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Compound Detail

CHEMBL4744272

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N#Cc1cc(C(=O)N2CC=CC2)cc(C(F)(F)F)c1O

Basic Information

ChEMBL ID CHEMBL4744272
Phase Preclinical
Structure Type MOL
InChI Key NKSZDQNCXVAZMK-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

282.2
MW (Da)
2.29
ALogP
3
HBA
1
HBD
64.3
PSA (Ų)
0.80
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H9F3N2O2
MW 282.22
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -1.16

Activity Summary

IC50 2 meas. best 4.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 2C9
CHEMBL3397
IC50 4.28 4.28 52000.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 9248.1 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 2C9 IC50 = 52000.0 nM 4.28 Inhibition of CYP2C9 (unknown origin) 33684442

Literature References

PubMed DOI Target Context # Activities
33684442 10.1016/j.bmcl.2021.127900 ADMET 4
33684442 10.1016/j.bmcl.2021.127900 Solute carrier family 22 member 12 1
33684442 10.1016/j.bmcl.2021.127900 Unchecked 1
33684442 10.1016/j.bmcl.2021.127900 Cytochrome P450 2C9 1
33684442 10.1016/j.bmcl.2021.127900 Sapajus apella 1

Data from ChEMBL 36 via Core Engine