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Compound Detail

CHEMBL2152921

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CO[C@H]1CC[C@]2(CC1)Cc1ccc(-c3cc(Cl)c(F)c(C#N)c3)cc1C21N=C(C)C(N)=N1

Basic Information

ChEMBL ID CHEMBL2152921
Phase Preclinical
Structure Type MOL
InChI Key FMNVIPHETSINMI-SSEMJGATSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

450.9
MW (Da)
5.13
ALogP
5
HBA
1
HBD
83.8
PSA (Ų)
0.69
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24ClFN4O
MW 450.95
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.06

Activity Summary

IC50 2 meas. best 9.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-secretase 1
CHEMBL4822
IC50 9.23 9.185 0.6 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-secretase 1 IC50 = 0.59 nM 9.23 Inhibition of BACE by secreted APPbeta release assay 24900397
Beta-secretase 1 IC50 = 0.72 nM 9.14 Inhibition of BACE by TR-FRET assay 24900397

Literature References

PubMed DOI Target Context # Activities
24900397 10.1021/ml300324q Beta-secretase 1 2

Data from ChEMBL 36 via Core Engine