# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA3804042 | F | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay | Homo sapiens | 26 | ALA3797196 | cell-based format | Scientific Literature | |
2. | ALA3804043 | F | Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium mobilization at 30 uM relative to (-)-PHCCC | Homo sapiens | 26 | ALA3797196 | cell-based format | Scientific Literature | |
3. | ALA3801271 | F | Reversal of haloperidol-induced catalepsy in Sprague-Dawley rat at 1 mg/kg, po administered 60 mins after haloperidol-challenge measured after 30 mins | Rattus norvegicus | 2 | ALA3797196 | organism-based format | Scientific Literature | |
4. | ALA3801272 | F | Reversal of haloperidol-induced catalepsy in Sprague-Dawley rat at 10 mg/kg, po administered 60 mins after haloperidol-challenge measured after 30 mins | Rattus norvegicus | 1 | ALA3797196 | organism-based format | Scientific Literature | |
5. | ALA3887397 | F | Receptor Activity Assay: The disclosed compounds and compositions can be evaluated for their ability to act as a potentiator of metabotropic glutamate receptor activity, in particular mGluR4 activity, by any suitable known methodology known in the art. For example, Chinese Hamster Ovary (CHO) cells transfected with human mGluR4 or HEK cells co-transfected with rat mGluR4 and the G-protein regulated Inwardly Rectifying Potassium channel (GIRK) were plated in clear bottom assay plates for assay in a Hamamatsu FDSS Fluorometric Plate Reader. The cells were loaded with either a Ca2+-sensitive fluorescent dye or the thallium responsive dye and the plates were washed and placed into a suitable kinetic plate reader. For human mGluR4 assays, a fluorescence baseline was established for 3-5 seconds, the disclosed compounds were then added to the cells, and the response in cells was measured. | 90 | ALA3886304 | cell-based format | BindingDB Database | ||
6. | ALA4233470 | F | Positive allosteric modulation of human mGluR4 expressed in CHO cells co-expressing Gqi5 assessed as increase in glutamate-induced calcium flux preincubated for 2.5 mins followed by glutamate addition by Fluo-4-AM dye based fluorescence assay | Homo sapiens | 47 | ALA4229425 | cell-based format | Scientific Literature | |
7. | ALA4233472 | A | Clearance in rat liver microsomes | Rattus norvegicus | 8 | ALA4229425 | microsome format | Scientific Literature | |
8. | ALA4233473 | A | Fraction unbound in human plasma | Homo sapiens | 8 | ALA4229425 | cell-free format | Scientific Literature | |
9. | ALA4233474 | A | Fraction unbound in rat plasma | Rattus norvegicus | 8 | ALA4229425 | cell-free format | Scientific Literature | |
10. | ALA4233475 | A | Inhibition of CYP1A2 in human liver microsomes | Homo sapiens | 8 | ALA4229425 | microsome format | Scientific Literature | |
11. | ALA4233476 | A | Activation of human AhR assessed as induction of CYP1A2 relative to control | Homo sapiens | 8 | ALA4229425 | single protein format | Scientific Literature | |
12. | ALA4310058 | F | Reversal of haloperidol-induced catalepsy in Sprague-Dawley rat assessed as decrease in latency to remove forepaws from bar at 10 mg/kg, po administered 30 mins prior to test | Rattus norvegicus | 3 | ALA4308847 | organism-based format | Scientific Literature | |
13. | ALA4737566 | F | Reversal of haloperidol-induced catalepsy in ip dosed Sprague-Dawley rat assessed as reduction in catalepsy measured after 15 mins relative to untreated control | Rattus norvegicus | 1 | ALA4732192 | organism-based format | Scientific Literature | |
14. | ALA4737567 | F | Reversal of haloperidol-induced catalepsy in ip dosed Sprague-Dawley rat assessed as latency time for withdrawl measured after 15 mins (Rvb = 49.8 sec) | Rattus norvegicus | 1 | ALA4732192 | organism-based format | Scientific Literature | |
15. | ALA5128636 | F | Agonist activity at human mGlu4 receptor assessed as increase in calcium flux | Homo sapiens | 1 | ALA5126552 | assay format | Scientific Literature | |
16. | ALA5128637 | B | Agonist activity at rat mGlu4 receptor assessed as increase in calcium flux | Rattus norvegicus | 1 | ALA5126552 | assay format | Scientific Literature | |
17. | ALA5128638 | A | Oral bioavailability in 6-OHDA-unilateral lesioned rat model of Parkinson's disease at 15 mg/kg | Rattus norvegicus | 1 | ALA5126552 | organism-based format | Scientific Literature |