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Compound Detail

CHEMBL423297

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CC(=O)NCCCC(NC(=O)c1ccc(NCc2cnc3nc(N)nc(N)c3n2)cc1)C(=O)O

Basic Information

ChEMBL ID CHEMBL423297
Phase Preclinical
Structure Type MOL
InChI Key RQVSBXOGFNAFLR-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
0.30
ALogP
10
HBA
6
HBD
211.1
PSA (Ų)
0.22
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H25N9O4
MW 467.49
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.61

Activity Summary

IC50 3 meas. best 7.77
Ki 1 meas. best 4.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 7.77 7.77 17.0 1
Dihydrofolate reductase
CHEMBL4564
IC50 7.55 7.55 28.0 1
Unchecked
CHEMBL612545
Ki 4.17 4.17 68000.0 1
L1210 ( R81)
CHEMBL614710
IC50 4.09 4.09 81000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3385730 10.1021/jm00402a013 Dihydrofolate reductase 1
3385730 10.1021/jm00402a013 Unchecked 1
3385730 10.1021/jm00402a013 L1210 1
3385730 10.1021/jm00402a013 L1210 ( R81) 1

Data from ChEMBL 36 via Core Engine