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Compound Detail

CHEMBL4848838

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

Basic Information

ChEMBL ID CHEMBL4848838
Phase Preclinical
Structure Type MOL
InChI Key OVXPWLPUGMYBAI-UHFFFAOYSA-N
5
Targets
5
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

340.3
MW (Da)
2.12
ALogP
4
HBA
1
HBD
81.5
PSA (Ų)
0.51
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 C15H11F3N2O4
MW 340.26
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -0.53

Activity Summary

Ki 4 meas. best 5.96
IC50 1 meas. best 5.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(1B) dopamine receptor
CHEMBL1850
Ki 5.96 5.96 1100.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 5.66 5.66 2200.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 5.36 5.36 4400.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 5.17 5.17 6700.0 1
P2Y purinoceptor 6
CHEMBL4714
IC50 5.12 5.12 7670.0 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
33831560 10.1016/j.bmcl.2021.128008 Alpha-2B adrenergic receptor 1

Data from ChEMBL 36 via Core Engine