Ligands organométalliques

Clinidipine is a dihydropyridine calcium channel blocker that is used to treat hypertension. This drug acts on L-type calcium channels of blood vessels by blocking calcium and suppressing the contraction of blood vessels, thereby reducing blood pressure. . Cilnidipine also shows activity against N-type calcium channels.

NMDA receptor antagonist

Potent inhibitor of the sodium-coupled citrate cotransporter SLC13A5 (NaCT, INDY). The compound is not structurally related to citrate and is selective for SLC13A over other related transporters.

Irreversible ErbB receptor tyrosine kinase inhibitor

Inhibitor of CPT1 and CPT2 enzymes; inhibitor of mTORC1 kinase; anti-fungal

Lamotrigine is an antiepileptic phenyltriazine drug that is used to treat epilepsy and as a mood stabilizer in bipolar disorder. Although, this drug’s action is not fully well understood it is similar to carbamazepine which involves inhibiting voltage-sensitive sodium channels. Lamotrigine blocks voltage-sensitive sodium channels, which reduces neuronal excitability by blocking action potentials.

Ranolazine is a group P2 drug that reverses the pathogenic mechanism of myocardial infarction. It is used to treat chronic angina. It decreases myocardial wall tension and improves coronary blood flow. It inhibits the ryanodine receptor, which is responsible for regulating the release of intracellular calcium in cardiac and skeletal muscle cells. Furthermore, it is also effective at preventing atrial fibrillation and has been studied as monotherapy as well as in combination with other medications used to treat irregular heartbeat.

Anti-spasmodic, choleretic and cholekinetic agent

Tadalafil analogue; PDE 5 inhibitor

Activator of soluble guanylyl cyclase (sGC) which stimulates cGMP production and is effective in cells under oxidative stress. Ataciguat stimulates the heme-free form of the sGC enzyme via the sGC N-terminus of β1-subunit. Ataciguat can promote vasorelaxation and hypotension by restoring or potentiating the nitric oxide (NO) signalling pathway.

Inhibitor of PIP5K1C

Potential treatment for gout and rheumatoid arthritis

Inhibitor of FLT3 receptor tyrosine kinases; anti-neoplastic

Amylin analogue; helps in the regulation of vblood glucose

Bronchodilator

Inhibitor of p38 MAPK kinase

Positive allosteric modulator of taste receptors T1R2 and T1R3 and enhancer of sucrose sweetness. In a human sensory evaluation test, FEMA 4774 increased the sucrose sweetness to 1.97 times. In vitro analyses showed that FEMA 4774 decreased the sucrose EC50 value from 31.7 mM to 0.6 mM.

Nitrogen mustard derivative; DNA crosslinking agent; anti-cancer agent

Inhibitor of histone deacetylase 3 (HDAC3) with IC50 in nanomolar range. BRD 9908 was shown to preserve the insulin-secreting pancreatic cells in nonobese diabetic mice. BRD 3308 supressed infiltration of mononuclear cells and prevented β-cell death in vivo as well as increased basal insulin secretion in vitro. Studies on HIV infection models showed that HDAC3 inhibition by BRD 3308 disrupts the HIV latency by increasing the gene expression from HIV promoter.

Selective, potent, competitive and reversible inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD-1) with IC50 of 2.3 nM and more than 10000-fold selectivity over the related 11β-HSD-2 isoform. BMS 823778 inhibits conversion of cortisone in cortisol and has applications in the treatment of diabetes type 2 since it can influence the occurrence of insulin resistance.