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Compound Detail

CHEMBL4869482

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Cl.Cn1ncc(Cl)c1-c1cc(F)c(C(=O)N[C@@H]2CNCC[C@H]2c2ccc(F)c(F)c2)cc1F

Basic Information

ChEMBL ID CHEMBL4869482
Phase Preclinical
Structure Type MOL
InChI Key YCKARSAOYZBMKD-XVHUJMMASA-N
Parent Compound CHEMBL5028586
Active Moiety CHEMBL5028586
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

466.9
MW (Da)
4.17
ALogP
4
HBA
2
HBD
59.0
PSA (Ų)
0.57
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20Cl2F4N4O
MW 503.33
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.24

Activity Summary

IC50 1 meas. best 7.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 7.31 7.31 48.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34375113 10.1021/acs.jmedchem.1c00815 RAC-alpha serine/threonine-protein kinase 1
34375113 10.1021/acs.jmedchem.1c00815 HGC-27 1
34375113 10.1021/acs.jmedchem.1c00815 786-0 1
34375113 10.1021/acs.jmedchem.1c00815 KHOS/NP 1

Data from ChEMBL 36 via Core Engine