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SGC-CAF382-1 | SGC-CAF382-1 : Inhibitor of CDKL5
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDKL5
  • IC50:6.7 nM
  • IC50:10 nM
Inhibitor
< 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: Radiometric enzyme assays were run for CDKL1–4. When comparing the ...

Potency
Cellular
In Vitro

CDKL5

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.7554/eLife.88206

In Vivo Validations

Mouse
Dose: 2.29 mg/kg
Route of delivery: Intraperitoneal
Plasma half life: 0.738 h
Cmax: 508 ng/mL
Tmax: 0.5 h
Area Under the Curve:: 646 h*ng/mL

DOI Reference: 10.7554/eLife.88206

Negative Control Compounds

SGC-CAF268-1N
SMILES: O=C(C1=CC=NC(N2CCN(CC2)C)=C1)NC3=NC=C(S3)SCC4=CC=CC(C(F)(F)F)=C4

Chemical Information

Molecular Formula C16H22N4O2S2
SMILEs CC(C)c1cnc(CSc2cnc(NC(=O)C3CCNCC3)s2)o1
InChI InChI=1S/C16H22N4O2S2/c1-10(2)12-7-18-13(22-12)9-23-14-8-19-16(24-14)20-15(21)11-3-5-17-6-4-11/h7-8,10-11,17H,3-6,9H2,1-2H3,(H,19,20,21)
Molecular weight 366.12 Da
AlogP 0.0
HBond acceptors 6
HBond donors 2
Atoms 46

Expert Reviews

No SERP comments found for SGC-CAF382-1

Probe SGC-CAF382-1 is in the process of SERP review.

Please continue to check back for new reviews and commentary.