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Compound Detail

CHEMBL513228

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CCOC(=O)c1ccc(NC(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)NC2CCN(CC)C2)cc1

Basic Information

ChEMBL ID CHEMBL513228
Phase Preclinical
Structure Type MOL
InChI Key AMISGKITNKHXTK-IAXKEJLGSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

468.6
MW (Da)
2.51
ALogP
6
HBA
4
HBD
120.0
PSA (Ų)
0.42
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H32N4O5
MW 468.55
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness -1.16

Activity Summary

IC50 2 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M3
CHEMBL245
IC50 6.1 6.1 794.3 1
Muscarinic acetylcholine receptor M2
CHEMBL211
IC50 5.6 5.6 2511.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18818072 10.1016/j.bmcl.2008.09.020 Muscarinic acetylcholine receptor M1 and M3 1
18818072 10.1016/j.bmcl.2008.09.020 Muscarinic acetylcholine receptor M2 1
18818072 10.1016/j.bmcl.2008.09.020 Muscarinic acetylcholine receptor M1 1
18818072 10.1016/j.bmcl.2008.09.020 Muscarinic acetylcholine receptor M3 1
18818072 10.1016/j.bmcl.2008.09.020 Muscarinic acetylcholine receptors; M2 & M3 1

Data from ChEMBL 36 via Core Engine