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.

A3AR antagonist 5 (Compound 16) is a selective antagonist for human adenosine A3 receptor with an affinity pC of 4.542 μM.

OGT-IN-1 (Compound 5) is a potent OGT inhibitor. OGT-IN-1 inhibits sOGT and ncOGT with IC50s of 27 and 10 μM, respectively.

NQTrp, an aromatic naphthoquinone-tryptophan hybrid molecule, an inhibitor of the aggregation of the tau protein with generic anti-amyloidogenic effects. NQTrp inhibits the in vitro aggregation of hexapeptide (41GCWMLY46 within the N-terminus of γD-crystallin) as well as full-length γD-crystallin.

GSK650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively.

Fexaramine is a potent, selective FXR activator.

L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM respectively.

Dynasore is a cell-permeable small molecule that inhibits the GTPase activity of dynamin1, dynamin2 and Drp1, the mitochondrial dynamin.

GPR183-IN-2 (compound 23) is a potent GPR183 inhibitor. GPR183-IN-2 inhibits Ca2+ mobilization with an IC50 value of 39.45 nM. GPR183-IN-2 has the potential for the research of cancer, autoimmune diseases, pain, and osteoporosis.