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Compound Detail

CHEMBL3234115

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COc1ccc(-c2ccccc2)cc1C(C)C#Cc1c(C)nc(N)nc1N

Basic Information

ChEMBL ID CHEMBL3234115
Phase Preclinical
Structure Type MOL
InChI Key PFZXPVFWXCUAJW-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

358.4
MW (Da)
3.78
ALogP
5
HBA
2
HBD
87.0
PSA (Ų)
0.70
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22N4O
MW 358.45
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.44

Activity Summary

IC50 5 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL3988594
IC50 7.64 7.64 23.0 1
Unchecked
CHEMBL612545
IC50 7.55 7.55 28.0 1
Dihydrofolate reductase
CHEMBL2329
IC50 7.52 7.52 30.0 1
Dihydrofolate reductase
CHEMBL1681620
IC50 7.12 7.12 75.0 1
Dihydrofolate reductase
CHEMBL202
IC50 7.01 7.01 97.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24568657 10.1021/jm401916j Unchecked 1
24568657 10.1021/jm401916j Dihydrofolate reductase 1
24568657 10.1021/jm401916j Nakaseomyces glabratus 1
24568657 10.1021/jm401916j Candida albicans 1

Data from ChEMBL 36 via Core Engine