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Compound Detail

CHEMBL193867

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COc1ccccc1N1CCN(CCCNc2nc3nc4c(c(=O)n(C)c(=O)n4C)n3cc2Br)CC1

Basic Information

ChEMBL ID CHEMBL193867
Phase Preclinical
Structure Type MOL
InChI Key GNPOCHWUDXCHTJ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

557.5
MW (Da)
1.68
ALogP
11
HBA
1
HBD
101.9
PSA (Ų)
0.34
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29BrN8O3
MW 557.45
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.52

Activity Summary

Ki 5 meas. best 7.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.44 7.44 36.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.42 7.42 38.0 1
D(2) dopamine receptor
CHEMBL339
Ki 6.49 6.49 325.0 1
Unchecked
CHEMBL612545
Ki 6.49 6.49 323.6 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 6.06 6.06 880.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15115407 10.1021/jm030946u 5-hydroxytryptamine receptor 1A 3
15115407 10.1021/jm030946u 5-hydroxytryptamine receptor 2A 2
15115407 10.1021/jm030946u D(2) dopamine receptor 1
15115407 10.1021/jm030946u Adrenergic receptor alpha-1 1
15808487 10.1016/j.bmcl.2005.02.012 Unchecked 1

Data from ChEMBL 36 via Core Engine