ-879 targets tubulin and can be used for the research of cancer.