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Compound Detail

CHEMBL2179866

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O=C(N[C@@H]1C2CCN(CC2)[C@H]1Cc1cccnc1)c1ccc(Br)o1

Basic Information

ChEMBL ID CHEMBL2179866
Phase Preclinical
Structure Type MOL
InChI Key FONCJXWMQYTPRQ-WMLDXEAASA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

390.3
MW (Da)
2.87
ALogP
4
HBA
1
HBD
58.4
PSA (Ų)
0.87
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20BrN3O2
MW 390.28
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.88

Activity Summary

Ki 2 meas. best 7.25
EC50 1 meas. best 5.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
Ki 7.25 7.25 56.3 1
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907589
Ki 6.3 6.3 500.0 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
EC50 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23126648 10.1021/jm301048a Neuronal acetylcholine receptor subunit alpha-7 3
23126648 10.1021/jm301048a 5-hydroxytryptamine receptor 3A 1
23126648 10.1021/jm301048a Neuronal acetylcholine receptor; alpha4/beta2 1

Data from ChEMBL 36 via Core Engine