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Compound Detail

CHEMBL4589123

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COc1ccccc1CCn1cnc2sc3c(c2c1=O)CCN(S(=O)(=O)c1ccc(F)cc1)C3

Basic Information

ChEMBL ID CHEMBL4589123
Phase Preclinical
Structure Type MOL
InChI Key IFSYYEGWQCBGLX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

499.6
MW (Da)
3.60
ALogP
7
HBA
0
HBD
81.5
PSA (Ų)
0.41
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 C24H22FN3O4S2
MW 499.59
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -2.08

Activity Summary

IC50 1 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 6.08 6.08 840.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 315.0 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 = 840.0 nM 6.08 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 No relevant target 1
27423478 10.1016/j.bmcl.2016.07.009 ADMET 1

Data from ChEMBL 36 via Core Engine