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Compound Detail

CHEMBL57462

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N#CC(C#N)=C1C(=O)Nc2cc(O)c(O)cc21

Basic Information

ChEMBL ID CHEMBL57462
Phase Preclinical
Structure Type MOL
InChI Key VDKNKEFDJLIAPS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

227.2
MW (Da)
0.85
ALogP
5
HBA
3
HBD
117.1
PSA (Ų)
0.26
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H5N3O3
MW 227.18
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness 0.44

Activity Summary

IC50 2 meas. best 5.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 5.6 5.56 2500.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 2500.0 nM 5.6 Inhibition of polyGAT phosphorylation 1676428
Epidermal growth factor receptor IC50 = 3000.0 nM 5.52 Inhibition of EGFR 1479375

Literature References

PubMed DOI Target Context # Activities
1676428 10.1021/jm00110a022 Epidermal growth factor receptor 2
1479375 10.1021/np50089a001 Epidermal growth factor receptor 1

Data from ChEMBL 36 via Core Engine