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Compound Detail

CHEMBL514038

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Cc1cc(Nc2cccc(F)c2)n2ncnc2n1

Basic Information

ChEMBL ID CHEMBL514038
Phase Preclinical
Structure Type MOL
InChI Key GTSBAPJTXCZABL-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

243.2
MW (Da)
2.32
ALogP
5
HBA
1
HBD
55.1
PSA (Ų)
0.75
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H10FN5
MW 243.25
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -2.88

Activity Summary

EC50 1 meas. best 4.47
IC50 1 meas. best 5.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydroorotate dehydrogenase
CHEMBL3486
IC50 5.04 5.04 9200.0 1
Plasmodium falciparum
CHEMBL364
EC50 4.47 4.47 34000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 18.0 mL.min-1.g-1 Homo sapiens
T1/2 1.617 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19296651 10.1021/jm801343r Liver microsomes 2
19296651 10.1021/jm801343r Plasmodium berghei 1
19296651 10.1021/jm801343r Dihydroorotate dehydrogenase (quinone), mitochondrial 1
19296651 10.1021/jm801343r Plasmodium falciparum 1
19296651 10.1021/jm801343r Dihydroorotate dehydrogenase 1

Data from ChEMBL 36 via Core Engine