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Compound Detail

CHEMBL3701197

A-226
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CCC(=N\O)/C(C)=C/c1ccc(F)c(C)c1

Basic Information

ChEMBL ID CHEMBL3701197
Name A-226
Phase Preclinical
Structure Type MOL
InChI Key WRHHATMLNUQQTB-MZRBSKCNSA-N

Known Names

A-1115226
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
20
Publications
1
Known Names

Molecular Properties

221.3
MW (Da)
3.78
ALogP
2
HBA
1
HBD
32.6
PSA (Ų)
0.47
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H16FNO
MW 221.27
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.42

Activity Summary

Ki 6 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 6.3 6.2867 501.2 3
Unchecked
CHEMBL612545
Ki 5.44 5.435 3630.8 2
Gamma-aminobutyric acid receptor subunit alpha-1
CHEMBL1962
Ki 5.43 5.43 3690.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507256 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507256 Epidermal growth factor receptor 12
- 10.6019/CHEMBL4507256 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4689842 U2OS 10
- 10.6019/CHEMBL4507256 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4507256 Unchecked 10
- 10.6019/CHEMBL4689842 Fibroblast 9
- 10.6019/CHEMBL4507256 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4689842 HEK-293T 9
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4507256 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507256 Hepatocyte growth factor receptor 3
- 10.6019/CHEMBL4507256 Sigma non-opioid intracellular receptor 1 3
- 10.6019/CHEMBL4507256 ALK tyrosine kinase receptor 3
- 10.6019/CHEMBL4507256 Ribosomal protein S6 kinase alpha-4 2
- 10.6019/CHEMBL4507256 Ribosomal protein S6 kinase alpha-1 2
- 10.6019/CHEMBL4507256 Ribosomal protein S6 kinase alpha-5 2

Data from ChEMBL 36 via Core Engine