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Compound Detail

CHEMBL295117

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COc1cccc(-c2cc(=O)c3ccc(C)nc3[nH]2)c1

Basic Information

ChEMBL ID CHEMBL295117
Phase Preclinical
Structure Type MOL
InChI Key UEXKSRLFFBWLCG-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

266.3
MW (Da)
2.91
ALogP
3
HBA
1
HBD
55.0
PSA (Ų)
0.78
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 C16H14N2O2
MW 266.30
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.35

Activity Summary

IC50 3 meas. best 6.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tubulin beta chain
CHEMBL3394
IC50 6.12 6.12 750.0 1
Tubulin alpha chain
CHEMBL3658
IC50 6.12 6.12 758.6 1
OVCAR-3
CHEMBL614213
IC50 6.12 6.12 750.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14987069 10.1021/np030373o NON-PROTEIN TARGET 2
9216846 10.1021/jm960858s SK-MEL-5 1
20187635 10.1021/np900821e Unchecked 1
20187635 10.1021/np900821e OVCAR-3 1
9216846 10.1021/jm960858s MDA-N 1
9216846 10.1021/jm960858s MDA-MB-435 1
9216846 10.1021/jm960858s PC-3 1
9216846 10.1021/jm960858s 786-0 1
9216846 10.1021/jm960858s OVCAR-3 1
10649972 10.1021/jm990333a Tubulin alpha chain 1
9216846 10.1021/jm960858s U-251 1
9216846 10.1021/jm960858s SF-295 1
9216846 10.1021/jm960858s HCT-116 1
9216846 10.1021/jm960858s NCI-H460 1
9216846 10.1021/jm960858s HL-60 1
9216846 10.1021/jm960858s Tumor Cell line 1
9216846 10.1021/jm960858s Tubulin alpha chain 1
9216846 10.1021/jm960858s Tubulin beta chain 1

Data from ChEMBL 36 via Core Engine