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Compound Detail

CHEMBL120366

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COc1c(I)cc(Cc2cnc(N)nc2N)cc1I

Basic Information

ChEMBL ID CHEMBL120366
Phase Preclinical
Structure Type MOL
InChI Key HOVOAFDUGCCWRG-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

482.1
MW (Da)
2.45
ALogP
5
HBA
2
HBD
87.0
PSA (Ų)
0.66
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 C12H12I2N4O
MW 482.06
Aromatic Rings 2
Heavy Atoms 19

Activity Summary

IC50 4 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydrofolate reductase
CHEMBL1809
IC50 8.0 8.0 10.0 1
Dihydrofolate reductase
CHEMBL3565
IC50 7.55 7.55 28.0 1
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL3963
IC50 7.51 7.51 31.0 1
Dihydrofolate reductase
CHEMBL2363
IC50 4.8 4.8 16000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
3100802 10.1021/jm00385a017 Dihydrofolate reductase 3
3100802 10.1021/jm00385a017 Bifunctional dihydrofolate reductase-thymidylate synthase 1
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1

Data from ChEMBL 36 via Core Engine