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Compound Detail

CHEMBL481324

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CS(=O)(=O)CCNCc1ccc(-c2cc3c(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)ncnc3s2)s1

Basic Information

ChEMBL ID CHEMBL481324
Phase Preclinical
Structure Type MOL
InChI Key VKGQZQGDXLIZTP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

603.2
MW (Da)
6.67
ALogP
9
HBA
2
HBD
93.2
PSA (Ų)
0.16
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24ClFN4O3S3
MW 603.17
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -1.87

Activity Summary

IC50 2 meas. best 7.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 7.02 7.02 95.0 1
Epidermal growth factor receptor
CHEMBL203
IC50 7.02 7.02 96.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 96.0 nM 7.02 Inhibition of EGFR 19111461
Receptor tyrosine-protein kinase erbB-2 IC50 = 95.0 nM 7.02 Inhibition of ErbB2 19111461

Literature References

PubMed DOI Target Context # Activities
19111461 10.1016/j.bmcl.2008.12.011 Epidermal growth factor receptor 1
19111461 10.1016/j.bmcl.2008.12.011 Receptor tyrosine-protein kinase erbB-2 1

Data from ChEMBL 36 via Core Engine