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Compound Detail

CHEMBL2442274

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N=C1NC(=O)/C(=C\c2c[nH]c3c(Br)cccc23)N1

Basic Information

ChEMBL ID CHEMBL2442274
Phase Preclinical
Structure Type MOL
InChI Key LWVFMDTWYOYNOZ-RUDMXATFSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

305.1
MW (Da)
1.93
ALogP
2
HBA
4
HBD
80.8
PSA (Ų)
0.61
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H9BrN4O
MW 305.13
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.04

Activity Summary

Ki 5 meas. best 6.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 5A
CHEMBL3426
Ki 6.95 6.95 112.0 1
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 6.34 6.34 457.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.08 6.08 841.0 1
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 5.85 5.85 1405.0 1
5-hydroxytryptamine receptor 2A
CHEMBL322
Ki 5.67 5.67 2147.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24084296 10.1016/j.bmc.2013.09.011 5-hydroxytryptamine receptor 1E 1
24084296 10.1016/j.bmc.2013.09.011 5-hydroxytryptamine receptor 2A 1
24084296 10.1016/j.bmc.2013.09.011 5-hydroxytryptamine receptor 6 1
24084296 10.1016/j.bmc.2013.09.011 5-hydroxytryptamine receptor 2C 1
24084296 10.1016/j.bmc.2013.09.011 5-hydroxytryptamine receptor 2B 1
24084296 10.1016/j.bmc.2013.09.011 5-hydroxytryptamine receptor 5A 1

Data from ChEMBL 36 via Core Engine