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Compound Detail

CHEMBL312688

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Nc1nc(N)c2nc(-c3ccc(Cl)c(Cl)c3)[nH]c2n1

Basic Information

ChEMBL ID CHEMBL312688
Phase Preclinical
Structure Type MOL
InChI Key GZDRYQKQDXYCQK-UHFFFAOYSA-N
3
Targets
8
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

295.1
MW (Da)
2.49
ALogP
5
HBA
3
HBD
106.5
PSA (Ų)
0.64
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H8Cl2N6
MW 295.13
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -1.10

Activity Summary

IC50 8 meas. best 5.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 5.17 5.17 6700.0 3
Dihydrofolate reductase
CHEMBL1926
IC50 4.71 4.71 19500.0 1
Dihydrofolate reductase
CHEMBL2364669
IC50 4.7 4.7 20000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9301665 10.1021/jm970271t Dihydrofolate reductase 2
11754594 10.1021/jm010407u Dihydrofolate reductase 2
20117005 10.1016/j.bmc.2009.12.066 Bifunctional dihydrofolate reductase-thymidylate synthase 2
20117005 10.1016/j.bmc.2009.12.066 Dihydrofolate reductase 2
9301665 10.1021/jm970271t Bifunctional dihydrofolate reductase-thymidylate synthase 1
9301665 10.1021/jm970271t Dihydrofolate reductase; P. carinii vs rat 1
9301665 10.1021/jm970271t Dihydrofolate reductase; T. gondii vs rat 1

Data from ChEMBL 36 via Core Engine