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Compound Detail

CHEMBL4588910

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CCc1nc(N)nc(N)c1C#C[C@@H](C)c1cc(-c2ccncc2)ccc1OC

Basic Information

ChEMBL ID CHEMBL4588910
Phase Preclinical
Structure Type MOL
InChI Key PPKWGSTVAQFAGZ-CQSZACIVSA-N
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

373.5
MW (Da)
3.43
ALogP
6
HBA
2
HBD
99.9
PSA (Ų)
0.68
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N5O
MW 373.46
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.53

Activity Summary

Ki 6 meas. best 8.79
IC50 1 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1681620
Ki 8.79 7.2783 1.6 6
Dihydrofolate reductase
CHEMBL202
IC50 6.84 6.84 144.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27308944 10.1021/acs.jmedchem.6b00688 Staphylococcus aureus 12
27308944 10.1021/acs.jmedchem.6b00688 Dihydrofolate reductase 6
27308944 10.1021/acs.jmedchem.6b00688 Unchecked 1

Data from ChEMBL 36 via Core Engine