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MRK-A | MRK-A : Inhibitor of TEAD1
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
TEAD1
  • ΔTm:9.65
  • EC50:3.4 nM
  • EC50:29 nM
  • EC50:328 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
The activity of MRK-A was profiled in Eurofins Cerep PanLab panel (Total number of assays: 108) usin ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
MRK-A was assessed against a panel of 247 Kinases @ 10 uM

Potency
Cellular
In Vitro

TEAD1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.5c02997

In Vivo Validations

Rat
Dose:
Route of delivery: Oral
Systemic clearance: 8 mL/min/Kg
Bioavailability: 96%
Volume of Distribution at Steady-State: 3.0 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c02997

Dog
Dose:
Route of delivery: Oral
Systemic clearance: 12 mL/min/Kg
Bioavailability: 44%
Volume of Distribution at Steady-State: 5.7 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c02997

Chemical Information

Coming Soon...

References

Publications

Cross References

Expert Reviews

No SERP comments found for MRK-A

Probe MRK-A is in the process of SERP review.

Please continue to check back for new reviews and commentary.