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Compound Detail

CHEMBL4522504

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Cc1ccccc1CC(=O)Nc1ccc(Oc2cccc(Cl)c2)c(S(N)(=O)=O)c1

Basic Information

ChEMBL ID CHEMBL4522504
Phase Preclinical
Structure Type MOL
InChI Key PDZXSDVDZUTJTM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

430.9
MW (Da)
4.27
ALogP
4
HBA
2
HBD
98.5
PSA (Ų)
0.61
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 C21H19ClN2O4S
MW 430.91
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.83

Activity Summary

IC50 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 4
CHEMBL2104
IC50 8.0 8.0 10.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 47.0 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 = 10.0 nM 8.0 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 Nuclear receptor subfamily 1 group I member 2 1
31746599 10.1021/acs.jmedchem.9b01304 P2X purinoceptor 4 1
31746599 10.1021/acs.jmedchem.9b01304 ADMET 1

Data from ChEMBL 36 via Core Engine