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Compound Detail

CHEMBL328384

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COc1cc2cc(C(=O)N3C[C@H]4C[C@@]45C3=CC(=O)c3[nH]c(C)c(/C=N/O)c35)[nH]c2c(OC)c1OC

Basic Information

ChEMBL ID CHEMBL328384
Phase Preclinical
Structure Type MOL
InChI Key UDJXXQFGLZWSJK-LSSWGCCBSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
3.13
ALogP
7
HBA
3
HBD
129.2
PSA (Ų)
0.29
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N4O6
MW 476.49
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness 0.17

Activity Summary

IC50 2 meas. best 10.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HeLa
CHEMBL399
IC50 10.09 9.99 0.1 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HeLa IC50 = 0.082 nM 10.09 In vitro inhibition HeLa S3 cell growth by 50% after 72 hr. 10425104
HeLa IC50 = 0.13 nM 9.89 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