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Compound Detail

CHEMBL124631

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Nc1nc(N)c2cc(CCc3ccc(C(=O)NC(CCC(=O)O)C(=O)O)cc3)cnc2n1

Basic Information

ChEMBL ID CHEMBL124631
Phase Preclinical
Structure Type MOL
InChI Key RGUQKUKRLMXLCM-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

438.4
MW (Da)
1.02
ALogP
8
HBA
5
HBD
194.4
PSA (Ų)
0.32
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 C21H22N6O5
MW 438.44
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.19

Activity Summary

IC50 5 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 7.77 7.67 17.0 2
NON-PROTEIN TARGET
CHEMBL3879801
IC50 7.43 7.43 37.0 1
Dihydrofolate reductase
CHEMBL2902
IC50 7.37 7.37 43.0 1
Thymidylate synthase
CHEMBL5328
IC50 4.04 4.04 92000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9022805 10.1021/jm950553y Mus musculus 24
4009615 10.1021/jm00145a012 Folylpolyglutamate synthase, mitochondrial 3
4009615 10.1021/jm00145a012 Mus musculus 2
4009615 10.1021/jm00145a012 Dihydrofolate reductase 1
4009615 10.1021/jm00145a012 Thymidylate synthase 1
4009615 10.1021/jm00145a012 L1210 1
9022805 10.1021/jm950553y L1210 1
9022805 10.1021/jm950553y NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine