potent

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.

Slingshot inhibitor D3 (JHN76359) is a potent inhibitor of the Protein Phosphatase Slingshot.

(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.

BMS-986242 is an orally active, potent, and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, suitable for cancer research.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor that inhibits BRD4 with an IC50 of 5193nM.

SCD1 inhibitor-4 is stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes.

CYM50308 is a high affinity agonist of sphingosine-1-phosphate receptor 4 (S1P4-R) (EC50: 56 nM). CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM and it shows 37-fold more selective for S1P4-R than S1P5-R.

A-803467 is a selective NaV1.8 channel blocker.

Maytansine (NSC-153858), an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata, inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site.

Hepln-13 is a hepsin inhibitor that acts by hindering prostate cancer bone metastasis.

VU0071063 is a Kir6.2/SUR1 activator.

Olodaterol is a novel, long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs.

Zopolrestat (CP 73850) is a potent inhibitor of aldose reductase (IC50 = 3.1 nM).

JNJ-67856633 is an orally active, first-in-class, potent, selective and allosteric inhibitor of MALT1 protease . JNJ-67856633 lead to tumor stasis in some cases.

Olodaterol hydrochloride (BI-1744 HCl) is a novel, long-acting β2-adrenergic agonist (EC50s: 97.7 nM for the human β2-adrenoceptor) that exerts its pharmacological effect by binding and activating β2-adrenergic receptors.

GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM.

Chetomin (BRN0077366) is an inhibitor of HIF-1 by weaken transcription of HIF-1, disrupting the binding of HIF-1α and HIF-2α to p300 at low nanomolar concentrations.

SB-366791 is a new and selective cinnamide TRPV1 antagonist.

PF-9363 (CTX-3648) is a potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.

GLPG2938 (1-(2-Ethoxy-6-(trifluoromethyl)pyridin-4-yl)-3-((5-methyl-6-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)pyridazin-3-yl)methyl)urea) is a potent and selective antagonist of S1P2.

DDO-5936 is a potent and specific inhibitor of the protein-protein interaction (PPI) between HSP90 and Cdc37.

ELOVL6-IN-2 is a orally active and selective ELOVL6 inhibitor.

RO-0335 is a potent diphenylether nonnucleoside reverse transcriptase inhibitor. RO-0335 inhibits Wt HIV-1 (IC50 = 1.1 nM) and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates.