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Compound Detail

CHEMBL3246228

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COc1cc(Br)ccc1C(O)CNC(C)C.Cl

Basic Information

ChEMBL ID CHEMBL3246228
Phase Preclinical
Structure Type MOL
InChI Key LGEKVENERQVGLW-UHFFFAOYSA-N
Parent Compound CHEMBL3303705
Active Moiety CHEMBL3303705
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

288.2
MW (Da)
2.49
ALogP
3
HBA
2
HBD
41.5
PSA (Ų)
0.87
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H19BrClNO2
MW 324.65
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -0.17

Activity Summary

Kd 2 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-1 adrenergic receptor
CHEMBL5471
Kd 8.24 8.24 5.8 1
Beta-2 adrenergic receptor
CHEMBL5414
Kd 7.87 7.87 13.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31474 10.1021/jm00208a015 Beta-1 adrenergic receptor 4
31474 10.1021/jm00208a015 Beta-2 adrenergic receptor 3
31474 10.1021/jm00208a015 Unchecked 1

Data from ChEMBL 36 via Core Engine