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Compound Detail

CHEMBL2059307

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O=C1CCc2ncccc2N1CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1

Basic Information

ChEMBL ID CHEMBL2059307
Phase Preclinical
Structure Type MOL
InChI Key LAMDTGOBCQBCBW-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

405.5
MW (Da)
2.73
ALogP
5
HBA
1
HBD
74.2
PSA (Ų)
0.71
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N5O2
MW 405.50
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.40

Activity Summary

EC50 1 meas. best 7.92
Ki 1 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL216
EC50 7.92 7.92 12.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22677319 10.1016/j.bmcl.2012.05.048 Muscarinic acetylcholine receptor M1 2
22677319 10.1016/j.bmcl.2012.05.048 Liver microsomes 1
22677319 10.1016/j.bmcl.2012.05.048 D(2) dopamine receptor 1
22677319 10.1016/j.bmcl.2012.05.048 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine