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Compound Detail

CHEMBL481331

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CS(=O)(=O)CCNCc1ccc(-c2cc3c(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)ncnc3s2)[nH]1

Basic Information

ChEMBL ID CHEMBL481331
Phase Preclinical
Structure Type MOL
InChI Key YCHMPCBHRODLET-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

586.1
MW (Da)
5.94
ALogP
8
HBA
3
HBD
109.0
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 C27H25ClFN5O3S2
MW 586.11
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -1.82

Activity Summary

IC50 2 meas. best 6.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 6.86 6.86 138.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 6.82 6.82 153.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 138.0 nM 6.86 Inhibition of EGFR 19111461
Receptor tyrosine-protein kinase erbB-2 IC50 = 153.0 nM 6.82 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