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BMS-986458 | BMS-986458 : Degrader (PROTAC) of BCL6
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
BCL6
  • IC50:1.9 ± 0.8 nM
  • IC50:41 ± 12 nM
  • EC50:2.2 nM
  • GI50:0.6 nM
  • EC50:0.2 ± 0.1 nM
Degrader (PROTAC)
up to 100 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
In a panel of known CRBN neosubstrate assays, no degradation of CK1α, GSPT1, IKZF1, IZKF3, nor SALL4 ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
The selectivity of BMS-986458 was confirmed in a global proteomics study where BCL6 was the only sig ...

Potency
Cellular
In Vitro

BCL6

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5c03123

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.1 h
Systemic clearance: 6.67 mL/min/Kg
Area Under the Curve:: 3.98 uM*h
Volume of Distribution at Steady-State: 0.51 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c03123

Dose: 30 mg/Kg
Route of delivery: Oral
Cmax: 24.9 ± 3.5 uM
Tmax: 0.5 ± 0 h
Area Under the Curve:: 75.6 ± 20.3 uM*h
Bioavailability: 53%

DOI Reference: 10.1021/acs.jmedchem.5c03123

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.90 ± 0.07 h
Systemic clearance: 9.74 ± 2.10 mL/min/Kg
Area Under the Curve:: 2.80 ± 0.54 uM*h
Volume of Distribution at Steady-State: 0.28 ± 0.03 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c03123

Dose: 10 mg/Kg
Route of delivery: Oral
Cmax: 0.90 ± 0.07 uM
Tmax: 2.33 ± 0.58 h
Area Under the Curve:: 44.6 ± 4.4 uM*h
Bioavailability: ~100%

DOI Reference: 10.1021/acs.jmedchem.5c03123

Dog
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 4.6 ± 1.7 h
Systemic clearance: 0.85 ± 0.34 mL/min/Kg
Area Under the Curve:: 35.4 ± 16.3 uM*h
Volume of Distribution at Steady-State: 0.3 ± 0.2 L/Kg

DOI Reference: 10.1021/acs.jmedchem.5c03123

Dose: 3 mg/Kg
Route of delivery: Oral
Cmax: 15.1 ± 3.7 uM
Tmax: 2.0 ± 1.8 h
Area Under the Curve:: 72.2 ± 15.1 uM*h
Bioavailability: 67%

DOI Reference: 10.1021/acs.jmedchem.5c03123

Chemical Information

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Expert Reviews

by SERP
(on 23 Feb 2026)
Cellular Use Rating
In Model Organisms
This is an excellent degrader with respect to potency, selectivity and in vivo activity.
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria