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Compound Detail

CHEMBL143463

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COc1ccccc1N1CCN(CCCN2C(=O)CSc3c(OCC(O)CNC(C)(C)C)cccc32)CC1

Basic Information

ChEMBL ID CHEMBL143463
Phase Preclinical
Structure Type MOL
InChI Key UORFXDKDNXZABJ-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

542.8
MW (Da)
3.47
ALogP
8
HBA
2
HBD
77.5
PSA (Ų)
0.45
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 C29H42N4O4S
MW 542.75
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -1.03

Activity Summary

Ki 4 meas. best 8.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 8.89 8.89 1.3 1
Beta-2 adrenergic receptor
CHEMBL2289
Ki 8.57 8.57 2.7 1
Beta-1 adrenergic receptor
CHEMBL3252
Ki 8.28 8.28 5.3 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 6.28 6.28 530.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10743949 10.1016/s0960-894x(00)00016-0 Adrenergic receptor alpha-1 1
10743949 10.1016/s0960-894x(00)00016-0 Adrenergic receptor alpha-2 1
10743949 10.1016/s0960-894x(00)00016-0 Beta-1 adrenergic receptor 1
10743949 10.1016/s0960-894x(00)00016-0 Beta-2 adrenergic receptor 1
10743949 10.1016/s0960-894x(00)00016-0 Unchecked 1

Data from ChEMBL 36 via Core Engine