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Compound Detail

CHEMBL533684

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Nc1nc(N)c2cc(CNc3ccc(Cl)c(Cl)c3)ccc2n1

Basic Information

ChEMBL ID CHEMBL533684
Phase Preclinical
Structure Type MOL
InChI Key LFMKPWQUJBLWEK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

334.2
MW (Da)
3.71
ALogP
5
HBA
3
HBD
89.8
PSA (Ų)
0.68
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 C15H13Cl2N5
MW 334.21
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -1.42

Activity Summary

IC50 1 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL4614
IC50 7.6 7.6 25.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bifunctional dihydrofolate reductase-thymidylate synthase IC50 = 25.0 nM 7.6 Inhibition of Leishmania major DHFR 33187806

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
110930 10.1021/jm00191a005 Dihydrofolate reductase 2
20485427 10.1038/nature09107 HepG2 1
20485427 10.1038/nature09107 Unchecked 1
319234 10.1021/jm00211a020 Plasmodium berghei 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
33187806 10.1016/j.ejmech.2020.112986 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine