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Compound Detail

CHEMBL2112361

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COc1ccccc1N1CCN(CCNc2nc3nc4c(c(=O)n(C)c(=O)n4C)n3cc2Br)CC1

Basic Information

ChEMBL ID CHEMBL2112361
Phase Preclinical
Structure Type MOL
InChI Key MRQQSBLXMAXDIC-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

543.4
MW (Da)
1.29
ALogP
11
HBA
1
HBD
101.9
PSA (Ų)
0.39
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27BrN8O3
MW 543.43
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.57

Activity Summary

Ki 4 meas. best 7.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.21 7.21 62.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 7.21 7.21 62.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 7.07 7.07 86.0 1
D(2) dopamine receptor
CHEMBL339
Ki 6.65 6.65 226.0 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

Data from ChEMBL 36 via Core Engine