Naltriben is a highly selective δ2 opioid receptor antagonist.Naltriben (NTB) has been used to differentiate the subtypes of delta opioid receptors, delta1 and delta2. NTB displaced the specific binding of [3H]DAMGO with Ki value of 19.79 +/- 1.12 nM in rat cortex membranes. Specific binding of [3H]diprenorphine ([3H]DIP) was inhibited by NTB with Ki value of 82.75 +/- 6.32 nM in the presence of DAMGO and DPDPE. Naltriben enhanced the MAPK/ERK signaling pathway, but not the PI3k/Akt pathway. Therefore, potentiated TRPM7 activity contributes to the devastating migratory and invasive characteristics of GBM.

Novel pendrin inhibitor, attenuating airway hyperresponsiveness and mucin expression in experimental murine asthma

DRAinh-A250 is a specific inhibitor of Cl-/anion exchanger SLC26A3 (DRA), fully and reversibly inhibits SLC26A3-mediated Cl- exchange with HCO3-, I-, and thiocyanate (SCN-) with IC50 of ~0.2 uM.

PAT1inh-A0030 is a potent and selective SLC26A6 (putative anion transporter 1, PAT1) inhibitor with IC50 of 1.0 uM, shows no activity on relevant ion transporters/channels (SLC26A3, SLC26A4, SLC26A9, CFTR, TMEM16A).

1PBC is a small molecule blocker of calcium-activated chloride channel TMEM16A, blocks TMEM16A completely with an IC50 of 4 uM at zero mV and saturating Ca2+ concentration (2 uM).

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).

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.

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.

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...

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

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).

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.

GSK-484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay.

G150 is a highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor with an IC50 of 10.2 nM. G150 represses dsDNA-triggered interferon expression, and G150 can be used for the research of inflammatory.

G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.

GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.

GW 4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).

LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. generation of catalytically active enzyme.

CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.