GFH018 |
GFH018 : Inhibitor of TGFB1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| TGFB1 |
|
|
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity assessment of GFH018 on the ALK family and selected kinases was performed at a concentra ...
Potency Cellular
In Vitro
TGFB1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/acs.jmedchem.5c00121
In Vivo Validations
Mouse
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
0.484 h
Systemic clearance:
63.3 mL/min/Kg
Volume of Distribution at Steady-State:
1.4 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c00121
Dose: 5 mg/Kg
Route of delivery:
Oral
Plasma half life:
0.917 h
Cmax:
355 nM/mL
Area Under the Curve::
285 nM*h/mL
Bioavailability:
8.74%
DOI Reference: 10.1021/acs.jmedchem.5c00121
Dose: 75 mg/Kg
Route of delivery:
Oral
Plasma half life:
0.856 h
Cmax:
24,233 nM/mL
Area Under the Curve::
18,137 nM*h/mL
Bioavailability:
36.8%
DOI Reference: 10.1021/acs.jmedchem.5c00121
Rat
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
0.87 h
Systemic clearance:
33.3 mL/min/Kg
Area Under the Curve::
1332 nM*h/mL
Volume of Distribution at Steady-State:
1.44 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c00121
Dose: 30 mg/Kg
Route of delivery:
Oral
Plasma half life:
2.01 h
Cmax:
9553 nM/mL
Area Under the Curve::
9614 nM*h/mL
Bioavailability:
29.9%
DOI Reference: 10.1021/acs.jmedchem.5c00121
Dog
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
3.16 h
Systemic clearance:
9.29 mL/min/Kg
Area Under the Curve::
5626 nM*h/mL
Volume of Distribution at Steady-State:
0.961 L/Kg
DOI Reference: 10.1021/acs.jmedchem.5c00121
Dose: 5 mg/Kg
Route of delivery:
Oral
Plasma half life:
2.83 h
Cmax:
5633 nM/mL
Area Under the Curve::
18284 nM*h/mL
Bioavailability:
65.5%
DOI Reference: 10.1021/acs.jmedchem.5c00121
Chemical Information
| Molecular Formula | C21H19N7O |
| SMILEs | Cc1cccc(-c2nn3c(c2-c2ccc4ncnn4c2/C=C/C(N)=O)CCC3)n1 |
| InChI | InChI=1S/C21H19N7O/c1-13-4-2-5-15(25-13)21-20(17-6-3-11-27(17)26-21)14-7-10-19-23-12-24-28(19)16(14)8-9-18(22)29/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,22,29)/b9-8+ |
| Molecular weight | 385.17 Da |
| AlogP | 2.40792 |
| HBond acceptors | 8 |
| HBond donors | 2 |
| Atoms | 48 |