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Compound Detail

CHEMBL5569159

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Cc1cccc(Cl)c1NC(=O)c1sc(Nc2ccc(F)c(Cl)c2)nc1N

Basic Information

ChEMBL ID CHEMBL5569159
Phase Preclinical
Structure Type MOL
InChI Key NGUNVBYQGKIOBV-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
16
PK Parameters
7
Publications
0
Known Names

Molecular Properties

411.3
MW (Da)
5.48
ALogP
5
HBA
3
HBD
80.0
PSA (Ų)
0.53
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H13Cl2FN4OS
MW 411.29
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -2.32

Activity Summary

EC50 2 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL2492
EC50 5.89 5.05 1300.0 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 1278.0 ng.hr.mL-1 Mus musculus
AUC 1282.0 ng.hr.mL-1 Mus musculus
AUC 4971.0 ng.hr.mL-1 Mus musculus
AUC 5107.0 ng.hr.mL-1 Mus musculus
CL 13.27 mL.min-1.kg-1 Mus musculus
Cmax 2.02 ug.mL-1 Mus musculus
Cmax 1.998 ug.mL-1 Mus musculus
F 39.0 % Mus musculus
MRT 0.7 hr Mus musculus
MRT 2.0 hr Mus musculus
T1/2 0.1733 hr Mus musculus
T1/2 1.1 hr Mus musculus
T1/2 1.5 hr Mus musculus
Tmax 0.1 hr Mus musculus
Tmax 0.5 hr Mus musculus
Vd 1.3 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38393821 10.1021/acs.jmedchem.3c02323 ADMET 16
38393821 10.1021/acs.jmedchem.3c02323 Neuronal acetylcholine receptor subunit alpha-7 10
38393821 10.1021/acs.jmedchem.3c02323 Mus musculus 4
38393821 10.1021/acs.jmedchem.3c02323 Sodium channel protein type 5 subunit alpha 1
38393821 10.1021/acs.jmedchem.3c02323 Neuronal acetylcholine receptor; alpha3/beta4 1
38393821 10.1021/acs.jmedchem.3c02323 Neuronal acetylcholine receptor; alpha4/beta2 1
38393821 10.1021/acs.jmedchem.3c02323 5-hydroxytryptamine receptor 3A 1

Data from ChEMBL 36 via Core Engine