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Compound Detail

CHEMBL421871

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COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC

Basic Information

ChEMBL ID CHEMBL421871
Phase Preclinical
Structure Type MOL
InChI Key UFPJRJORSDHDFB-UHFFFAOYSA-N
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
4.22
ALogP
6
HBA
3
HBD
80.2
PSA (Ų)
0.52
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27NO5
MW 421.49
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness 0.84

Activity Summary

EC50 3 meas. best 7.57
IC50 2 meas. best 6.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 7.57 7.57 27.0 1
Beta-2 adrenergic receptor
CHEMBL210
IC50 6.12 6.12 760.0 1
Beta-2 adrenergic receptor
CHEMBL210
EC50 5.82 5.82 1500.0 1
Beta-1 adrenergic receptor
CHEMBL213
IC50 5.75 5.75 1800.0 1
Beta-1 adrenergic receptor
CHEMBL213
EC50 5.21 5.21 6100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11055339 10.1016/s0960-894x(00)00459-5 Beta-1 adrenergic receptor 3
11055339 10.1016/s0960-894x(00)00459-5 Beta-2 adrenergic receptor 3
11055339 10.1016/s0960-894x(00)00459-5 Beta-3 adrenergic receptor 2

Data from ChEMBL 36 via Core Engine