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CBPD-268 | CBPD-268 : Degrader (PROTAC) of CREBBP and EP300
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CREBBP
  • IC50:11 nM
  • DC50:0.5 nM
  • DC50:0.01 nM
  • DC50:0.01 nM
  • DC50:0.02 nM
  • IC50:3.7 nM
  • IC50:10.3 nM
  • IC50:4.6 nM
EP300
  • IC50:9.5 nM
  • DC50:0.8 nM
  • DC50:0.03 nM
  • DC50:0.03 nM
  • DC50:<0.01 nM
Degrader (PROTAC)
up to 10 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
To investigate the degradation selectivity of CBPD-268 on a global level in an unbiased manner, a pr ...
Selectivity Assessment Description:
CBPD-268 showed a profound and significant depletion of CBP/p300 proteins, with the CBP and p300 pro ...

Potency
Cellular
In Vitro

CREBBP

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c02124

EP300

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c02124

In Vivo Validations

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.9 h
Systemic clearance: 34.6 mL/min/Kg
Volume of Distribution at Steady-State: 4.9 L/Kg

DOI Reference: 10.1021/acs.jmedchem.3c02124

Dose: 3 mg/Kg
Route of delivery: Oral
Plasma half life: 1.3 h
Cmax: 220.6 ng/mL
Area Under the Curve:: 936.9 h*ng/mL
Bioavailability: 67%

DOI Reference: 10.1021/acs.jmedchem.3c02124

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 3.4 h
Systemic clearance: 6.0 mL/min/Kg
Volume of Distribution at Steady-State: 1.6 L/Kg

DOI Reference: 10.1021/acs.jmedchem.3c02124

Dose: 3 mg/Kg
Route of delivery: Oral
Plasma half life: 3.1 h
Cmax: 724.7 ng/mL
Area Under the Curve:: 4190.4 h*ng/mL
Bioavailability: 60%

DOI Reference: 10.1021/acs.jmedchem.3c02124

Chemical Information

Molecular Formula C44H47F2N9O5
SMILEs CC(=O)N1CCc2c(c(N3CCCc4cc(-c5cnn(C)c5)c(C(F)F)cc43)nn2[C@H]2CC[C@H](CN3Cc4cc5c(cc4C3)C(=O)N(C3CCC(=O)NC3=O)C5=O)CC2)C1
InChI InChI=1S/C44H47F2N9O5/c1-24(56)52-13-11-36-35(23-52)41(53-12-3-4-26-14-31(29-18-47-50(2)20-29)32(40(45)46)17-38(26)53)49-55(36)30-7-5-25(6-8-30)19-51-21-27-15-33-34(16-28(27)22-51)44(60)54(43(33)59)37-9-10-39(57)48-42(37)58/h14-18,20,25,30,37,40H,3-13,19,21-23H2,1-2H3,(H,48,57,58)/t25-,30-,37?
Molecular weight 819.37 Da
AlogP 5.358400000000005
HBond acceptors 14
HBond donors 1
Atoms 107
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

Cross References

canSARChEMBL

Expert Reviews

by SERP
(on 23 Dec 2025 )
Cellular Use Rating
In Model Organisms
The compound appears to be active in a single cell line at an IC50 of 11 nM. However, as a degrader, total protein loss is seen at much lower doses, so this dosing feels sensible for the proposed MoA. Mouse...
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