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Compound Detail

CHEMBL1628078

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COc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2(C)[C@@H](NCCNc3ccc([N+](=O)[O-])cn3)CC[C@@H]12

Basic Information

ChEMBL ID CHEMBL1628078
Phase Preclinical
Structure Type MOL
InChI Key KYMJWJCKOMPUHJ-XRKIENNPSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

450.6
MW (Da)
4.92
ALogP
6
HBA
2
HBD
89.3
PSA (Ų)
0.35
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H34N4O3
MW 450.58
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness 0.14

Activity Summary

IC50 2 meas. best 5.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-lactamase
CHEMBL2026
IC50 5.3 5.3 5000.0 1
Chymotrypsin-C
CHEMBL2386
IC50 4.89 4.89 13000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Beta-lactamase IC50 = 5000.0 nM 5.3 Inhibitory activity against beta-lactamase 11931626
Chymotrypsin-C IC50 = 13000.0 nM 4.89 Inhibitory activity against chymotrypsinogen 11931626

Literature References

PubMed DOI Target Context # Activities
11931626 10.1021/jm010533y Beta-lactamase 3
11931626 10.1021/jm010533y Chymotrypsin-C 1
11931626 10.1021/jm010533y Unchecked 1

Data from ChEMBL 36 via Core Engine