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PZ2891 | PZ2891 : Modulator of PANK1, PANK2 and PANK3, acting as allosteric activator and orthosteric inhibitor
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
PANK1
  • IC50:40.2 ± 4.4 nM
  • K 0.5:8.7 ± 2.6 uM
PANK2
  • IC50:0.7 ± 0.08 nM
  • K 0.5:8.7 ± 2.6 uM
PANK3
  • IC50:1.3 ± 0.2 nM
  • Kd: 0.203 nM
  • K 0.5:8.7 ± 2.6 uM
Allosteric Activator, Orthosteric Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
PZ-2891 did not have significant inhibitory activity in a screen of 468 mammalian kinases. <p> ...

Potency
Cellular
In Vitro

PANK1

Mode of Action: Allosteric Activator, Orthosteric Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/s41467-018-06703-2

PANK2

Mode of Action: Allosteric Activator, Orthosteric Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/s41467-018-06703-2

PANK3

Mode of Action: Allosteric Activator, Orthosteric Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1038/s41467-018-06703-2

In Vivo Validations

Mouse
Dose: 2 (IV), 10 (PO) mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 0.28 h (IV)
Systemic clearance: 54.51 (IV) ml/min/Kg

DOI Reference: 10.1038/s41467-018-06703-2

Negative Control Compounds

PZ-3067

Chemical Information

Molecular Formula C20H23N5O
SMILEs CC(C)c1ccc(CC(=O)N2CCN(c3ccc(C#N)nn3)CC2)cc1
InChI InChI=1S/C20H23N5O/c1-15(2)17-5-3-16(4-6-17)13-20(26)25-11-9-24(10-12-25)19-8-7-18(14-21)22-23-19/h3-8,15H,9-13H2,1-2H3
Molecular weight 349.19 Da
AlogP 2.3629800000000003
HBond acceptors 6
HBond donors --
Atoms 49

References

Publications

Cross References

canSARChEMBLBindingDBPDBPubMed

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Expert Reviews

by SERP
(on 11 Oct 2021 )
Cellular Use Rating
In Model Organisms
I recommend PZ-2891 is a chemical probe for the PANK family, particularly for studying activation effects. PZ-2891 has an intriguing mechanism of action where it serves as either an orthosteric inhibitor...
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