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Compound Detail

CHEMBL5555218

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CC[N+]1(C)CCN(c2ccc(C(=O)Nc3cccc(C)n3)cc2)CC1.[I-]

Basic Information

ChEMBL ID CHEMBL5555218
Phase Preclinical
Structure Type MOL
InChI Key TYKIRTIGTHHZSX-UHFFFAOYSA-N
Parent Compound CHEMBL6070794
Active Moiety CHEMBL6070794
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

339.5
MW (Da)
2.93
ALogP
3
HBA
1
HBD
45.2
PSA (Ų)
0.87
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27IN4O
MW 466.37
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.36

Activity Summary

EC50 3 meas. best 6.32
IC50 1 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha9/alpha10
CHEMBL2109238
EC50 6.32 6.32 480.0 1
Neuronal acetylcholine receptor subunit alpha-9
CHEMBL2184
EC50 6.29 6.29 510.0 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
EC50 5.21 5.21 6100.0 1
Unchecked
CHEMBL612545
IC50 5.05 5.05 9000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38748608 10.1021/acs.jmedchem.3c02429 ADMET 15
38748608 10.1021/acs.jmedchem.3c02429 Unchecked 9
38748608 10.1021/acs.jmedchem.3c02429 Neuronal acetylcholine receptor subunit alpha-9 3
38748608 10.1021/acs.jmedchem.3c02429 Neuronal acetylcholine receptor; alpha9/alpha10 3
38748608 10.1021/acs.jmedchem.3c02429 Neuronal acetylcholine receptor subunit alpha-7 3
38748608 10.1021/acs.jmedchem.3c02429 Mus musculus 3
38748608 10.1021/acs.jmedchem.3c02429 Neuronal acetylcholine receptor; alpha4/beta2 2
38748608 10.1021/acs.jmedchem.3c02429 Neuronal acetylcholine receptor; alpha3/beta4 2
38748608 10.1021/acs.jmedchem.3c02429 THP-1 1
38748608 10.1021/acs.jmedchem.3c02429 No relevant target 1

Data from ChEMBL 36 via Core Engine