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Compound Detail

CHEMBL5569615

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Nc1ncc(-c2ccc(Cl)c([N+](=O)[O-])c2)c(N)n1

Basic Information

ChEMBL ID CHEMBL5569615
Phase Preclinical
Structure Type MOL
InChI Key JHEFDWFRUMMPQA-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

265.7
MW (Da)
1.87
ALogP
6
HBA
2
HBD
121.0
PSA (Ų)
0.63
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H8ClN5O2
MW 265.66
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -1.36

Activity Summary

IC50 1 meas. best 4.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
IC50 4.76 4.76 17500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dihydrofolate reductase IC50 = 17500.0 nM 4.76 Inhibition of recombinant human DHFR using DHF as substrate measured for 1 hr in... 38071795

Literature References

PubMed DOI Target Context # Activities
38071795 10.1016/j.ejmech.2023.115971 Dihydrofolate reductase 4
38071795 10.1016/j.ejmech.2023.115971 MDA-MB-468 1
38071795 10.1016/j.ejmech.2023.115971 MDA-MB-231 1
38071795 10.1016/j.ejmech.2023.115971 MCF7 1
38071795 10.1016/j.ejmech.2023.115971 No relevant target 1

Data from ChEMBL 36 via Core Engine