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Compound Detail

CHEMBL3298512

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C=CC(=O)[C@H](Cc1ccccc1)NC(=O)OC(C)(C)C

Basic Information

ChEMBL ID CHEMBL3298512
Phase Preclinical
Structure Type MOL
InChI Key YAABAAPIHZWIND-ZDUSSCGKSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

275.4
MW (Da)
2.88
ALogP
3
HBA
1
HBD
55.4
PSA (Ų)
0.84
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 C16H21NO3
MW 275.35
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.28

Activity Summary

IC50 4 meas. best 6.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.24 6.24 580.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 4.67 4.67 21500.0 1
NCI-H460
CHEMBL396
IC50 4.64 4.64 22900.0 1
Unchecked
CHEMBL612545
IC50 4.28 4.28 52600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900862 10.1021/ml500088x Unchecked 5
24900862 10.1021/ml500088x RAC-alpha serine/threonine-protein kinase 3
24900862 10.1021/ml500088x Tyrosine-protein kinase Yes 1
24900862 10.1021/ml500088x Vascular endothelial growth factor receptor 2 1
24900862 10.1021/ml500088x Vascular endothelial growth factor receptor 1 1
24900862 10.1021/ml500088x Receptor tyrosine-protein kinase erbB-4 1
24900862 10.1021/ml500088x Epidermal growth factor receptor 1
24900862 10.1021/ml500088x Tyrosine-protein kinase CSK 1
24900862 10.1021/ml500088x Serine/threonine-protein kinase Chk1 1
24900862 10.1021/ml500088x CDK2/Cyclin A2 1
24900862 10.1021/ml500088x Cyclin-dependent kinase 1/cyclin B1 1
24900862 10.1021/ml500088x Calcium/calmodulin-dependent protein kinase type 1D 1
24900862 10.1021/ml500088x Aurora kinase A 1
24900862 10.1021/ml500088x AMP-activated protein kinase, AMPK 1
24900862 10.1021/ml500088x Tyrosine-protein kinase ABL1 1
24900862 10.1021/ml500088x NCI-H460 1
24900862 10.1021/ml500088x NON-PROTEIN TARGET 1
24900862 10.1021/ml500088x Maternal embryonic leucine zipper kinase 1
24900862 10.1021/ml500088x Serine/threonine-protein kinase Chk2 1
24900862 10.1021/ml500088x Calcium/calmodulin-dependent protein kinase type IV 1

Data from ChEMBL 36 via Core Engine