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Compound Detail

CHEMBL16065

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COc1cccc([C@@H]2CC(=O)c3ccccc3N2)c1

Basic Information

ChEMBL ID CHEMBL16065
Phase Preclinical
Structure Type MOL
InChI Key LFMVMPCOOSRSFY-HNNXBMFYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

253.3
MW (Da)
3.43
ALogP
3
HBA
1
HBD
38.3
PSA (Ų)
0.89
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15NO2
MW 253.30
Aromatic Rings 2
Heavy Atoms 19
NP-Likeness 0.14

Activity Summary

IC50 1 meas. best 5.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tubulin
CHEMBL2094134
IC50 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tubulin IC50 = 1200.0 nM 5.92 Inhibition of bovine brain tubulin polymerization (ITP). 9544215

Literature References

PubMed DOI Target Context # Activities
9544215 10.1021/jm9707479 KB 1
9544215 10.1021/jm9707479 A549 1
9544215 10.1021/jm9707479 HCT-8 1
9544215 10.1021/jm9707479 CAKI-1 1
9544215 10.1021/jm9707479 MCF7 1
9544215 10.1021/jm9707479 Tubulin 1

Data from ChEMBL 36 via Core Engine