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Compound Detail

CHEMBL350730

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COc1ccc(OC)c(NCc2cccc3nc(N)nc(N)c23)c1

Basic Information

ChEMBL ID CHEMBL350730
Phase Preclinical
Structure Type MOL
InChI Key PEPWPBUTUYSCAU-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

325.4
MW (Da)
2.42
ALogP
7
HBA
3
HBD
108.3
PSA (Ų)
0.66
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 C17H19N5O2
MW 325.37
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.96

Activity Summary

Ki 2 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
Ki 7.48 7.09 33.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
7877140 10.1021/jm00005a002 Dihydrofolate reductase 5
7877140 10.1021/jm00005a002 Bifunctional dihydrofolate reductase-thymidylate synthase 1
7877140 10.1021/jm00005a002 Dihydrofolate reductase; P. carinii vs rat 1
7877140 10.1021/jm00005a002 Dihydrofolate reductase; T. gondii vs rat 1

Data from ChEMBL 36 via Core Engine