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Compound Detail

CHEMBL23713

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COc1ccc(C)c(NCc2cnc3nc(N)nc(N)c3c2C)c1

Basic Information

ChEMBL ID CHEMBL23713
Phase Preclinical
Structure Type MOL
InChI Key JGJKINSQWJXDJD-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

324.4
MW (Da)
2.43
ALogP
7
HBA
3
HBD
112.0
PSA (Ų)
0.68
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H20N6O
MW 324.39
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.98

Activity Summary

IC50 6 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL5457
IC50 9.4 9.4 0.4 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 7.64 7.64 23.0 1
Toxoplasma gondii
CHEMBL612888
IC50 7.52 7.52 30.0 1
Dihydrofolate reductase
CHEMBL1926
IC50 7.42 7.42 38.0 1
Dihydrofolate reductase
CHEMBL202
IC50 6.82 6.82 150.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 6.82 6.82 150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11754578 10.1021/jm010360c Dihydrofolate reductase 4
8632434 10.1021/jm950760y Dihydrofolate reductase 2
8632434 10.1021/jm950760y Bifunctional dihydrofolate reductase-thymidylate synthase 1
8632434 10.1021/jm950760y Toxoplasma gondii 1
8632434 10.1021/jm950760y Dihydrofolate reductase; P. carinii vs rat 1
8632434 10.1021/jm950760y Dihydrofolate reductase; T. gondii vs rat 1

Data from ChEMBL 36 via Core Engine