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Compound Detail

CHEMBL380478

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COc1cc2c(Nc3ncc(CC(=O)Nc4cccc(F)c4)s3)ncnc2cc1OCCCN1CCC[C@H]1CO

Basic Information

ChEMBL ID CHEMBL380478
Phase Preclinical
Structure Type MOL
InChI Key GOKZEHPYAIHCMO-FQEVSTJZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

566.7
MW (Da)
4.38
ALogP
10
HBA
3
HBD
121.7
PSA (Ų)
0.21
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31FN6O4S
MW 566.66
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.58

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
SW-620
CHEMBL612262
IC50 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
SW-620 IC50 = 4.0 nM 8.4 Inhibition of phosphorylation of histone H3 in human SW620 cells 16451062

Literature References

PubMed DOI Target Context # Activities
16451062 10.1021/jm050786h Aurora kinase A 1
16451062 10.1021/jm050786h Unchecked 1
16451062 10.1021/jm050786h SW-620 1

Data from ChEMBL 36 via Core Engine