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Compound Detail

CHEMBL4797299

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CCC(O)Cn1cc(CN2CCc3c(Br)c4c(c(OC)c3[C@@H]2[C@H]2OC(=O)c3c2ccc(OC)c3OC)OCO4)nn1

Basic Information

ChEMBL ID CHEMBL4797299
Phase Preclinical
Structure Type MOL
InChI Key LPUZGAZZKFRCQO-YVLFHOQNSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

631.5
MW (Da)
3.58
ALogP
12
HBA
1
HBD
126.6
PSA (Ų)
0.35
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31BrN4O8
MW 631.48
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness 0.30

Activity Summary

Kd 1 meas. best 6.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tubulin beta
CHEMBL3832942
Kd 6.88 6.88 132.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tubulin beta Kd = 132.0 nM 6.88 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