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Compound Detail

CHEMBL24503

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C=CCc1cc(Cc2cnc(N)nc2N)cc(CCC)c1O

Basic Information

ChEMBL ID CHEMBL24503
Phase Preclinical
Structure Type MOL
InChI Key RZABJMIODMWRPV-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

298.4
MW (Da)
2.62
ALogP
5
HBA
3
HBD
98.0
PSA (Ų)
0.71
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H22N4O
MW 298.39
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 0.55

Activity Summary

IC50 5 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
IC50 7.7 7.7 20.0 1
Dihydrofolate reductase
CHEMBL4012
IC50 7.7 7.7 20.0 1
Dihydrofolate reductase
CHEMBL1809
IC50 7.62 7.62 24.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 5.7 5.57 2000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
2754716 10.1021/jm00128a043 Dihydrofolate reductase 3
3121854 10.1021/jm00396a018 Dihydrofolate reductase 2
2754716 10.1021/jm00128a043 Klebsiella aerogenes 1
- 10.6019/CHEMBL3433997 Glucose transporter 1
2754716 10.1021/jm00128a043 Bacteroides thetaiotaomicron 1
2754716 10.1021/jm00128a043 Phocaeicola vulgatus 1
2754716 10.1021/jm00128a043 Clostridioides difficile 1
2754716 10.1021/jm00128a043 Clostridium perfringens 1
2754716 10.1021/jm00128a043 Fusobacterium nucleatum 1
2754716 10.1021/jm00128a043 Bacteroides fragilis 1
2754716 10.1021/jm00128a043 Proteus vulgaris 1
2754716 10.1021/jm00128a043 Streptococcus pyogenes 1
2754716 10.1021/jm00128a043 Klebsiella pneumoniae 1
2754716 10.1021/jm00128a043 Serratia marcescens 1
2754716 10.1021/jm00128a043 Escherichia coli 1
2754716 10.1021/jm00128a043 Shigella flexneri 1
2754716 10.1021/jm00128a043 NON-PROTEIN TARGET 1
2754716 10.1021/jm00128a043 Mycolicibacterium smegmatis 1
2754716 10.1021/jm00128a043 Pasteurella multocida 1

Data from ChEMBL 36 via Core Engine