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Compound Detail

CHEMBL253581

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COc1ccc(Cn2c(C)cc3nc(N)[nH]c(=O)c32)cc1

Basic Information

ChEMBL ID CHEMBL253581
Phase Preclinical
Structure Type MOL
InChI Key JRTRRGFUCMJTIT-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

284.3
MW (Da)
1.67
ALogP
5
HBA
2
HBD
85.9
PSA (Ų)
0.77
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H16N4O2
MW 284.32
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -0.95

Activity Summary

IC50 4 meas. best 5.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Thymidylate synthase
CHEMBL1952
IC50 5.82 5.82 1500.0 1
Unchecked
CHEMBL612545
IC50 5.46 5.115 3500.0 2
Thymidylate synthase
CHEMBL6137
IC50 4.82 4.82 15000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18072727 10.1021/jm701052u Unchecked 5
18072727 10.1021/jm701052u Thymidylate synthase 2
18072727 10.1021/jm701052u Dihydrofolate reductase 2

Data from ChEMBL 36 via Core Engine