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Compound Detail

CHEMBL162270

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COc1cc(N(C)Cc2cccc3nc(N)nc(N)c23)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL162270
Phase Preclinical
Structure Type MOL
InChI Key RJJKDQLFIKMANF-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

369.4
MW (Da)
2.46
ALogP
8
HBA
2
HBD
108.8
PSA (Ų)
0.68
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 C19H23N5O3
MW 369.43
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.67

Activity Summary

IC50 1 meas. best 4.28
Ki 1 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL202
Ki 7.31 7.31 49.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.28 4.28 53000.0 1

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