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Compound Detail

CHEMBL101908

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Nc1nc(N)c2nc(CSc3ccc4ccccc4c3)[nH]c2n1

Basic Information

ChEMBL ID CHEMBL101908
Phase Preclinical
Structure Type MOL
InChI Key YFFHNJSASTWAQX-UHFFFAOYSA-N
1
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

322.4
MW (Da)
2.96
ALogP
6
HBA
3
HBD
106.5
PSA (Ų)
0.50
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H14N6S
MW 322.40
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -1.18

Activity Summary

IC50 5 meas. best 4.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL2425
IC50 4.35 4.35 45000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9301665 10.1021/jm970271t 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
20117005 10.1016/j.bmc.2009.12.066 Bifunctional dihydrofolate reductase-thymidylate synthase 1
20117005 10.1016/j.bmc.2009.12.066 Dihydrofolate reductase 1

Data from ChEMBL 36 via Core Engine