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Compound Detail

CHEMBL3290978

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OCc1cc(C(O)CNCCc2ccc(N3CCN(c4ccccc4)CC3)cc2)ccc1O

Basic Information

ChEMBL ID CHEMBL3290978
Phase Preclinical
Structure Type MOL
InChI Key GRABPNBVFQHUCW-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
3.08
ALogP
6
HBA
4
HBD
79.2
PSA (Ų)
0.38
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H33N3O3
MW 447.58
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.28

Activity Summary

EC50 1 meas. best 6.7
Ki 1 meas. best 4.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-2 adrenergic receptor
CHEMBL210
EC50 6.7 6.7 199.5 1
Beta-2 adrenergic receptor
CHEMBL210
Ki 4.5 4.5 31622.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24813741 10.1016/j.bmcl.2014.04.069 Beta-2 adrenergic receptor 2
24813741 10.1016/j.bmcl.2014.04.069 Beta-1 adrenergic receptor 1
24813741 10.1016/j.bmcl.2014.04.069 Unchecked 1

Data from ChEMBL 36 via Core Engine