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Compound Detail

CHEMBL492379

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C[C@@H](CN1CCC(n2c(=O)[nH]c3c(F)cccc32)CC1)NC(=O)c1ccc(F)c(F)c1

Basic Information

ChEMBL ID CHEMBL492379
Phase Preclinical
Structure Type MOL
InChI Key XJRPOXWRHJABGE-ZDUSSCGKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

432.4
MW (Da)
3.20
ALogP
4
HBA
2
HBD
70.1
PSA (Ų)
0.65
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23F3N4O2
MW 432.45
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.79

Activity Summary

IC50 2 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Phospholipase D1
CHEMBL2536
IC50 7.42 7.42 38.0 1
Phospholipase D2
CHEMBL2734
IC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Phospholipase D1 IC50 = 38.0 nM 7.42 Inhibition of human PLD1 in Calu1 cells 19268584
Phospholipase D2 IC50 = 14000.0 nM 4.85 Inhibition of GFP-labelled human PLD2 HEK293 cells 19268584

Literature References

PubMed DOI Target Context # Activities
19268584 10.1016/j.bmcl.2009.02.057 Phospholipase D1 1
19268584 10.1016/j.bmcl.2009.02.057 Unchecked 1
19268584 10.1016/j.bmcl.2009.02.057 Phospholipase D2 1

Data from ChEMBL 36 via Core Engine