RO4938581

RO4938581 : Negative Allosteric Modulator of GABRA5

Structure

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Information

GABRA5

Negative Allosteric

up to 1 uM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: P31644

Target Class: Ion Channel

Target SubClass: --

Potency: Ki

Potency Value: 4.65 ± 0.79 nM

Potency Assay: Radioligand competition displacement assay (recombinant human GABAA subtypes expressed in HEK293 cells)

PDB ID for probe-target interaction (3D structure): 8BHS

Target aliases:

Gamma-aminobutyric acid receptor subunit alpha-5, ...

DOI Reference: 10.1016/j.bmcl.2009.08.053

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within family: Radioligand competition displacement assay: GABRA1 (α1β3γ2): rat (Ki = 174 ± 28 nM old assay; Ki = 384 nM new assay) ,human (Ki =198 ± 93 nM, n=9 new assay), GABAA2 (α2β3γ2): rat (Ki = 185 ± 5nM old assay); human (Ki = 335 ± 26 nM, n=6, new assay), GABAA3 (α3β3γ2): rat (Ki = 79.6 ± 16 nM); >30-fold selectivity over the other GABAA subtypes

Probe Selectivity in Vitro:

Roche CEREP panel (82 targets) at 10 µM: clean; Kinase panel (468 kinases) at 10 µM: clean with closest off-target GRK4 (50 % inhibition)

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