CCT251455 | CCT251455 : Inhibitor of TTK
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
TTK
  • IC50:3 nM
  • IC50:43 nM
  • GI50:160 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
High selectivity versus kinases tested in a broad kinome profiling panel.

Potency
Cellular
In Vitro

TTK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm401395s

In Vivo Validations

Mouse
Dose: 5 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 4.2 h
Systemic clearance: 23.8 mL/min/kg
Fb : 99.93%
Bioavailability: 83%
Volume of Distribution at Steady-State: 2.3 L/Kg

DOI Reference: 10.1021/jm401395s

Rat
Dose: 5 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 3.1 h
Systemic clearance: 7.04 mL/min/kg
Bioavailability: 32%
Volume of Distribution at Steady-State: 1.75 L/Kg

DOI Reference: 10.1021/jm401395s

Orthogonal Probes def

CFI-402257
BAY1217389
MPS1-IN-1

Chemical Information

Molecular Formula C26H26ClN7O2
SMILEs Cn1cc(-c2cc3cnc(Nc4ccc(-c5cncn5C)cc4Cl)cc3n2C(=O)OC(C)(C)C)cn1
InChI InChI=1S/C26H26ClN7O2/c1-26(2,3)36-25(35)34-21(18-12-30-33(5)14-18)9-17-11-29-24(10-22(17)34)31-20-7-6-16(8-19(20)27)23-13-28-15-32(23)4/h6-15H,1-5H3,(H,29,31)
Molecular weight 503.18 Da
AlogP 6.0175
HBond acceptors 9
HBond donors 1
Atoms 62

Vendors

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Expert Reviews


No SERP comments found for CCT251455

Probe CCT251455 is in the process of SERP review.

Please continue to check back for new reviews and commentary.