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Compound Detail

CHEMBL102048

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

Basic Information

ChEMBL ID CHEMBL102048
Phase Preclinical
Structure Type MOL
InChI Key CRXTYILZRAAGBT-XHIYKSJMSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
3.29
ALogP
4
HBA
1
HBD
65.6
PSA (Ų)
0.76
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 C25H27N3O3
MW 417.51
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness 0.12

Activity Summary

IC50 2 meas. best 9.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HeLa
CHEMBL399
IC50 9.41 8.925 0.4 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HeLa IC50 = 0.39 nM 9.41 In vitro inhibition HeLa S3 cell growth by 50% after 72 hr. 10425104
HeLa IC50 = 3.6 nM 8.44 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