α4-α6

BRD9876 is a selective inhibitor of MM1S growth.

CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxi

MK0343 is an orally bioavailable GABAA receptor subtype-selective partial agonist and is a non-sedating anxiolytic.

PVZB1194, a biphenyl-type inhibitor of Kinesin spindle protein Eg5 (KIF11), exhibits anticancer potential by inducing cell cycle arrest and apoptosis through inhibiting Eg5 ATPase activity. It binds to the α4 α6 allosteric pocket and demonstrates ATP-competitive activity [1].

CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1].

α-Conotoxin BuIA is a paralytic peptide neurotoxin that acts as a competitive antagonist of nicotinic acetylcholine receptors (nAChR), with inhibitory concentration 50 (IC50) values of 0.258 nM for α6 α3β2, 1.54 nM for α6 α3β4, and 5.72 nM for α3β2. It serves to differentiate between nAChRs containing the β2- and β4-subunits and selectively inhibits αxβ2 nAChRs, exhibiting a potency hierarchy of α6>α3>α2>α4 [1].