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Compound Detail

CHEMBL4535866

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COCc1ccccc1[C@@H]1OCCn2cc(-c3cc4c(OC)c(C#N)ccc4[nH]3)nc21

Basic Information

ChEMBL ID CHEMBL4535866
Phase Preclinical
Structure Type MOL
InChI Key PKLALEKIGAUIEA-QHCPKHFHSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
4.18
ALogP
6
HBA
1
HBD
85.1
PSA (Ų)
0.53
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22N4O3
MW 414.47
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.65

Activity Summary

IC50 2 meas. best 7.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.07 7.07 85.0 1
Gamma-secretase
CHEMBL2094135
IC50 6.96 6.96 110.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu - - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31122869 10.1016/j.bmcl.2019.05.023 ADMET 4
31122869 10.1016/j.bmcl.2019.05.023 Unchecked 2
31122869 10.1016/j.bmcl.2019.05.023 Mus musculus 2
31122869 10.1016/j.bmcl.2019.05.023 Gamma-secretase 1

Data from ChEMBL 36 via Core Engine