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Compound Detail

CHEMBL5085443

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

Basic Information

ChEMBL ID CHEMBL5085443
Phase Preclinical
Structure Type MOL
InChI Key LSDHELURKNKBDP-IBGZPJMESA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

577.1
MW (Da)
3.66
ALogP
8
HBA
3
HBD
122.8
PSA (Ų)
0.33
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 C29H33ClN8O3
MW 577.09
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -1.45

Activity Summary

IC50 3 meas. best 5.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 5.97 5.97 1060.0 1
HeLa
CHEMBL399
IC50 5.63 5.63 2330.0 1
MDA-MB-231
CHEMBL400
IC50 5.38 5.38 4150.0 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