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Compound Detail

CHEMBL195849

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Cn1c(=O)c2c(nc3nc(NCCCN4CCN(c5cccc(Cl)c5)CC4)c(Br)cn32)n(C)c1=O

Basic Information

ChEMBL ID CHEMBL195849
Phase Preclinical
Structure Type MOL
InChI Key JUFILDWSJBSFAQ-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

561.9
MW (Da)
2.32
ALogP
10
HBA
1
HBD
92.7
PSA (Ų)
0.36
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26BrClN8O2
MW 561.87
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.77

Activity Summary

Ki 5 meas. best 7.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.34 7.34 46.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.31 7.31 49.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 7.07 7.07 85.0 1
D(2) dopamine receptor
CHEMBL339
Ki 6.58 6.58 264.0 1
Unchecked
CHEMBL612545
Ki 6.58 6.58 263.0 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