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Compound Detail

CHEMBL578424

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COc1cc(-c2ccc(C(C)(C)C)cc2)cc(C(C)C#Cc2c(C)nc(N)nc2N)c1

Basic Information

ChEMBL ID CHEMBL578424
Phase Preclinical
Structure Type MOL
InChI Key AOJOORYEHDDWCH-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

414.6
MW (Da)
5.08
ALogP
5
HBA
2
HBD
87.0
PSA (Ų)
0.58
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30N4O
MW 414.55
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.61

Activity Summary

IC50 3 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL2329
IC50 7.47 7.47 34.0 1
Dihydrofolate reductase
CHEMBL202
IC50 6.68 6.68 210.0 1
ADMET
CHEMBL612558
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19560363 10.1016/j.bmc.2009.06.021 Dihydrofolate reductase 2
19560363 10.1016/j.bmc.2009.06.021 Unchecked 1
19560363 10.1016/j.bmc.2009.06.021 ADMET 1
19560363 10.1016/j.bmc.2009.06.021 Candida albicans 1

Data from ChEMBL 36 via Core Engine