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Compound Detail

CHEMBL4549121

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COc1c(C#N)ccc2[nH]c(-c3cn4c(n3)[C@H](c3ccccc3Cl)OCC4)cc12

Basic Information

ChEMBL ID CHEMBL4549121
Phase Preclinical
Structure Type MOL
InChI Key CHLUUWQLDURKRV-NRFANRHFSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

404.9
MW (Da)
4.68
ALogP
5
HBA
1
HBD
75.9
PSA (Ų)
0.54
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 C22H17ClN4O2
MW 404.86
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.87

Activity Summary

IC50 2 meas. best 7.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.64 7.64 23.0 1
Gamma-secretase
CHEMBL2094135
IC50 7.58 7.58 26.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.0047 - 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