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Compound Detail

CHEMBL1915566

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COc1ccc(Br)cc1-c1csc(Nc2ccc(-n3cnc(C)c3)c(OC)c2)n1

Basic Information

ChEMBL ID CHEMBL1915566
Phase Preclinical
Structure Type MOL
InChI Key IILXHJHOJNRNFS-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

471.4
MW (Da)
5.83
ALogP
7
HBA
1
HBD
61.2
PSA (Ų)
0.38
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 C21H19BrN4O2S
MW 471.38
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.65

Activity Summary

IC50 2 meas. best 6.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-secretase
CHEMBL2094135
IC50 6.05 6.05 898.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21924610 10.1016/j.bmcl.2011.08.060 Cytochrome P450 2D6 1
21924610 10.1016/j.bmcl.2011.08.060 Gamma-secretase 1
21924610 10.1016/j.bmcl.2011.08.060 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine