Idelalisib | Idelalisib : Inhibitor of PIK3CD
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 reviews)
In Vivo
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIK3CD
  • IC50:2.5 nM
  • EC50:8 nM
Inhibitor
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
In cell-based assays, CAL-101 had 240- to 2500-fold selectivity for p110δ over the other class I PI3 ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
40- to 300-fold more selective for p110δ relative to other PI3K class I enzymes (IC50 p110δ = 2.5nM; ...

Potency
Cellular
In Vitro

PIK3CD

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1182/blood-2010-03-275305

Chemical Information

Molecular Formula C22H18FN7O
SMILEs CC[C@H](Nc1ncnc2[nH]cnc12)c1nc2cccc(F)c2c(=O)n1-c1ccccc1
InChI InChI=1S/C22H18FN7O/c1-2-15(28-20-18-19(25-11-24-18)26-12-27-20)21-29-16-10-6-9-14(23)17(16)22(31)30(21)13-7-4-3-5-8-13/h3-12,15H,2H2,1H3,(H2,24,25,26,27,28)/t15-/m0/s1
Molecular weight 415.16 Da
AlogP 0.0
HBond acceptors 8
HBond donors 2
Atoms 49

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews


(on 3 Jul 2023 )
Cellular Use Rating
This compound is likely to be a pan-p110 inhibitor unless used at <100 nM in cells
(on 18 Jul 2023 )
Cellular Use Rating
( The reviewer did not leave any comments )
(on 17 Jun 2024 )
Cellular Use Rating
This is a highly selective 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