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Compound Detail

CHEMBL4856060

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CC(C)(C)OC(=O)NCC#Cc1ccc2c(c1)C=C([N+](=O)[O-])C(C(F)(F)F)O2

Basic Information

ChEMBL ID CHEMBL4856060
Phase Preclinical
Structure Type MOL
InChI Key LIKDQKPQARRCAR-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

398.3
MW (Da)
3.50
ALogP
5
HBA
1
HBD
90.7
PSA (Ų)
0.47
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17F3N2O5
MW 398.34
Aromatic Rings 1
Heavy Atoms 28
NP-Likeness -0.61

Activity Summary

Ki 3 meas. best 6.03
IC50 1 meas. best 5.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.03 6.03 940.0 1
P2Y purinoceptor 6
CHEMBL4714
IC50 5.92 5.92 1200.0 1
D(1B) dopamine receptor
CHEMBL1850
Ki 5.9 5.9 1250.0 1
D(3) dopamine receptor
CHEMBL234
Ki 5.77 5.77 1700.0 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 D(3) dopamine receptor 1

Data from ChEMBL 36 via Core Engine