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Compound Detail

CHEMBL3618440

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C/C(=N\c1ccc2c(c1)[C@@H](NC(=O)c1ccc(Br)cc1)[C@H](O)C2)NCc1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL3618440
Phase Preclinical
Structure Type MOL
InChI Key JVWDGMMGXIGYDW-DNQXCXABSA-N
3
Targets
3
Activities
1
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

496.4
MW (Da)
4.82
ALogP
3
HBA
3
HBD
73.7
PSA (Ų)
0.35
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 C25H23BrFN3O2
MW 496.38
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.71

Activity Summary

EC50 3 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL216
EC50 7.68 7.68 20.9 1
Muscarinic acetylcholine receptor M2
CHEMBL211
EC50 7.14 7.14 71.8 1
Muscarinic acetylcholine receptor M4
CHEMBL1821
EC50 6.94 6.94 115.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 634.0 ng.hr/g Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26299349 10.1016/j.bmcl.2015.08.011 Muscarinic acetylcholine receptor M1 2
26299349 10.1016/j.bmcl.2015.08.011 Muscarinic acetylcholine receptor M2 2
26299349 10.1016/j.bmcl.2015.08.011 Muscarinic acetylcholine receptor M4 2
26299349 10.1016/j.bmcl.2015.08.011 No relevant target 2
26299349 10.1016/j.bmcl.2015.08.011 Muscarinic acetylcholine receptor M3 1
26299349 10.1016/j.bmcl.2015.08.011 Muscarinic acetylcholine receptor M5 1
26299349 10.1016/j.bmcl.2015.08.011 Brain 1
26299349 10.1016/j.bmcl.2015.08.011 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine