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Compound Detail

CHEMBL4067591

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COc1ccc(N2C[C@H]3[C@@H](CS[C@]4(C(=O)Nc5cccc(Br)c54)[C@@H]3c3ccc(Br)cc3)CC2=O)cc1

Basic Information

ChEMBL ID CHEMBL4067591
Phase Preclinical
Structure Type MOL
InChI Key CINQLVZJEDMXEK-VVAOOJQESA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

628.4
MW (Da)
6.57
ALogP
4
HBA
1
HBD
58.6
PSA (Ų)
0.36
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H24Br2N2O3S
MW 628.39
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.25

Activity Summary

IC50 3 meas. best 5.52
Kd 1 meas. best 5.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 5.52 5.52 3000.0 1
A549
CHEMBL392
IC50 5.37 5.37 4300.0 1
E3 ubiquitin-protein ligase Mdm2
CHEMBL5023
Kd 5.19 5.19 6400.0 1
HCT-116
CHEMBL394
IC50 5.08 5.08 8300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28797774 10.1016/j.bmc.2017.07.049 A549 1
28797774 10.1016/j.bmc.2017.07.049 MCF7 1
28797774 10.1016/j.bmc.2017.07.049 HCT-116 1
28797774 10.1016/j.bmc.2017.07.049 E3 ubiquitin-protein ligase Mdm2 1

Data from ChEMBL 36 via Core Engine