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Compound Detail

CHEMBL357217

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COC1=CC(=O)c2c(c(COc3ccc([N+](=O)[O-])cc3)c(C)n2C)C1=O

Basic Information

ChEMBL ID CHEMBL357217
Phase Preclinical
Structure Type MOL
InChI Key IBLWSLZYYZHSRG-UHFFFAOYSA-N

Known Names

ES-936
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
1
Known Names

Molecular Properties

356.3
MW (Da)
2.73
ALogP
7
HBA
0
HBD
100.7
PSA (Ų)
0.60
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C18H16N2O6
MW 356.33
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.11

Activity Summary

IC50 4 meas. best 6.29
Ki 1 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NAD(P)H dehydrogenase [quinone] 1
CHEMBL3623
Ki 6.35 6.35 450.0 1
MIA PaCa-2
CHEMBL614725
IC50 6.29 6.245 508.0 2
NCI-H596
CHEMBL612256
IC50 5.7 5.7 2000.0 1
NCI-H460
CHEMBL396
IC50 5.55 5.55 2810.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29712428 10.1021/acs.jmedchem.8b00124 NAD(P)H dehydrogenase [quinone] 1 3
9822546 10.1021/jm980328r NAD(P)H dehydrogenase [quinone] 1 2
17944451 10.1021/jm070396q MIA PaCa-2 2
9822546 10.1021/jm980328r NCI-H460 1
9822546 10.1021/jm980328r NCI-H596 1
9822546 10.1021/jm980328r Unchecked 1
17944451 10.1021/jm070396q NAD(P)H dehydrogenase [quinone] 1 1

Data from ChEMBL 36 via Core Engine