SGC-SMARCA-BRDVIII is a potent and selective SMARCA2/4 BRD inhibitor.

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.

ML-T531 is a potent, selective hERG potassium channel (Kv11.1) activator with EC50 of 3.13 uM.

DPO-1 is a potent inhibitor of the voltage-gated potassium channel subtype Kv1.5 and a blocker of ultrarapid delayed rectifier potassium current. DPO-1 prevents atrial arrhythmia.

Anisole-piperazine-methanone-benzothiazole-p-methylpiperidine is an active compound.

KM91104, a cell-permeable V-ATPase inhibitor, specifically targets the a3-b2 subunits of V-ATPase.

Verubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals.

Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235 µM). Anti-multiple myeloma (MM) activity.

TG8-260 is a second-generation, potent, selective EP2 antagonist with Schild KB of 13.2 nM.TG8-260 displays 500-fold selectivity to EP2 against other prostanoid receptors.TG8-260 has a plasma half-life of 2.14 h (PO) and excellent oral bioavailability (77.3%), TG8-260 is a potent inhibitor of CYP450 enzymes.TG8-260 displays antagonistic activity on the induction of EP2 receptor-mediated inflammatory gene expression in microglia BV2-hEP2 cells.TG8-260 reduces hippocampal neuroinflammation and gliosis after pilocarpine-induced status epilepticus in rats.TG8-260 is a tool for investigating anti-inflammatory pathways in peripheral inflammatory disease animal models.

THP104c is a mitochondrial fission inhibitor.

RP-5063 (Brilaroxazine) is a multimodal dopamine and serotonin modulator with partial agonist activity at DA D2, D3, D4, 5-HT1A, and 5-HT2ARs, and antagonist activity at 5-HT2B, 5-HT6 and 5-HT7Rs.

ZINC36395841 is a small-molecule binder of the m6A-reader domain of YTHDC1.

SMS1-IN-1, compound SAPA 1j, is a novel and the most potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 value of 2.1 μM. SMS1-IN-1 has the potential for the treatment of atherosclerosis.

CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.

BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes.

ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial.

PTC-258 2HCl is a specific and orally active splicing modulator of Elongator complex protein 1 gene (ELP1). PTC258 increases the expression of ELP1 in vitro and in vivo. PTC258 is well tolerated in mouse model.

(S)-ErSO is the dextrorotatory enantiomer of ErSO. (S)-ErSO is inactive in MCF-7 cells (from patent WO2020009958A1, compound (s)-105).

MCI-INI-3 is a potent, selective, competitive inhibitor of ALDH1A3 (Ki=0.55 uM), shows poor inhibitory effect on the structurally related isoform ALDH1A1 (>140-fold selectivity).MCI-INI-3 also displays on inhibition against six isoforms of ALDH (ALDH16A1, ALDH7A1, ALDH9A1, ALDH2, ALDH1B1, ALDH18A1).MCI-INI-3 demonstrates selective binding to ALDH1A3 in glioma stem cell lysates, inhibits ALDH activity and affects RA synthesis in cells.

GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM.GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases.GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.

AC1-IN-38 is a potent, selective inhibitor of adenylyl cyclase type 1 (AC1) with IC50 of 0.54 uM.AC1-IN-38 shows selectivity over a closely related isoform AC8, and no activity against AC2/5 and other common neurological targets.AC1-IN-38 displayed modest antiallodynic effects in a mouse model of inflammatory pain.

I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.

Glutathione synthesis-IN-1 (DC-1) is a glutathione synthesis inhibitor.

INE963 (INE-963) is a potent and fast-acting blood-stage antimalarial, demonstrates potent cellular activity against Pf 3D7 with EC50 of 6 nM in Pf growth inhibition assay.

SGK1-IN-4 (compound 17a) is a highly selective, orally active SGK1 inhibitor. SGK1-IN-4 can be used for osteoarthritis research.

GSK251 is a highly potent, highly selective, orally bioavailable inhibitor of PI3Kδ with a novel binding mode.

JADA82 (PCK82) is a potent KDM5A (lysine demethylase 5A) inhibitor. From patent WO2020033377A1.

CCF0058981 (CCF981), 3-chlorophenyl analogue, is a noncovalent SARS-CoV-2 3CLpro (SC2) inhibitor with an IC50 of 68 nM. CCF0058981 inhibits SC1 (SARS-CoV-1 3CLpro) with an IC50 of 19 nM. CCF0058981 has antiviral efficacy and has the potential for COVID-19 research.

RUVBL1/2 ATPase-IN-1 (compound 18) is a potent and selective inhibitor of RUVBL1/2 ATPase with IC50 values of 6.0 and 7.7 μM, respectively. RUVBL1 and RUVBL2 are highly conserved AAA ATPases (ATPases Associated with various cellular Activities) and highly relevant to the progression of cancer. RUVBL1/2 ATPase-IN-1 has the potential for the research of cancer diseases.