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Compound Detail

CHEMBL545921

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CC1(C)N=C(N)N=C(N)N1OCCCOc1cc(Cl)c(Cl)cc1Cl.Cl

Basic Information

ChEMBL ID CHEMBL545921
Phase Preclinical
Structure Type MOL
InChI Key VOTSDCGUYAGUNS-UHFFFAOYSA-N
Parent Compound CHEMBL129788
Active Moiety CHEMBL129788
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

394.7
MW (Da)
3.03
ALogP
7
HBA
2
HBD
98.5
PSA (Ų)
0.57
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H19Cl4N5O2
MW 431.15
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -0.43

Activity Summary

IC50 1 meas. best 9.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional dihydrofolate reductase-thymidylate synthase
CHEMBL1939
IC50 9.24 9.24 0.6 1

Pharmacokinetic Data

Parameter Value Units Species
F 1.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bifunctional dihydrofolate reductase-thymidylate synthase IC50 = 0.57 nM 9.24 Inhibition of Plasmodium falciparum DHFR 29111368

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
20485427 10.1038/nature09107 HepG2 1
20485427 10.1038/nature09107 Unchecked 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
- 10.1039/C6MD00084C Rattus norvegicus 1
29111368 10.1016/j.bmc.2017.10.017 Bifunctional dihydrofolate reductase-thymidylate synthase 1

Data from ChEMBL 36 via Core Engine