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CPI-0610 | CPI-0610 : BET family (BRD2, BRD4, BRD3, BRDT) inhibitor
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
BRD2
  • IC50:160 nM BD1, 25 nM BD2
  • EC50:180 nM
BRD4
  • IC50:39 nM
  • IC50:120 nM BD1, 18 nM BD2
  • EC 50:180 nM
BRD3
  • IC50:170 nM BD1, 21 nM BD2
  • EC50:180 nM
BRDT
  • IC50:220nM BD1, 130 nM BD2
  • EC50:180 nM
Inhibitor
10-500 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
CPI-0610 had IC50s>15 uM against other bromodomain proteins in Alphalisa assays (CBP, BRD9, BRPF1, P ...

Potency
Cellular
In Vitro

BRD2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b01882

BRD4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b01882

BRD3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b01882

BRDT

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.5b01882

In Vivo Validations

Mouse
Dose: 30 mg/kg (oral), 10 mg/kg (SC)
Route of delivery: Oral, Subcutaneous
Organ of interest (O): MV4-11 xenograft
Target engagement assay: Indirect, Myc expression assay

DOI Reference: 10.1021/acs.jmedchem.5b01882

Orthogonal Probes def

JQ1
PFI-1
MT1

Chemical Information

Molecular Formula C20H16ClN3O2
SMILEs Cc1noc2c1-c1ccccc1C(c1ccc(Cl)cc1)=N[C@H]2CC(N)=O
InChI InChI=1S/C20H16ClN3O2/c1-11-18-14-4-2-3-5-15(14)19(12-6-8-13(21)9-7-12)23-16(10-17(22)25)20(18)26-24-11/h2-9,16H,10H2,1H3,(H2,22,25)/t16-/m0/s1
Molecular weight 365.09 Da
AlogP 4.070920000000003
HBond acceptors 5
HBond donors 2
Atoms 42

References

Publications

Cross References

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Expert Reviews

by SERP
(on 19 May 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 22 May 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 13 Jul 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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