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Compound Detail

CHEMBL4851349

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C[Si](C)(C)C#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2

Basic Information

ChEMBL ID CHEMBL4851349
Phase Preclinical
Structure Type MOL
InChI Key BXRYWEUVCDCBRM-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

341.4
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H14F3NO3Si
MW 341.36

Activity Summary

Ki 3 meas. best 5.85
IC50 1 meas. best 6.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 6
CHEMBL4714
IC50 6.11 6.11 785.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 5.85 5.85 1400.0 1
D(1B) dopamine receptor
CHEMBL1850
Ki 5.38 5.38 4200.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 5.33 5.33 4700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33831560 10.1016/j.bmcl.2021.128008 P2Y purinoceptor 6 1
33831560 10.1016/j.bmcl.2021.128008 Alpha-2A adrenergic receptor 1
33831560 10.1016/j.bmcl.2021.128008 D(1B) dopamine receptor 1
33831560 10.1016/j.bmcl.2021.128008 Sigma non-opioid intracellular receptor 1 1
36089113 10.1016/j.bmcl.2022.128981 P2Y purinoceptor 1 1
36089113 10.1016/j.bmcl.2022.128981 P2Y purinoceptor 2 1
36089113 10.1016/j.bmcl.2022.128981 P2Y purinoceptor 4 1
36089113 10.1016/j.bmcl.2022.128981 HEK293 1

Data from ChEMBL 36 via Core Engine