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Compound Detail

CHEMBL5069458

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C=CC(=O)N[C@@H](C)C(=O)N1CCN(c2ccc(Nc3ncc(Cl)c(Nc4ccccc4C(=O)NC)n3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL5069458
Phase Preclinical
Structure Type MOL
InChI Key SQMGCXJZSMCVHC-SFHVURJKSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

563.1
MW (Da)
3.32
ALogP
8
HBA
4
HBD
131.6
PSA (Ų)
0.29
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31ClN8O3
MW 563.06
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -1.61

Activity Summary

IC50 3 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 6.75 6.75 180.0 1
MDA-MB-231
CHEMBL400
IC50 5.94 5.94 1160.0 1
HeLa
CHEMBL399
IC50 5.8 5.8 1590.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34757216 10.1016/j.bmcl.2021.128433 HeLa 1
34757216 10.1016/j.bmcl.2021.128433 HCT-116 1
34757216 10.1016/j.bmcl.2021.128433 MDA-MB-231 1
34757216 10.1016/j.bmcl.2021.128433 Focal adhesion kinase 1 1

Data from ChEMBL 36 via Core Engine