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Compound Detail

CHEMBL169376

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O=C(O)CCC(NC(=O)c1ccc(CNc2ccc3ncnc(O)c3c2)cc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL169376
Phase Preclinical
Structure Type MOL
InChI Key DRAKYKMPCLOQIC-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

424.4
MW (Da)
2.00
ALogP
7
HBA
5
HBD
161.7
PSA (Ų)
0.35
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20N4O6
MW 424.41
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.75

Activity Summary

IC50 3 meas. best 6.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
IC50 6.5 6.5 320.0 1
L1210
CHEMBL386
IC50 6.28 6.28 530.0 1
Thymidylate synthase
CHEMBL3160
IC50 4.6 4.6 25000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2704031 10.1021/jm00124a019 L1210 2
2704031 10.1021/jm00124a019 Dihydrofolate reductase 1
2704031 10.1021/jm00124a019 Thymidylate synthase 1

Data from ChEMBL 36 via Core Engine