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Compound Detail

CHEMBL582843

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COc1cc(C(C#Cc2c(C)nc(N)nc2N)C(C)C)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL582843
Phase Preclinical
Structure Type MOL
InChI Key OHPJUBBWTNCBPF-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

370.4
MW (Da)
2.77
ALogP
7
HBA
2
HBD
105.5
PSA (Ų)
0.78
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 C20H26N4O3
MW 370.45
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.20

Activity Summary

IC50 3 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL2329
IC50 7.48 7.48 33.0 1
Dihydrofolate reductase
CHEMBL202
IC50 6.54 6.54 290.0 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 Candida albicans 1
19560363 10.1016/j.bmc.2009.06.021 ADMET 1

Data from ChEMBL 36 via Core Engine