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DORAMAPIMOD | DORAMAPIMOD : Inhibitor of MAPK14
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
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
  • IC50:38 nM
  • Kd:0.45 nM
  • IC50:8 nM
  • EC50:780 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
The SafetyScreen44™ panel has been measured (@10 mM) for BIRB 796, and for 0/44 proteins >70% inhibi ...

Potency
Cellular
In Vitro

MAPK14

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm030121k

In Vivo Validations

Mouse
Dose: 1 mg/Kg (IV), 10 mg/Kg (PO)
Route of delivery: Intravenous, Oral
Systemic clearance: 0.33 mL/min/Kg IV
Cmax: 27000 ng/mL PO
Tmax: 1.0 h PO
Bioavailability: 23% PO
Volume of Distribution at Steady-State: 0.07 L/Kg IV

DOI Reference: 10.1021/jm030121k

Rat
Dose: 1 mg/Kg (IV), 10 mg/Kg (PO)
Route of delivery: Intravenous, Oral
Systemic clearance: 4% QH
Cmax: 5500 ng/ml PO
Bioavailability: 75% PO
Volume of Distribution at Steady-State: 0.2 L/Kg IV

DOI Reference: 10.1021/jm030121k

Orthogonal Probes def

Skepinone-L
SR-301
FS-694

Chemical Information

Molecular Formula C31H37N5O3
SMILEs Cc1ccc(-n2nc(C(C)(C)C)cc2NC(=O)Nc2ccc(OCCN3CCOCC3)c3ccccc23)cc1
InChI InChI=1S/C31H37N5O3/c1-22-9-11-23(12-10-22)36-29(21-28(34-36)31(2,3)4)33-30(37)32-26-13-14-27(25-8-6-5-7-24(25)26)39-20-17-35-15-18-38-19-16-35/h5-14,21H,15-20H2,1-4H3,(H2,32,33,37)
Molecular weight 527.29 Da
AlogP 5.98642
HBond acceptors 8
HBond donors 2
Atoms 76

Vendors

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Expert Reviews

by SERP
(on 17 Jun 2022 )
Cellular Use Rating
In Model Organisms
According to the literature the compound is very unselective. see: Fabian et al.: DOI: 10.1038/nbt1068; Karaman et al.: DOI 10.1038/nbt1358 With PH 797804, VX702, VX745 there are by far more selective...
by SERP
(on 4 Jul 2022 )
Cellular Use Rating
In Model Organisms
Cell-based modulation of THF-a by BIRB796 in THP1 cells has been demonstrated with an EC50 of 0,01 to 0.065 uM and in human whole blood with an EC50 of 0.78uM( https://pubs.acs.org/doi/10.1021/jm030121k)....
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