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Compound Detail

CHEMBL1222575

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COc1ccc([C@H]2CC(=O)O[C@@H](C)C[C@@H](C)/C=C(\C)C[C@H](C)C(=O)N[C@@H](C)C(=O)N(C)[C@H](Cc3c(Br)[nH]c4ccccc34)C(=O)N2)cc1

Basic Information

ChEMBL ID CHEMBL1222575
Phase Preclinical
Structure Type MOL
InChI Key SNJRDJWQWQDJGC-KVSNERESSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

723.7
MW (Da)
6.00
ALogP
6
HBA
3
HBD
129.8
PSA (Ų)
0.22
QED
2
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H47BrN4O6
MW 723.71
Aromatic Rings 3
Heavy Atoms 48
NP-Likeness 1.58

Activity Summary

IC50 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CA46
CHEMBL612566
IC50 7.7 7.7 20.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CA46 IC50 = 20.0 nM 7.7 Growth inhibition of human CA46 cells assessed as induction of actin assembly af... 20678932

Literature References

PubMed DOI Target Context # Activities
20678932 10.1016/j.bmcl.2010.07.023 CA46 1

Data from ChEMBL 36 via Core Engine