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Compound Detail

CHEMBL116993

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CCc1cc(Cc2cnc(N)nc2N)cc(CC)c1OCCOCc1ccccc1

Basic Information

ChEMBL ID CHEMBL116993
Phase Preclinical
Structure Type MOL
InChI Key WYDKBAJLSXXPOM-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

406.5
MW (Da)
3.95
ALogP
6
HBA
2
HBD
96.3
PSA (Ų)
0.49
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N4O2
MW 406.53
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.39

Activity Summary

IC50 4 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
IC50 7.82 7.82 15.0 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL3963
IC50 7.47 7.47 34.0 1
Dihydrofolate reductase
CHEMBL3565
IC50 7.32 7.32 48.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.58 4.58 26000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3100802 10.1021/jm00385a017 Dihydrofolate reductase 3
3100802 10.1021/jm00385a017 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine