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Compound Detail

CHEMBL63421

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COc1ccc(CCNC[C@H](O)COc2ccc(-c3nc(C(C)=O)c[nH]3)cc2)cc1OC

Basic Information

ChEMBL ID CHEMBL63421
Phase Preclinical
Structure Type MOL
InChI Key PUGVVCVHIQBVOQ-IBGZPJMESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
2.87
ALogP
7
HBA
3
HBD
105.7
PSA (Ų)
0.29
QED
0
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N3O5
MW 439.51
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.46

Activity Summary

Kd 2 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Beta-1 adrenergic receptor
CHEMBL5471
Kd 7.76 7.76 17.4 1
Beta-2 adrenergic receptor
CHEMBL5414
Kd 4.2 4.2 63095.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
2872332 10.1021/jm00156a028 No relevant target 2
2903243 10.1021/jm00119a004 Adrenergic receptor beta 1
2903243 10.1021/jm00119a004 Beta-1 adrenergic receptor 1
2903243 10.1021/jm00119a004 Beta-2 adrenergic receptor 1
2872332 10.1021/jm00156a028 Beta-1 adrenergic receptor 1
2872332 10.1021/jm00156a028 Beta-2 adrenergic receptor 1
2872332 10.1021/jm00156a028 Rattus norvegicus 1
2872332 10.1021/jm00156a028 Adrenergic receptor beta; ADRB1 & ADRB2 1

Data from ChEMBL 36 via Core Engine