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Compound Detail

CHEMBL4760917

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Cc1cc(NC2CCc3cc(F)c(F)cc3C2)n2nc(C(C)(F)F)nc2n1

Basic Information

ChEMBL ID CHEMBL4760917
Phase Preclinical
Structure Type MOL
InChI Key RGHQYQGIGDHRAW-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

379.4
MW (Da)
3.79
ALogP
5
HBA
1
HBD
55.1
PSA (Ų)
0.70
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17F4N5
MW 379.36
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.55

Activity Summary

IC50 3 meas. best 7.22
EC50 1 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 7.66 7.66 22.0 1
Unchecked
CHEMBL612545
IC50 7.22 6.67 60.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27127993 10.1021/acs.jmedchem.6b00275 Unchecked 4
27127993 10.1021/acs.jmedchem.6b00275 ADMET 3
27127993 10.1021/acs.jmedchem.6b00275 Dihydroorotate dehydrogenase (quinone), mitochondrial 2
27127993 10.1021/acs.jmedchem.6b00275 Plasmodium falciparum 2
27127993 10.1021/acs.jmedchem.6b00275 No relevant target 2
27127993 10.1021/acs.jmedchem.6b00275 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine