BI-7190 |
BI-7190 : Inhibitor of BPTF
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| BPTF |
|
|
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
No significant hits were observed in Kinase and CEREP panel. BI-7190 shows high selectivity at 10 µM ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
NanoBRET EC50 BRD9 1100 nM, BRPF1 2960 nM, CECR2 13200 nM
Potency Cellular
In Vitro
BPTF
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? No
DOI Reference: 10.1002/cmdc.202200686
In Vivo Validations
Mouse
Dose: 5 mg/kg
Route of delivery:
Intravenous
Plasma half life:
0.6 h (MRT)
Systemic clearance:
64% QH
Volume of Distribution at Steady-State:
2.1 L/Kg
DOI Reference: 10.1002/cmdc.202200686
Dose: 30 mg/Kg
Route of delivery:
Oral
Cmax:
7,900 nM
Tmax:
1 h
Area Under the Curve::
33,200 nM∙h
Bioavailability:
145%
DOI Reference: 10.1002/cmdc.202200686
Negative Control Compounds
BI-4827
Notes: BI-4827 (BPTF KD (BPTF, DiscoveRx) > 10µM) is an inactive analog of BI-7190 and can be used as negative control for in vitro experiments.
SMILES:
CN1CCN(CC1)C(=O)C1=CC=C(C2=CN(C)C(=O)C(C)=C2)C(=C1)C(F)(F)F
Chemical Information
| Molecular Formula | C23H31N3O2 |
| SMILEs | COc1cc(-c2cn(C)c(=O)c(C)c2C)ccc1C1(N2CCN(C)CC2)CC1 |
| InChI | InChI=1S/C23H31N3O2/c1-16-17(2)22(27)25(4)15-19(16)18-6-7-20(21(14-18)28-5)23(8-9-23)26-12-10-24(3)11-13-26/h6-7,14-15H,8-13H2,1-5H3 |
| Molecular weight | 381.24 Da |
| AlogP | 2.9142400000000013 |
| HBond acceptors | 5 |
| HBond donors | -- |
| Atoms | 59 |