In some cases, receptor activation caused by ligand binding to a receptor is directly coupled to the cell's response to the ligand. For example, the neurotransmitter GABA can activate a cell surface receptor that is part of an ion channel. GABA binding to a GABAA receptor on a neuron opens a chloride-selective ion channel that is part of the receptor. GABAA receptor activation allows negatively charged chloride ions to move into the neuron, which inhibits the ability of the neuron to produce action potentials.
Aztreonam is a synthetic monocyclic beta-lactam antibiotic, which is resistant to beta-lactamases and is used in gram-negative infections, especially of the meninges, bladder, and kidneys. Aztreonam has a very high affinity for penicillin-binding protein 3 (PBP-3).
MoreNorfloxacin is a broad-spectrum antibiotic which is a fluorinated quinolone Pefloxacin derivative.Norfloxacin blocks DNA replication by interfering with an ATP-induced structural transition of DNA complexed with DNA gyrase (topoisomerase).
MoreTadalafil is a potent and selective inhibitor of PDE5A (Phosphodiesterase-5, PDE5) with an IC50 value of 1.8 nM.
MorePimobendan is a selective inhibitor of phosphodiesterase III(PDE3) with IC50 of 0.32 μM. Pimobendan is an inotropic agent with a dual mechanism of action: it increases myocardial contractility by increasing calcium sensitization to troponin C and it promotes vasodilatio.
MoreApixaban is a highly selective, reversible, and direct inhibitor of Human Factor X and Rabbit Factor X with Ki of 0.08 nM and 0.17 nM, respectively. Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor X with Ki of 0.08 nM and 0.17 nM for Human Factor X and Rabbit Factor X, respectively.
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