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Compound Detail

CHEMBL104803

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COc1ccc2c(c1)CCN1Cc3c(ccc4[nH]c(C)c(-c5nc(C)no5)c34)OC21

Basic Information

ChEMBL ID CHEMBL104803
Phase Preclinical
Structure Type MOL
InChI Key LEYDLUKDXKBMCP-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

402.4
MW (Da)
4.29
ALogP
6
HBA
1
HBD
76.4
PSA (Ų)
0.54
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N4O3
MW 402.45
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.52

Activity Summary

Ki 5 meas. best 7.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor M4
CHEMBL1821
Ki 7.21 7.21 61.7 1
Muscarinic acetylcholine receptor M2
CHEMBL211
Ki 5.66 5.66 2187.8 1
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 5.51 5.51 3090.3 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
Ki 5.21 5.21 6165.9 1
Muscarinic acetylcholine receptor M1
CHEMBL216
Ki 5.12 5.12 7585.8 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12086495 10.1021/jm011116o Muscarinic acetylcholine receptor M1 1
12086495 10.1021/jm011116o Muscarinic acetylcholine receptor M2 1
12086495 10.1021/jm011116o Muscarinic acetylcholine receptor M3 1
12086495 10.1021/jm011116o Muscarinic acetylcholine receptor M4 1
12086495 10.1021/jm011116o Muscarinic acetylcholine receptor M5 1

Data from ChEMBL 36 via Core Engine