Potency data for probe RO4938581 and control RO4991571
In vitro potency
| Target name | Target information | Species | Assay description | RO4938581 | RO4991571 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| GABRA5, GABRB3, GABRG2 | recombinant human GABAA subtypes expressed in HEK293 cells | Homo sapiens | [3H]flumazenil competition displacement assay (human GABRA5) new assay type | Ki = 4.65 nM ± 0.790 nM (n=8) | ||
| GABRA5, GABRB3, GABRG2 | recombinant rat GABAA subtypes expressed in HEK293 cells | Rattus norvegicus | [3H]flumazenil competition displacement assay (rat GABRA5) new assay type | Ki = 13.8 nM | ||
| GABRA5, GABRB3, GABRG2 | recombinant rat GABAA subtypes expressed in HEK293 cells | Rattus norvegicus | [3H]flumazenil competition displacement assay (rat GABRA5) old assay type | Ki = 4.6 nM ± 1.400 nM | Ki > 3.16 µM | PMID: 18936916 |
| GABRA1, GABRB3, GABRG2 | recombinant human GABAA subtypes expressed in HEK293 cells | Homo sapiens | [3H]flumazenil competition displacement assay (human GABRA1) new assay type | Ki = 198 nM ± 93.000 nM (n=9) | ||
| GABRA1, GABRB3, GABRG2 | recombinant rat GABAA subtypes expressed in HEK293 cells | Rattus norvegicus | [3H]flumazenil competition displacement assay (rat GABRA1) old assay type | Ki = 174 nM ± 28.000 nM | Ki > 3.16 µM | PMID: 18936916 |
| GABRA1, GABRB3, GABRG2 | recombinant rat GABAA subtypes expressed in HEK293 cells | Rattus norvegicus | [3H]flumazenil competition displacement assay (rat GABRA1) new assay type | Ki = 384 nM | ||
| GABRA2, GABRB3, GABRG2 | recombinant human GABAA subtypes expressed in HEK293 cells | Homo sapiens | [3H]flumazenil competition displacement assay (human GABRA2) new assay type | Ki = 335 nM ± 26.000 nM (n=6) | ||
| GABRA2, GABRB3, GABRG2 | recombinant rat GABAA subtypes expressed in HEK293 cells | Rattus norvegicus | [3H]flumazenil competition displacement assay (rat GABRA2) old assay type | Ki = 185 nM ± 5.000 nM | PMID: 18936916 | |
| GABRA3, GABRB3, GABRG2 | recombinant rat GABAA subtypes expressed in HEK293 cells | Rattus norvegicus | [3H]flumazenil competition displacement assay (rat GABRA3) old assay type | Ki = 80 nM ± 16.000 nM | PMID: 18936916 |
In cell potency
| Target name | Target information | Species | Assay description | RO4938581 | RO4991571 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| GABRA5, GABRB3, GABRG2 | recombinant rat GABAA subtypes expressed in HEK293 cells | Rattus norvegicus | Whole cell patch-clamp (GABRA5): Meassured inhibition of GABA-induced current | IC50 = 7.4 nM | PMID: 18936916 |