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Compound Detail

CHEMBL4875317

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O=C(Oc1cccc2c1C(=O)C=CC2=O)c1ccccc1

Basic Information

ChEMBL ID CHEMBL4875317
Phase Preclinical
Structure Type MOL
InChI Key RMNMUVXBOYSHJV-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

278.3
MW (Da)
2.84
ALogP
4
HBA
0
HBD
60.4
PSA (Ų)
0.63
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 C17H10O4
MW 278.26
Aromatic Rings 2
Heavy Atoms 21
NP-Likeness 0.41

Activity Summary

IC50 3 meas. best 5.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KB
CHEMBL398
IC50 5.19 5.19 6470.0 1
HeLa
CHEMBL399
IC50 4.89 4.89 13010.0 1
DNA topoisomerase 1
CHEMBL1781
IC50 4.04 4.04 90560.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KB IC50 = 6470.0 nM 5.19 Cytotoxicity against human KB cells 33766765
HeLa IC50 = 13010.0 nM 4.89 Cytotoxicity against human HeLa cells 33766765
DNA topoisomerase 1 IC50 = 90560.0 nM 4.04 Inhibition of DNA topoisomerase 1 (unknown origin) 33766765

Literature References

PubMed DOI Target Context # Activities
33766765 10.1016/j.bmcl.2021.127976 KB 1
33766765 10.1016/j.bmcl.2021.127976 HeLa 1
33766765 10.1016/j.bmcl.2021.127976 No relevant target 1
33766765 10.1016/j.bmcl.2021.127976 DNA topoisomerase 1 1

Data from ChEMBL 36 via Core Engine