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TP-004 | TP-004 : Inhibitor of METAP2
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
METAP2
  • IC50:5 nM
  • IC50:31 nM
  • EC50:15 nM
Inhibitor
200 nM to 1 uM

Selectivity

In Cell Selectivity Assessment
Selectivity Assessment Description:
> 100 fold. Evaluated in a Ricerca Comprehensive Pharmacological Profile panel of 100 biological tar ...

Potency
Cellular
In Vitro

METAP2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.bmcl.2016.04.072

In Vivo Validations

Rat, Mouse
Dose: 30 mg/Kg, 10 mg/Kg, 5 mg/Kg
Route of delivery: Oral
Plasma half life: 6 h
Systemic clearance: 17.2 ml/min/Kg

Reference: --

Negative Control Compounds

TPn-004

Chemical Information

Molecular Formula C17H16F3N5O
SMILEs Cc1nc(N2CC[C@@H](O)C2)ncc1-c1cc(C(F)(F)F)cc2[nH]ncc12
InChI InChI=1S/C17H16F3N5O/c1-9-13(6-21-16(23-9)25-3-2-11(26)8-25)12-4-10(17(18,19)20)5-15-14(12)7-22-24-15/h4-7,11,26H,2-3,8H2,1H3,(H,22,24)/t11-/m1/s1
Molecular weight 363.13 Da
AlogP 2.91812
HBond acceptors 6
HBond donors 2
Atoms 42

References

Publications

Cross References

SGC additional analysis

Vendors

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Expert Reviews

by SERP
(on 2 Jun 2020 )
Cellular Use Rating
In Model Organisms
The probe was evaluated against a panel of 100 GPCR receptors, ion channels, transporters and enzymes, (referred to as the Ricerca Comprehensive Pharmacological Profile screen) and 26 proteases and...
by SERP
(on 30 Jul 2020 )
Cellular Use Rating
In Model Organisms
My reasons for concern in recommending this probe are that much of the data reported for this compound is not publicly available. For example, a selectivity profile of >1000 is reported in this form...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria