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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

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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

Vendors

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

Expert Reviews

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