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Compound Detail

CHEMBL45735

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Nc1nc(N)c2nc(CNc3ccc(C(=O)NC(CCC(=O)Nc4ccccc4)C(=O)O)cc3)cnc2n1

Basic Information

ChEMBL ID CHEMBL45735
Phase Preclinical
Structure Type MOL
InChI Key XOSBKXWUQHSWSX-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

515.5
MW (Da)
1.80
ALogP
10
HBA
6
HBD
211.1
PSA (Ų)
0.18
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25N9O4
MW 515.53
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.77

Activity Summary

IC50 6 meas. best 8.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
L1210
CHEMBL386
IC50 8.46 7.3 3.5 3
Dihydrofolate reductase
CHEMBL4564
IC50 7.22 7.22 60.0 1
Homo sapiens
CHEMBL372
IC50 5.75 5.54 1800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
3462394 10.1021/jm00159a023 Mus musculus 13
3462394 10.1021/jm00159a023 L1210 3
3462394 10.1021/jm00159a023 Dihydrofolate reductase 2
3462394 10.1021/jm00159a023 Homo sapiens 2

Data from ChEMBL 36 via Core Engine