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Compound Detail

CHEMBL276541

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COc1cccc(-c2cc(O)c3cccnc3n2)c1

Basic Information

ChEMBL ID CHEMBL276541
Phase Preclinical
Structure Type MOL
InChI Key DVIFGVPPUSCDGE-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

252.3
MW (Da)
3.01
ALogP
4
HBA
1
HBD
55.2
PSA (Ų)
0.76
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 C15H12N2O2
MW 252.27
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -0.59

Activity Summary

IC50 3 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tubulin
CHEMBL2094134
IC50 6.1 6.1 790.0 1
Tubulin beta chain
CHEMBL3394
IC50 6.02 6.02 960.0 1
Tubulin alpha chain
CHEMBL3658
IC50 6.02 6.02 955.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9544215 10.1021/jm9707479 Tubulin 2
10649972 10.1021/jm990333a Tubulin alpha chain 1
9216846 10.1021/jm960858s Tubulin beta chain 1
9216846 10.1021/jm960858s Tubulin alpha chain 1
9216846 10.1021/jm960858s Tumor Cell line 1
9216846 10.1021/jm960858s HL-60 1
9216846 10.1021/jm960858s NCI-H460 1
9216846 10.1021/jm960858s HCT-116 1
9216846 10.1021/jm960858s SF-295 1
9216846 10.1021/jm960858s U-251 1
9216846 10.1021/jm960858s SK-MEL-5 1
9216846 10.1021/jm960858s OVCAR-3 1
9216846 10.1021/jm960858s 786-0 1
9216846 10.1021/jm960858s PC-3 1
9216846 10.1021/jm960858s MDA-MB-435 1
9216846 10.1021/jm960858s MDA-N 1

Data from ChEMBL 36 via Core Engine