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Compound Detail

CHEMBL424135

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COc1ccc(OC)c(NCc2cnc3nc(N)nc(N)c3c2)c1

Basic Information

ChEMBL ID CHEMBL424135
Phase Preclinical
Structure Type MOL
InChI Key YSSYHMDWUMVMEA-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

326.4
MW (Da)
1.82
ALogP
8
HBA
3
HBD
121.2
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H18N6O2
MW 326.36
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.92

Activity Summary

IC50 5 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
IC50 6.35 5.78 450.0 2
Dihydrofolate reductase
CHEMBL2363
IC50 6.3 5.8 500.0 2
Unchecked
CHEMBL612545
IC50 5.21 5.21 6100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14584957 10.1021/jm030312n Dihydrofolate reductase 3
14584957 10.1021/jm030312n Unchecked 2
14584957 10.1021/jm030312n Pneumocystis carinii 1
14584957 10.1021/jm030312n Toxoplasma gondii 1
31176699 10.1016/j.bmcl.2019.06.004 Unchecked 1
31176699 10.1016/j.bmcl.2019.06.004 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine