UNC2541 is a potent and MerTK-specific inhibitor that exhibits sub-micromolar inhibitory activity in the cell-based ELISA. In addition, an X-ray structure of MerTK protein in complex with 11 was resolved to show that these macrocycles bind in the MerTK ATP pocket. UNC2541 showed IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM.

ZM-447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively.

TG4-155 is a brain penetrant EP2 antagonist (KB = 2.4 nM) that is over 1000-fold less effective at EP4 (KB = 11.4 µM) and a panel of other receptors and channels. It blocks the induced expression of inflammatory markers in microglial cells.

PIM/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively; also inhibits MPSK1 and TNIK.

GRA Ex-25 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk.

GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively).

GNE-7915 is a highly potent, selective, and brain-penetrable LRRK2 small molecule inhibitor with IC50 of 9 nM in cellular LRRK2 assay; > 100 fold selectivity against a panel of 187 kianses(Ki).

Filgotinib (GLPG0634) is a selective, orally available JAK1 inhibitor with anti-inflammatory and antiviral activities. Filgotinib can effectively inhibit the activities of JAK1, JAK2, JAK3 and TYK2 with IC50 values of 10 nM, 28 nM, 810 nM and 116 nM, respectively. Filgotinib also inhibits HIV-1 driven gene transcription and reduces proliferation of HIV-1 infected cells. Filgotinib can be used in the study of rheumatoid arthritis and inflammatory bowel disease.

FITM is a nove mGlu1 inhibitor. FITM shows high affinity (Ki = 2.5 nM, fig. S2) and selectivity for mGlu1 over mGlu5.

FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease.

Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.

E-4031 is a benzenesulfonamide antiarrhythmic agent; blocks the ATP-sensitive potassium channel.

CAY10594 is a potent phospholipase D2 inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis.

ARN14974 is a benzoxazolone carboxamide inhibitor of acid ceramidase (IC50 = 79 nM).

BAL-0028 is a reversible inhibitor of NLRP3 activation with an IC50 value of 25 nM. BAL-0028 binds closely to the NACHT domain of the NLRP3 with KD values of 104-123 nM. BAL-0028 can inhibit the secretion of IL-1β and has anti-inflammatory activity.

TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.

Pindolol is a moderately lipophilic beta blocker. Pindolol is a SR-1A/SR-1B antagonist with similar affinity for each subtype. Pindolol acts as a partial agonist at mouse and human β3-AR (β3-adrenoceptors). Pindolol is an inhibitor of β1-AR.

BSJ-05-037 is a potent and selective heterobifunctional degrader of ITK with DC50 of 17.6-41.8 nM in TCL lines DERL-2 and Hut78.

AZD9574 is a CNS-penetrant, PARP1-selective inhibitor with IC50 of <0.005 μM. AZD9574 demonstrates >10,000-fold selectivity for PARP1 over PARP2 and shows excellent preclinical PK acrossseveral species, with low clearance and high oral bioavailability, and demonstrated in vivo efficacy in a BRCA2−/− DLD-1 mouse xenograft model.

KAI-11101 is a potent, selective, brain-penetrant DLK inhibitor with Ki of 0.7 nM. KAI-11101 also demonstrates favorable preclinical PK, including good CNS penetration, and in vitro safety profiles.

EF24 HCl is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.

TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.

BCTC is a potent and specific inhibitor of transient receptor potential cation channel subfamily M member 8 (TRPM8) in prostate cancer (PCa) DU145 cells.

Zacopride is a selective agonist with the activity of enhancing the inward rectifier potassium current (IK1) in rabbit hearts. Zacopride also exhibits significant antiarrhythmic effects, inhibiting ventricular arrhythmias by increasing IK1 without affecting atrial arrhythmias. Zacopride can hyperpolarize the resting membrane potential and shorten the action potential duration (APD) in a concentration-dependent manner. Zacopride significantly reduced the incidence of compound-induced early afterdepolarizations (EADs) at 1 μmol/L.

VA-012 is a potent, selective 5-HT2C receptor positive allosteric modulator (PAM) that exhibits dose-dependent potentiation of 5-HT efficacy with EC50 of 16 nM.