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Compound Detail

CHEMBL5178333

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O=C(Cn1c(=O)n(Cc2ccc(Cl)cc2)c2c(N3CCOCC3)nc(Cl)nc21)Nc1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL5178333
Phase Preclinical
Structure Type MOL
InChI Key ZKPPECAMJDRQNC-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

547.8
MW (Da)
4.08
ALogP
8
HBA
1
HBD
94.3
PSA (Ų)
0.37
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21Cl3N6O3
MW 547.83
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.73

Activity Summary

IC50 1 meas. best 5.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 5.51 5.51 3070.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 3070.0 nM 5.51 Antagonist activity at human P2X3R expressed in HEK293 cells assessed as reducti... 35849939

Literature References

PubMed DOI Target Context # Activities
35849939 10.1016/j.ejmech.2022.114556 P2X purinoceptor 3 1

Data from ChEMBL 36 via Core Engine