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Compound Detail

CHEMBL255898

BARETTIN
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N=C(N)NCCC[C@@H]1NC(=O)/C(=C/c2c[nH]c3cc(Br)ccc23)NC1=O

Basic Information

ChEMBL ID CHEMBL255898
Name BARETTIN
Phase Preclinical
Structure Type MOL
InChI Key YYFNNPXWRXQUPR-JVXNRYDGSA-N
5
Targets
6
Activities
3
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

419.3
MW (Da)
1.15
ALogP
3
HBA
6
HBD
135.9
PSA (Ų)
0.19
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C17H19BrN6O2
MW 419.28
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness 0.37

Activity Summary

Ki 3 meas. best 6.47
EC50 2 meas. best 6.05
IC50 1 meas. best 5.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.47 6.47 340.0 1
Amphibalanus improvisus
CHEMBL613909
EC50 6.05 6.05 900.0 2
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 5.72 5.72 1910.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 5.71 5.71 1930.0 1
Receptor-interacting serine/threonine-protein kinase 2
CHEMBL5014
IC50 5.1 5.1 8000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1021/np50060a041 Ileum 2
18271554 10.1021/np0705209 Amphibalanus improvisus 1
17067154 10.1021/np0601760 Amphibalanus improvisus 1
17067154 10.1021/np0601760 Serotonin 2 receptors; 5-HT2a & 5-HT2c 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 1A 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 1D 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 2A 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 2C 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 3A 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 4 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 5A 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 6 1
17067154 10.1021/np0601760 5-hydroxytryptamine receptor 7 1
37857324 10.1021/acs.jmedchem.3c00593 Receptor-interacting serine/threonine-protein kinase 2 1

Data from ChEMBL 36 via Core Engine