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Compound Detail

CHEMBL4747307

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COc1ccc2c(c1OC)C(=O)O[C@@H]2[C@H]1c2c(c(Br)c3c(c2OC)OCO3)CCN1Cc1cn(-c2ccc(Cl)c(Cl)c2)nn1

Basic Information

ChEMBL ID CHEMBL4747307
Phase Preclinical
Structure Type MOL
InChI Key BOAJGQIITIVEMZ-RPBOFIJWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

704.4
MW (Da)
6.10
ALogP
11
HBA
0
HBD
106.4
PSA (Ų)
0.21
QED
3
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H25BrCl2N4O7
MW 704.36
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -0.19

Activity Summary

Kd 1 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tubulin beta
CHEMBL3832942
Kd 6.43 6.43 374.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tubulin beta Kd = 374.3 nM 6.43 Binding affinity to CM5 chip immobilized beta tubulin (unknown origin) assessed ... 32784088

Literature References

PubMed DOI Target Context # Activities
32784088 10.1016/j.bmcl.2020.127489 Tubulin beta 1
32784088 10.1016/j.bmcl.2020.127489 MCF7 1

Data from ChEMBL 36 via Core Engine