Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability.

Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).

Semaglutide acetate, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist. Semaglutide acetate has the potential for type 2 diabetes treatment.

TMinh-23 is (Compound 10bm) is a potent, selective inhibitor of transmembrane protein 16A (TMEM16A or ANO1, DOG1, ORAOV2, TAOS-2) with IC50 of 30 nM in short-circuit current assays, weakly inhibits TMEM16B (IC50=400 nM, 13 -fold selectivity).

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

Compound 12f (LPA1 antagonist) is a potent and highly selective LPA1 antagonist with IC50 of 16.0 nM (cAMP assay) and 18.4 nM (calcium mobilization assay), respectively.

R1-ICR-5 is a highly selective and efficacious PROTAC degrader of both human and murine RIPK1.

A-910 is a orally bioavailable, highly potent and selective dual MerTK/Axl inhibitor with IC50 of 0.3 nM/0.8 nM. A-910 exhibits favorable oral bioavailability, exceptional kinome selectivity, and significantly improved in MerTK Ba/F3 xenograft tumor model.

Compound 13 (MET inhibitor) is a selective, potent, and mutant-active MET inhibitor with a MET D1228N cell line IC50 of 23 nM and shows good efficacy in the MET-D1228N Type I resistance mutation model.

Arvanil is a CB1 and TRPV1 agonist. It increases lung tidal volume, diaphragm activity, mean arterial blood pressure and inhibits lymphocyte proliferation.

Palvanil is a capsaicin analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects.

CB31 is a highly potent and orally bioavailable PD-L1 inhibitor with IC50 of 0.2 nM (PD-1/PD-L1 alphs) and EC50 of 15 nM (NFAT), with high passive permeability, good metabolic stability and favorable oral PK. CB31 targets both the surface and intracellular PD-L1, reducing tumor size and killing cells in a 3D spheroid model.

AZ'3137 is an orally bioavailable androgen receptor (AR) degrader that recruit the Cereblon (CRBN) E3 ligase with DC50 of 22 nM (LNCaP) and 92 nM (LNCaP L720H), respectively.

CID-2858522 is a selectively inhibits protein kinase C (PKC)-induced activation of the NF-κB pathway (IC50 < 0.1 μM for PMA-stimulated IL-8 production).

PAT1inh-B01 is a small-molecule, selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor, could fully inhibit PAT1-mediated anion exchange with IC50 of 350 nM.

UNC0737 is a negative control of UNC0638 and the N-methyl analog of UNC0638. UNC0737 was designed to eliminate the hydrogen bond interaction seen in the G9a-UNC0224 cocrystal structure between Asp1083 of G9a and the secondary amino group at the 4-position of UNC0224's quinazoline ring3. UNC0737 was >300-fold less potent than UNC0638 in G9a and GLP biochemical assays. As expected, UNC0737 was a poor inhibitor of G9a (IC50 = 5,000 ± 200 nM (n = 2)) and GLP (IC50 > 10,000 nM (n = 2)) in the SAHH-coupled assays.

A novel protein kinase affinity probe...

SN38 NHS ester is the NHS ester derivative of SN38. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis. SN38 NHS ester can be used for the synthesis of antibody-drug conjugates (ADCs).

IT 901 is a c-Rel inhibitor (IC50 = 3 μM). Inhibits IL-2 expression in activated T-cells in vitro.

CBPD-409 is a highly potent, selective and orally bioavailable PROTAC degrader of CBP/p300. CBPD-409 induces robust CBP/p300 degradation with DC50 0.2-0.4 nM and displays strong antiproliferative effects with IC50 1.2-2.0 nM in the VCaP, LNCaP, and 22Rvl AR+ prostatcancer cell lines.

ERAS-0015 is a pan-RAS modulator glue and demonstrates siganificantly more potent inhibition of cellular proliferation across KRAS mutant cell lines vs RMC-6236.

BRD-810 is a potent and selective MCL1 inhibitor with Kd of 0.3 nM (SPR) and IC50 of 0.4 nM (MCL1-Noxa HTRF), respectively. BRD-810 is a rapidly cleared inhibitor of MCL1 that has robust antitumor efficacy in hematological and solid tumor cancer models.

PF-06648671 is a potent γ-secretase modulator with IC50 of 8.9 nM against Aβ42. PF-06648671 has favorable brain availability in rodent, which translated into excellent central exposure in human and robust reduction of amyloid β (Aβ) 42 in cerebrospinal fluid (CSF).

Compound 33 (HYOU1 inhibitor) is a first-in-class inhibitor of hypoxia up-regulated protein 1 (HYOU1) with EC50 of 3.2 μM/2.6 μM/16.1 μM/3.0 μM in WT-MIP3/WT-RANTES/hTNFtg-MIP3/hTNFtg-RANTES, respectively.

Maraviroc (Selzentry, UK-427857, Celsentri) is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively.

DFV890 (IFM-2427) is apotent, selective and orally active inhibitor of NLRP3 inflammasome, directly binds to NLRP3 and locks the protein in an inactive conformation,prevents NLRP3 inflammasome assembly in response to sterile danger signals.

CHF-6523 is an inhaled PI3Kδ inhibitor.

AZD4144 is an NLRP3 inhibitor.