LNP-023 | Inhibitor of CFB
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CFB
  • Kd:7.9 nM
  • IC50:12 nM
  • IC50:130 nM
  • IC50:110 nM
  • IC50:150 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
IC50 values of >30 μM across a panel of 41 human proteases, including the AP protein factor D ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
LNP023 provided IC50 values of >30 μM across an internal panel of ∼110 enzymes, receptors, and ...

Potency
Cellular
In Vitro

CFB

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1073/pnas.1820892116

In Vivo Validations

Mouse, Rat, Dog
Dose: 1 to 30 mg/Kg (R), 0.1 to 10 mg/Kg (D), 1 (IV), 10 (PO) mg/Kg (m)
Route of delivery: Intravenous, Oral
Plasma half life: 7 (R) , 5.6 (D) 7.2 (m) h
Systemic clearance: 8 (R), 2 (D), 16 (m) mL/min/Kg

DOI Reference: 10.1073/pnas.1820892116

Chemical Information

Molecular Formula C25H30N2O4
SMILEs CCO[C@H]1CCN(Cc2c(OC)cc(C)c3[nH]ccc23)[C@H](c2ccc(C(=O)O)cc2)C1
InChI InChI=1S/C25H30N2O4/c1-4-31-19-10-12-27(22(14-19)17-5-7-18(8-6-17)25(28)29)15-21-20-9-11-26-24(20)16(2)13-23(21)30-3/h5-9,11,13,19,22,26H,4,10,12,14-15H2,1-3H3,(H,28,29)/t19-,22-/m0/s1
Molecular weight 422.22 Da
AlogP 4.925320000000004
HBond acceptors 6
HBond donors 2
Atoms 61

References

Cross References

Vendors

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Expert Reviews


(on 12 Mar 2021 )
Cellular Use Rating
In Model Organisms
LNP023 is a first in class, potent reversible inhibitor of the serine protease factor B (FB). This protease is a key component of the alternative complement pathway. This pathway is dysregulated in...
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