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Compound Detail

CHEMBL358060

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COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CCl)cc3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL358060
Phase Preclinical
Structure Type MOL
InChI Key UIQGXHPFAXTQFN-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

500.0
MW (Da)
4.74
ALogP
7
HBA
1
HBD
93.8
PSA (Ų)
0.28
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H34ClN5O3
MW 500.04
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.83

Activity Summary

Kd 4 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1B adrenergic receptor
CHEMBL315
Kd 9.15 9.15 0.7 1
Alpha-1D adrenergic receptor
CHEMBL326
Kd 7.71 7.71 19.5 1
Alpha-1A adrenergic receptor
CHEMBL319
Kd 7.11 7.11 77.6 1
Adrenergic receptor alpha-2
CHEMBL2093864
Kd 5.54 5.54 2884.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9822553 10.1021/jm9810654 Alpha-1A adrenergic receptor 1
9822553 10.1021/jm9810654 Alpha-1B adrenergic receptor 1
9822553 10.1021/jm9810654 Alpha-1D adrenergic receptor 1
9822553 10.1021/jm9810654 Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine