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Compound Detail

CHEMBL30938

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COc1cc(OC)cc(N2C3CCC2CC(c2cnc(N)nc2N)C3)c1

Basic Information

ChEMBL ID CHEMBL30938
Phase Preclinical
Structure Type MOL
InChI Key JGPAZLDJBCRUKN-UHFFFAOYSA-N

Known Names

Ro-173279
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
1
Known Names

Molecular Properties

355.4
MW (Da)
2.57
ALogP
7
HBA
2
HBD
99.5
PSA (Ų)
0.87
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H25N5O2
MW 355.44
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.25

Activity Summary

IC50 3 meas. best 9.62
Ki 1 meas. best 9.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL2329
IC50 9.62 8.6 0.2 2
Dihydrofolate reductase
CHEMBL1809
Ki 9.31 9.31 0.5 1
Dihydrofolate reductase
CHEMBL2363
IC50 7.08 7.08 84.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14695838 10.1021/jm030931w Candida albicans 6
14695838 10.1021/jm030931w Dihydrofolate reductase 4
14695838 10.1021/jm030931w Nakaseomyces glabratus 3
3290487 10.1021/jm00402a025 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine