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Compound Detail

CHEMBL283702

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Nc1nc(N)c2nc(CN(C=O)c3ccc(C(=O)NC(CCCNC(=O)c4ccc(Cl)cc4)C(=O)O)cc3)cnc2n1

Basic Information

ChEMBL ID CHEMBL283702
Phase Preclinical
Structure Type MOL
InChI Key XVKWCKAUCRQXJE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

592.0
MW (Da)
1.79
ALogP
10
HBA
5
HBD
219.4
PSA (Ų)
0.12
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26ClN9O5
MW 592.02
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.52

Activity Summary

IC50 2 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL4564
IC50 7.82 7.82 15.0 1
L1210
CHEMBL386
IC50 6.7 6.7 200.0 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