PAMAPIMOD |
PAMAPIMOD : Inhibitor of MAPK14A
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| MAPK14 |
|
|
Inhibitor
1 µM necessary for cellular activity
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Ligand displacement at 10 μM test compound was assessed using the Ambit Biosciences kinase screen of ...
Potency Cellular
In Vitro
MAPK14
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/jm101423y
In Vivo Validations
Rat
Dose: 5 mg/Kg IV, PO
Route of delivery:
Intravenous, Oral
Plasma half life:
4.04 h PO
Systemic clearance:
1.26 (L/h)/kg IV
Cmax:
1.34 ug/mL PO
Tmax:
0.5 h PO
Area Under the Curve::
3.13 (24 h)μg·h/mL PO
Bioavailability:
80.1% PO
Volume of Distribution at Steady-State:
3.56 L/Kg IV
DOI Reference: 10.1021/jm101423y
Monkey (Cynomolgus)
Dose: 5 mg/Kg IV, PO
Route of delivery:
Intravenous, Oral
Plasma half life:
13.8 h PO
Systemic clearance:
0.65 (L/h)/Kg IV
Cmax:
1.86 ug/mL PO
Tmax:
1.50 h PO
Area Under the Curve::
9.41 (72h) μg·h/mL PO
Bioavailability:
>100% PO
Volume of Distribution at Steady-State:
20.6 L/Kg IV
DOI Reference: 10.1021/jm101423y
Dog
Dose: 5 mg/Kg
Route of delivery:
Intravenous, Oral
Plasma half life:
9.18 h PO
Systemic clearance:
0.75 (L/h)/kg IV
Cmax:
1.38 ug/mL PO
Tmax:
0.67 h PO
Area Under the Curve::
5.22 μg·h/mL PO
Bioavailability:
78.2% PO
Volume of Distribution at Steady-State:
12.7 L/Kg IV
DOI Reference: 10.1021/jm101423y
Chemical Information
| Molecular Formula | C19H20F2N4O4 |
| SMILEs | Cn1c(=O)c(Oc2ccc(F)cc2F)cc2cnc(NC(CCO)CCO)nc21 |
| InChI | InChI=1S/C19H20F2N4O4/c1-25-17-11(10-22-19(24-17)23-13(4-6-26)5-7-27)8-16(18(25)28)29-15-3-2-12(20)9-14(15)21/h2-3,8-10,13,26-27H,4-7H2,1H3,(H,22,23,24) |
| Molecular weight | 406.15 Da |
| AlogP | 1.9442999999999997 |
| HBond acceptors | 8 |
| HBond donors | 3 |
| Atoms | 49 |