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Compound Detail

CHEMBL533269

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Cc1cc(C(=O)OCC(=O)Nc2c(C)n(C)n(-c3ccccc3)c2=O)c(C)n1-c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL533269
Phase Preclinical
Structure Type MOL
InChI Key OFHDGHFNTKVFPI-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
2
PK Parameters
11
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
3.83
ALogP
7
HBA
1
HBD
87.3
PSA (Ų)
0.43
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 C26H25FN4O4
MW 476.51
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.96

Activity Summary

IC50 4 meas. best 6.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum K1
CHEMBL612856
IC50 6.82 6.82 152.0 1
Plasmodium falciparum
CHEMBL364
IC50 6.61 6.535 245.0 2

Pharmacokinetic Data

Parameter Value Units Species
CLint 60.0 uL min-1 mg-1 Homo sapiens
T1/2 0.4833 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL2113921 ADMET 5
20485427 10.1038/nature09107 Plasmodium falciparum 4
- 10.6019/CHEMBL2113921 Plasmodium falciparum 3
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1
- 10.6019/CHEMBL2113921 HEK293 1
- 10.6019/CHEMBL2113921 Plasmodium berghei 1
- 10.6019/CHEMBL2113921 Plasmodium falciparum K1 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