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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

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