MU1742 |
Inhibitor of CSNK1D, CSNK1E
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| CSNK1D |
|
|
| CSNK1E |
|
|
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
The selectivity profile of MU1742 was determined by a kinome-wide screening against 415 protein kina ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
NanoBRET excludes CK1alpha and p38a as cellular targets for MU1742
Potency Cellular
In Vitro
CSNK1D
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1002/anie.202217532
CSNK1E
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1002/anie.202217532
In Vivo Validations
Mouse
Dose: 20 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
45.70 min
Cmax:
6.71 uM
Area Under the Curve::
0.27 uM*min/L
DOI Reference: 10.1002/anie.202217532
Dose: 20 mg/Kg
Route of delivery:
Oral
Plasma half life:
58.50 h
Cmax:
1.58 uM
Tmax:
15 min
Area Under the Curve::
0.15 uM*min/mL
DOI Reference: 10.1002/anie.202217532
Negative Control Compounds
MU2027
Notes: MU2027 was assessed in biochemical and NanoBRET cellular assay and it proved inactive.
Chemical Information
| Molecular Formula | C22H22F2N6 |
| SMILEs | CN1CCC(F)(Cn2cnc(-c3ccc(F)cn3)c2-c2ccnc3[nH]ccc23)CC1 |
| InChI | InChI=1S/C22H22F2N6/c1-29-10-6-22(24,7-11-29)13-30-14-28-19(18-3-2-15(23)12-27-18)20(30)16-4-8-25-21-17(16)5-9-26-21/h2-5,8-9,12,14H,6-7,10-11,13H2,1H3,(H,25,26) |
| Molecular weight | 408.19 Da |
| AlogP | 4.061400000000003 |
| HBond acceptors | 6 |
| HBond donors | 1 |
| Atoms | 52 |