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Compound Detail

CHEMBL4852444

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CC#C[C@@]1(c2cc(NC(=O)c3ccc(C#N)cn3)ccc2F)CCOC(N)=N1

Basic Information

ChEMBL ID CHEMBL4852444
Phase Preclinical
Structure Type MOL
InChI Key DWCWSXLKLMTBSD-FQEVSTJZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

377.4
MW (Da)
2.30
ALogP
6
HBA
2
HBD
113.4
PSA (Ų)
0.80
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16FN5O2
MW 377.38
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.33

Activity Summary

IC50 2 meas. best 7.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-secretase 1
CHEMBL4822
IC50 7.15 7.15 71.0 1
Beta-secretase 2
CHEMBL2525
IC50 5.75 5.75 1778.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33719429 10.1021/acs.jmedchem.0c01858 Beta-secretase 1 1
33719429 10.1021/acs.jmedchem.0c01858 Beta-secretase 2 1
33719429 10.1021/acs.jmedchem.0c01858 Unchecked 1
33719429 10.1021/acs.jmedchem.0c01858 Voltage-gated inwardly rectifying potassium channel KCNH2 1
33719429 10.1021/acs.jmedchem.0c01858 ATP-dependent translocase ABCB1 1
33719429 10.1021/acs.jmedchem.0c01858 No relevant target 1

Data from ChEMBL 36 via Core Engine