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Compound Detail

CHEMBL100710

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COc1ccc(/C=C/C(=O)N2C[C@H]3C[C@@]34C2=CC(=O)c2[nH]c(C)c(C)c24)cc1

Basic Information

ChEMBL ID CHEMBL100710
Phase Preclinical
Structure Type MOL
InChI Key KNBDJSXNOLEDNX-PLFRZCSDSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

374.4
MW (Da)
3.53
ALogP
3
HBA
1
HBD
62.4
PSA (Ų)
0.84
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N2O3
MW 374.44
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness 0.31

Activity Summary

IC50 2 meas. best 9.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HeLa
CHEMBL399
IC50 9.66 8.89 0.2 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HeLa IC50 = 0.22 nM 9.66 In vitro inhibition HeLa S3 cell growth by 50% after 72 hr. 10425104
HeLa IC50 = 7.5 nM 8.12 In vitro inhibition of HeLa S3 cell growth by 50% after 1 hr. 10425104

Literature References

PubMed DOI Target Context # Activities
10425104 10.1021/jm990094r Mus musculus 3
10425104 10.1021/jm990094r HeLa 2

Data from ChEMBL 36 via Core Engine