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Compound Detail

CHEMBL1795874

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C#Cc1cccc(NC2CC(Nc3cccc(-c4cn([C@H](CNCc5cccc(Br)c5)Cc5ccccc5)nn4)c3)C(O)CC2O)c1

Basic Information

ChEMBL ID CHEMBL1795874
Phase Preclinical
Structure Type MOL
InChI Key MTQZRUPTXKMEGE-NOECDHMVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

691.7
MW (Da)
6.04
ALogP
8
HBA
5
HBD
107.3
PSA (Ų)
0.10
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H39BrN6O2
MW 691.67
Aromatic Rings 5
Heavy Atoms 47
NP-Likeness -0.81

Activity Summary

IC50 1 meas. best 5.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-secretase 1
CHEMBL4822
IC50 5.62 5.62 2400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-secretase 1 IC50 = 2400.0 nM 5.62 Inhibition of BACE1 by cell-free FRET assay 21621412

Literature References

PubMed DOI Target Context # Activities
21621412 10.1016/j.bmcl.2011.05.007 Beta-secretase 1 2

Data from ChEMBL 36 via Core Engine