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Compound Detail

CHEMBL473429

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N#CCNCc1ccc(-c2cc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3s2)o1

Basic Information

ChEMBL ID CHEMBL473429
Phase Preclinical
Structure Type MOL
InChI Key NXSMOWZBERTEAU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

520.0
MW (Da)
6.68
ALogP
8
HBA
2
HBD
96.0
PSA (Ų)
0.17
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H19ClFN5O2S
MW 519.99
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.82

Activity Summary

IC50 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 8.52 8.52 3.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 7.17 7.17 68.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 3.0 nM 8.52 Inhibition of EGFR 19111461
Receptor tyrosine-protein kinase erbB-2 IC50 = 68.0 nM 7.17 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