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Compound Detail

CHEMBL5560391

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O=C1Nc2cccc(OC3CCN(C(=O)C4CC4)CC3)c2/C1=C/c1ccc2[nH]cnc2c1

Basic Information

ChEMBL ID CHEMBL5560391
Phase Preclinical
Structure Type MOL
InChI Key XLOIDRXYQMEUMU-PDGQHHTCSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

428.5
MW (Da)
3.84
ALogP
4
HBA
2
HBD
87.3
PSA (Ų)
0.62
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N4O3
MW 428.49
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.74

Activity Summary

IC50 2 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutaminyl-peptide cyclotransferase
CHEMBL4508
IC50 7.46 7.46 35.0 1
Glutaminyl-peptide cyclotransferase-like protein
CHEMBL3638349
IC50 6.75 6.75 180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38817193 10.1021/acs.jmedchem.4c00049 Glutaminyl-peptide cyclotransferase 1
38817193 10.1021/acs.jmedchem.4c00049 Glutaminyl-peptide cyclotransferase-like protein 1
38817193 10.1021/acs.jmedchem.4c00049 Pyroglutamyl-peptidase 1 1

Data from ChEMBL 36 via Core Engine