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Compound Detail

CHEMBL576234

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COc1ccc(N2CCN(CCCCNC(=O)c3ccc(-c4ccccn4)cc3)CC2)c(OC)c1

Basic Information

ChEMBL ID CHEMBL576234
Phase Preclinical
Structure Type MOL
InChI Key KKVXRFAQMOVXOX-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

474.6
MW (Da)
4.10
ALogP
6
HBA
1
HBD
66.9
PSA (Ų)
0.45
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34N4O3
MW 474.61
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.42

Activity Summary

EC50 3 meas. best 5.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
EC50 5.55 5.55 2840.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19515567 10.1016/j.bmc.2009.05.040 Neuronal acetylcholine receptor subunit alpha-7 1
22410083 10.1016/j.bmcl.2012.02.052 Neuronal acetylcholine receptor subunit alpha-7 1
25827398 10.1016/j.ejmech.2015.03.025 Neuronal acetylcholine receptor subunit alpha-7 1

Data from ChEMBL 36 via Core Engine