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Compound Detail

CHEMBL4759615

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Cc1c(-c2ccc(-c3ccccc3F)cc2)nc2ccc(F)cc2c1C(=O)NO

Basic Information

ChEMBL ID CHEMBL4759615
Phase Preclinical
Structure Type MOL
InChI Key GAYOEHUUOCPGQU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

390.4
MW (Da)
5.27
ALogP
3
HBA
2
HBD
62.2
PSA (Ų)
0.37
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H16F2N2O2
MW 390.39
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.03

Activity Summary

IC50 2 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dihydroorotate dehydrogenase (quinone), mitochondrial
CHEMBL1966
IC50 8.85 8.85 1.4 1
MOLM-13
CHEMBL3706572
IC50 7.64 7.64 23.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 3.0 hr Homo sapiens
T1/2 0.6 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33007394 10.1016/j.bmcl.2020.127589 ADMET 2
33007394 10.1016/j.bmcl.2020.127589 Dihydroorotate dehydrogenase (quinone), mitochondrial 1
33007394 10.1016/j.bmcl.2020.127589 MOLM-13 1

Data from ChEMBL 36 via Core Engine