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Compound Detail

CHEMBL301078

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COc1ccccc1N1CCN(CCNc2ccc3c4c(=O)n(C)nc(Cl)c4cn3n2)CC1

Basic Information

ChEMBL ID CHEMBL301078
Phase Preclinical
Structure Type MOL
InChI Key STIKULJYVCUQJQ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

468.0
MW (Da)
2.48
ALogP
9
HBA
1
HBD
79.9
PSA (Ų)
0.47
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26ClN7O2
MW 467.96
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.57

Activity Summary

Ki 5 meas. best 8.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
Ki 8.96 8.96 1.1 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 8.52 8.52 3.0 1
Alpha-1B adrenergic receptor
CHEMBL232
Ki 7.82 7.82 15.2 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.79 7.79 16.3 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.13 7.13 73.3 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9888842 10.1021/jm981006q Adrenergic receptor alpha-1 1
9888842 10.1021/jm981006q 5-hydroxytryptamine receptor 1A 1
9888842 10.1021/jm981006q Alpha-1A adrenergic receptor 1
9888842 10.1021/jm981006q Alpha-1B adrenergic receptor 1
9888842 10.1021/jm981006q Alpha-1D adrenergic receptor 1
9888842 10.1021/jm981006q Unchecked 1

Data from ChEMBL 36 via Core Engine