A New Pyridazine Series of GABAA α5 Ligands
Van Niel, M.B., Wilson, K., Adkins, C.H., Atack, J.R., Castro, J.L., Clarke, D.E., Fletcher, S., Gerhard, U., Mackey, M.M., Malpas, S., Maubach, K., Newman, R., O'Connor, D., Pillai, G.V., Simpson, P.B., Thomas, S.R. and MacLeod, A.M.
(2005)
A New Pyridazine Series of GABAA α5 Ligands.
Journal of Medicinal Chemistry (19).
pp. 6004-6011.
ISSN 0022-2623
Screening of the Merck compound collection identified 6 as an unusually simple, low molecular weight hit with moderate affinity for GABAA receptors. The structural novelty of 6, compared to our advanced series of GABAA α5 inverse agonists, made it an attractive molecule for further exploration. This paper will describe the evolution of 6 into a new series of ligands with nanomolar affinity and functional selectivity for GABAA α5 receptor subtypes.
| Item Type | Article |
|---|---|
| Date Deposited | 29 May 2025 09:10 |
| Last Modified | 29 May 2025 09:10 |