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Compound Detail

CHEMBL289981

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COc1ccccc1N1CCN(C[C@H](C(=O)NC(C)(C)C)c2ccccc2)CC1

Basic Information

ChEMBL ID CHEMBL289981
Phase Preclinical
Structure Type MOL
InChI Key UMTDAKAAYOXIKU-FQEVSTJZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

395.6
MW (Da)
3.52
ALogP
4
HBA
1
HBD
44.8
PSA (Ų)
0.81
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 C24H33N3O2
MW 395.55
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.09

Activity Summary

IC50 2 meas. best 6.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
IC50 6.36 6.36 437.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
IC50 5.56 5.56 2781.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8496920 10.1021/jm00062a028 5-hydroxytryptamine receptor 1A 1
8496920 10.1021/jm00062a028 5-hydroxytryptamine receptor 1B 1
8496920 10.1021/jm00062a028 5-hydroxytryptamine receptor 2C 1
8496920 10.1021/jm00062a028 Serotonin 2 (5-HT2) receptor 1
8496920 10.1021/jm00062a028 D(1A) dopamine receptor 1
8496920 10.1021/jm00062a028 D(2) dopamine receptor 1
8496920 10.1021/jm00062a028 Adrenergic receptor alpha-1 1
8496920 10.1021/jm00062a028 Adrenergic receptor alpha-2 1
8496920 10.1021/jm00062a028 Adrenergic receptor beta 1

Data from ChEMBL 36 via Core Engine