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Compound Detail

CHEMBL1085637

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CC(C)C(=O)c1cn(CC(=O)COc2ccc(Oc3ccccc3)cc2)c2ccc(C(=O)O)cc12

Basic Information

ChEMBL ID CHEMBL1085637
Phase Preclinical
Structure Type MOL
InChI Key HTOJZPHWNDZOPQ-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

471.5
MW (Da)
5.62
ALogP
6
HBA
1
HBD
94.8
PSA (Ų)
0.30
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25NO6
MW 471.51
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.52

Activity Summary

IC50 4 meas. best 7.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytosolic phospholipase A2
CHEMBL3816
IC50 7.92 7.92 12.0 1
Unchecked
CHEMBL612545
IC50 7.92 7.8867 12.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20583844 10.1021/jm1001088 Mus musculus 7
20583844 10.1021/jm1001088 ADMET 4
20583844 10.1021/jm1001088 Plasma 4
27810597 10.1016/j.ejmech.2016.10.039 NADPH--cytochrome P450 reductase 3
21067218 10.1021/jm101094p Intestine 2
36495814 10.1016/j.bmc.2022.117110 ADMET 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
27810597 10.1016/j.ejmech.2016.10.039 Unchecked 2
20583844 10.1021/jm1001088 Unchecked 2
21067218 10.1021/jm101094p Plasma 2
20583844 10.1021/jm1001088 No relevant target 2
20583844 10.1021/jm1001088 Phospholipase A2, major isoenzyme 1
20583844 10.1021/jm1001088 85/88 kDa calcium-independent phospholipase A2 1
27810597 10.1016/j.ejmech.2016.10.039 Cytosolic phospholipase A2 1
27810597 10.1016/j.ejmech.2016.10.039 No relevant target 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
20583844 10.1021/jm1001088 Liver microsomes 1
36495814 10.1016/j.bmc.2022.117110 Unchecked 1

Data from ChEMBL 36 via Core Engine