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Compound Detail

CHEMBL204467

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OCc1ccc(C#Cc2cncnc2Nc2ccc(OCc3cccc(F)c3)c(Cl)c2)o1

Basic Information

ChEMBL ID CHEMBL204467
Phase Preclinical
Structure Type MOL
InChI Key KOKYNLBDBNLOPA-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

449.9
MW (Da)
5.08
ALogP
6
HBA
2
HBD
80.4
PSA (Ų)
0.40
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17ClFN3O3
MW 449.87
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.20

Activity Summary

IC50 5 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 7.48 7.48 33.0 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 7.33 7.33 47.0 1
HN5
CHEMBL614828
IC50 6.03 6.03 930.0 1
BT-474
CHEMBL614529
IC50 5.69 5.69 2040.0 1
HFF
CHEMBL614071
IC50 4.8 4.8 15800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16483772 10.1016/j.bmcl.2006.01.111 Epidermal growth factor receptor 1
16483772 10.1016/j.bmcl.2006.01.111 Receptor tyrosine-protein kinase erbB-2 1
16483772 10.1016/j.bmcl.2006.01.111 HN5 1
16483772 10.1016/j.bmcl.2006.01.111 BT-474 1
16483772 10.1016/j.bmcl.2006.01.111 HFF 1

Data from ChEMBL 36 via Core Engine