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Compound Detail

CHEMBL4447043

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NS(=O)(=O)c1cc(NC(=O)Cc2c(F)cccc2Cl)ccc1Oc1cccc(Cl)c1

Basic Information

ChEMBL ID CHEMBL4447043
Phase Preclinical
Structure Type MOL
InChI Key OVAMQESCERMHIF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

469.3
MW (Da)
4.75
ALogP
4
HBA
2
HBD
98.5
PSA (Ų)
0.54
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15Cl2FN2O4S
MW 469.32
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -2.13

Activity Summary

IC50 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 4
CHEMBL2104
IC50 8.05 8.05 9.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 44.83 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 4 IC50 = 9.0 nM 8.05 Antagonist activity at human P2X4 receptor tranfected in HEK293 cells assessed a... 31746599

Literature References

PubMed DOI Target Context # Activities
31746599 10.1021/acs.jmedchem.9b01304 P2X purinoceptor 4 1
31746599 10.1021/acs.jmedchem.9b01304 Nuclear receptor subfamily 1 group I member 2 1
31746599 10.1021/acs.jmedchem.9b01304 ADMET 1
31746599 10.1021/acs.jmedchem.9b01304 No relevant target 1

Data from ChEMBL 36 via Core Engine