VU6066098 |
VU6066098 : Negative Allosteric of GRM2
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| GRM2 |
|
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family:
Inactive (>10 μM) on human mGlu1,3,4,5,7 and a weak PAM of human m ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
CEREP safety screen of 44 targets, NAM 7 was clean (no inhibition >50% @10 μM)
Potency Cellular
In Vitro
GRM2
Mode of Action: Negative Allosteric
Structure-Activity-Relationship data available? No
DOI Reference: 10.1021/acschemneuro.6c00324
In Vivo Validations
Mouse
Dose: 0.2 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.23
Systemic clearance:
23.9 mL/min/Kg
Area Under the Curve::
139 h*ng/mL
Volume of Distribution at Steady-State:
2.24 L/Kg
DOI Reference: 10.1021/acschemneuro.6c00324
Dose: 10 mg/Kg
Route of delivery:
Oral
Systemic clearance:
228%
Cmax:
2822 ng/mL
Tmax:
1.50 h
Area Under the Curve::
15865 h*ng/mL
DOI Reference: 10.1021/acschemneuro.6c00324
Dose: 100 mg/Kg
Route of delivery:
Oral
Cmax:
8995 ng/mL
Tmax:
1.50 h
Area Under the Curve::
150228 h*ng/mL
Bioavailability:
216%
DOI Reference: 10.1021/acschemneuro.6c00324
Chemical Information
| Molecular Formula | C19H15F2N3O |
| SMILEs | Cc1cc(-c2cc(-c3ccc(F)cc3F)cc3c2CNC3=O)n(C)n1 |
| InChI | InChI=1S/C19H15F2N3O/c1-10-5-18(24(2)23-10)14-6-11(7-15-16(14)9-22-19(15)25)13-4-3-12(20)8-17(13)21/h3-8H,9H2,1-2H3,(H,22,25) |
| Molecular weight | 339.12 Da |
| AlogP | 3.5841200000000013 |
| HBond acceptors | 4 |
| HBond donors | 1 |
| Atoms | 40 |