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Compound Detail

CHEMBL2012521

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CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c3ccccc3c12.Cl

Basic Information

ChEMBL ID CHEMBL2012521
Phase Preclinical
Structure Type MOL
InChI Key WXJMSVGWWYAGRR-FTBISJDPSA-N
Parent Compound CHEMBL2012520
Active Moiety CHEMBL2012520
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

524.6
MW (Da)
4.96
ALogP
6
HBA
4
HBD
122.5
PSA (Ų)
0.19
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H33ClN4O4
MW 561.08
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -0.65

Activity Summary

EC50 2 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-3 adrenergic receptor
CHEMBL246
EC50 8.62 8.62 2.4 1
Beta-3 adrenergic receptor
CHEMBL4031
EC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900353 10.1021/ml200071k Beta-3 adrenergic receptor 4
24900353 10.1021/ml200071k Beta-2 adrenergic receptor 2
24900353 10.1021/ml200071k Beta-1 adrenergic receptor 2

Data from ChEMBL 36 via Core Engine