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Compound Detail

CHEMBL3818016

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COCCn1c(=O)c(-c2ccc(-n3cccc(C)c3=O)cc2Cl)cc2cnc(NC3COC3)nc21

Basic Information

ChEMBL ID CHEMBL3818016
Phase Preclinical
Structure Type MOL
InChI Key MXFNRZNGPALJHJ-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

493.9
MW (Da)
3.03
ALogP
9
HBA
1
HBD
100.3
PSA (Ų)
0.42
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24ClN5O4
MW 493.95
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.46

Activity Summary

IC50 1 meas. best 6.54
Ki 1 meas. best 8.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase PAK 1
CHEMBL4600
Ki 8.23 8.23 5.9 1
Serine/threonine-protein kinase PAK 1/PAK 2
CHEMBL3885636
IC50 6.54 6.54 290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27167326 10.1021/acs.jmedchem.6b00638 No relevant target 2
27167326 10.1021/acs.jmedchem.6b00638 MDCK 2
27167326 10.1021/acs.jmedchem.6b00638 Serine/threonine-protein kinase PAK 1 1
27167326 10.1021/acs.jmedchem.6b00638 Unchecked 1
27167326 10.1021/acs.jmedchem.6b00638 Serine/threonine-protein kinase PAK 1/PAK 2 1

Data from ChEMBL 36 via Core Engine