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Compound Detail

CHEMBL13820

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COc1cc(Cc2cnc(N)nc2N)cc(OCCC(=O)O)c1OC

Basic Information

ChEMBL ID CHEMBL13820
Phase Preclinical
Structure Type MOL
InChI Key LRSUQXJTLJXWDF-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
1.10
ALogP
8
HBA
3
HBD
142.8
PSA (Ų)
0.64
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H20N4O5
MW 348.36
Aromatic Rings 2
Heavy Atoms 25

Activity Summary

Ki 3 meas. best 9.43
IC50 1 meas. best 4.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
Ki 9.43 9.43 0.4 3
Dihydrofolate reductase
CHEMBL2363
IC50 4.13 4.13 74000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3973902 10.1021/jm00381a008 Dihydrofolate reductase 3
6754932 10.1021/jm00352a002 ADMET 1
6754932 10.1021/jm00352a002 Dihydrofolate reductase 1
3973902 10.1021/jm00381a008 Staphylococcus aureus 1
3973902 10.1021/jm00381a008 Escherichia coli 1
3973902 10.1021/jm00381a008 NON-PROTEIN TARGET 1
3973902 10.1021/jm00381a008 Proteus vulgaris 1
3290487 10.1021/jm00402a025 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine