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Compound Detail

CHEMBL4161165

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COc1cc2nc(N3CCC[C@H](NC(=O)c4ccco4)C3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL4161165
Phase Preclinical
Structure Type MOL
InChI Key KUSUAKLXHXASTN-LBPRGKRZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

397.4
MW (Da)
2.22
ALogP
8
HBA
2
HBD
115.7
PSA (Ų)
0.67
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H23N5O4
MW 397.44
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.35

Activity Summary

Ki 3 meas. best 9.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1B adrenergic receptor
CHEMBL232
Ki 9.55 9.55 0.3 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 9.48 9.48 0.3 1
Alpha-1A adrenergic receptor
CHEMBL229
Ki 9.2 9.2 0.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28499171 10.1016/j.ejmech.2017.05.003 Alpha-1D adrenergic receptor 1
28499171 10.1016/j.ejmech.2017.05.003 Alpha-1B adrenergic receptor 1
28499171 10.1016/j.ejmech.2017.05.003 Alpha-1A adrenergic receptor 1
28499171 10.1016/j.ejmech.2017.05.003 Panel NCI-60 (60 carcinoma cell lines) 1
28499171 10.1016/j.ejmech.2017.05.003 DU-145 1
28499171 10.1016/j.ejmech.2017.05.003 PC-3 1
28499171 10.1016/j.ejmech.2017.05.003 LNCaP 1

Data from ChEMBL 36 via Core Engine