BenevolentAl Therapeutics Pipeline and Triage
Inhibition of Target A has antifibrotic effect in TGF-☐ activated
primary human hepatic stellate cells
Fibroblast to myofibroblast transition
aSMA
150
Run 1
Mean +/- SD
Collagen
a-SMA/Col 1 mean cellular intensity
TGF-
HSCs, TGFb, 72h
1750-
1250
1000
1500-
1250-
1000-
750-
500-
- 750
- 500
250
250-
0
0
0.01
0.1
1
10
TGF+ [ng/ml]
Source: Company internal drug programme
O Cells per well
% inhibition
% inhibition
100-
50-
-50-
-8
-7
-6
-5
Log Compound [M]
150
Run 2
Mean +/- SD
100
50-
Nuceli Count
α-SMA
→ Collagen I
Tool compound
Target A SPR KD 17nM
Cell-based TE assay IC 50 5.4nM
WLP >30-fold selectivity
Kinome profiling >200-fold
selectivity
No effect on cell viability
a-SMA
Collagen 1
Nuclei
Count
RUN 1
(IC50)
9.5nM
7.OnM
2.3μM
D
-8
-7
-6
-5
RUN 2
9.6nM
5.3nM
-50
Log Compound [M]
(IC50)
1.4μM
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