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Compound Detail

CHEMBL417982

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OCc1cc2c3ccccc3nc-2c[nH]1

Basic Information

ChEMBL ID CHEMBL417982
Phase Preclinical
Structure Type MOL
InChI Key MRZIXPOFRWIKDR-UHFFFAOYSA-N
1
Targets
3
Activities
2
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

198.2
MW (Da)
2.16
ALogP
2
HBA
2
HBD
48.9
PSA (Ų)
0.63
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H10N2O
MW 198.22
Aromatic Rings 1
Heavy Atoms 15
NP-Likeness -0.23

Activity Summary

Ki 2 meas. best 5.83
IC50 1 meas. best 5.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
IC50 5.83 5.83 1470.0 1
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.83 5.83 1470.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26235951 10.1016/j.bmcl.2015.07.058 NON-PROTEIN TARGET 3
6127411 10.1021/jm00351a015 GABA-A receptor; anion channel 2
3031296 10.1021/jm00387a033 GABA-A receptor; anion channel 1
6325688 10.1021/jm00371a002 GABA-A receptor; anion channel 1
26235951 10.1016/j.bmcl.2015.07.058 HL-60 1
26235951 10.1016/j.bmcl.2015.07.058 A498 1
26235951 10.1016/j.bmcl.2015.07.058 COLO 205 1
26235951 10.1016/j.bmcl.2015.07.058 SK-OV-3 1
26235951 10.1016/j.bmcl.2015.07.058 Detroit 551 1

Data from ChEMBL 36 via Core Engine