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Compound Detail

CHEMBL473437

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CN(C)Cc1ccc(-c2cc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3s2)[nH]1

Basic Information

ChEMBL ID CHEMBL473437
Phase Preclinical
Structure Type MOL
InChI Key ATEQNOXHLBHSBB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

508.0
MW (Da)
6.86
ALogP
6
HBA
2
HBD
66.1
PSA (Ų)
0.24
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23ClFN5OS
MW 508.02
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.72

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 8.4 8.4 4.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 7.12 7.12 76.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 4.0 nM 8.4 Inhibition of EGFR 19111461
Receptor tyrosine-protein kinase erbB-2 IC50 = 76.0 nM 7.12 Inhibition of ErbB2 19111461

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
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
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1

Data from ChEMBL 36 via Core Engine