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Compound Detail

CHEMBL40554

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C[N+](C)(C)CC#CCOC(=O)Nc1cccc(Cl)c1

Basic Information

ChEMBL ID CHEMBL40554
Phase Preclinical
Structure Type MOL
InChI Key DDKOMKXCUXCQBS-UHFFFAOYSA-O
5
Targets
8
Activities
1
Assay Types
1
PK Parameters
17
Publications
0
Known Names

Molecular Properties

281.8
MW (Da)
2.60
ALogP
2
HBA
1
HBD
38.3
PSA (Ų)
0.68
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H18ClN2O2+
MW 281.76
Aromatic Rings 1
Heavy Atoms 19
NP-Likeness -1.12

Activity Summary

Ki 8 meas. best 5.71

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M1
CHEMBL216
Ki 5.71 5.71 1949.8 1
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 5.62 5.62 2398.8 1
Muscarinic acetylcholine receptor M2
CHEMBL211
Ki 5.49 5.49 3235.9 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
Ki 5.42 5.42 3801.9 1
Muscarinic acetylcholine receptor M4
CHEMBL1821
Ki 5.04 5.04 9120.1 1

Pharmacokinetic Data

Parameter Value Units Species
KA 8.75 uM Oryctolagus cuniculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18543900 10.1021/jm800145d Unchecked 2
9703467 10.1021/jm9708588 Rattus norvegicus 2
1379640 10.1021/jm00093a011 Rattus norvegicus 2
2472484 10.1021/jm00127a031 Muscarinic acetylcholine receptor 1
18543900 10.1021/jm800145d Muscarinic acetylcholine receptor M5 1
18543900 10.1021/jm800145d Muscarinic acetylcholine receptor M4 1
18543900 10.1021/jm800145d Muscarinic acetylcholine receptor M3 1
18543900 10.1021/jm800145d Muscarinic acetylcholine receptor M2 1
18543900 10.1021/jm800145d Muscarinic acetylcholine receptor M1 1
1379640 10.1021/jm00093a011 Muscarinic acetylcholine receptor M1 1
9703467 10.1021/jm9708588 Muscarinic acetylcholine receptor M1 1
2472484 10.1021/jm00127a031 Rattus norvegicus 1
9703467 10.1021/jm9708588 Muscarinic receptor M2 and M3 1
9703467 10.1021/jm9708588 Unchecked 1
9703467 10.1021/jm9708588 Muscarinic receptor M1 and M2 1
9703467 10.1021/jm9708588 Muscarinic acetylcholine receptor M3 1
9703467 10.1021/jm9708588 Muscarinic acetylcholine receptor M2 1

Data from ChEMBL 36 via Core Engine