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PI-3065 | Inhibitor of PIK3CD
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
PIK3CD
  • Ki, IC50:1.5 nM; 15 nM
  • IC50:36, 38 nM
Inhibitor
up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selective against PI3K family members: p110alpha, beta and gamma (1.1, 2.3, 27.5 uM). No signific ...

Potency
Cellular
In Vitro

PIK3CD

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

Mouse
Dose: 75 mg/Kg
Route of delivery: Oral

Reference: --

Orthogonal Probes def

Pictilisib, Idelalisib

Chemical Information

Molecular Formula C27H31FN6OS
SMILEs Fc1ccc2[nH]ccc2c1-c1nc(N2CCOCC2)c2sc(CN3CCN(CC4CC4)CC3)cc2n1
InChI InChI=1S/C27H31FN6OS/c28-21-3-4-22-20(5-6-29-22)24(21)26-30-23-15-19(17-33-9-7-32(8-10-33)16-18-1-2-18)36-25(23)27(31-26)34-11-13-35-14-12-34/h3-6,15,18,29H,1-2,7-14,16-17H2
Molecular weight 506.23 Da
AlogP 4.342900000000004
HBond acceptors 7
HBond donors 1
Atoms 67

References

Publications

    Cross References

    canSARChEMBLBindingDBPubMed

    Vendors

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    Expert Reviews

    by SERP
    (on 5 Jun 2021 )
    Cellular Use Rating
    In Model Organisms
    PI-3065 is an older and well-studied PI3Kdelta inhibitor. The compound lacks a negative control and overall, off-target evaluation is somewhat modest. While the selectivity within the family has been...
    by SERP
    (on 25 Jun 2021 )
    Cellular Use Rating
    In Model Organisms
    ( The reviewer did not leave any comments )
    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