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Compound Detail

CHEMBL4440083

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COc1cc(CCn2cnc3sc4c(c3c2=O)CCN(S(=O)(=O)C2CCCC2)C4)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL4440083
Phase Preclinical
Structure Type MOL
InChI Key VXBOFAACMMKOEG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

503.6
MW (Da)
3.35
ALogP
8
HBA
0
HBD
90.7
PSA (Ų)
0.49
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N3O5S2
MW 503.65
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.48

Activity Summary

IC50 1 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 7.4 7.4 40.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 190.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 40.0 nM 7.4 Antagonist activity at human recombinant P2X3 receptor expressed in HEK293-Tet-o... 27423478

Literature References

PubMed DOI Target Context # Activities
27423478 10.1016/j.bmcl.2016.07.009 P2X purinoceptor 3 1
27423478 10.1016/j.bmcl.2016.07.009 ADMET 1

Data from ChEMBL 36 via Core Engine