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Compound Detail

CHEMBL4128051

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COc1ccc(C(=O)C2=C(O)C(=O)N(c3ccc(C(=O)N(C)C)cc3)C2c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL4128051
Phase Preclinical
Structure Type MOL
InChI Key LAMZIMAABVNXEM-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

456.5
MW (Da)
4.18
ALogP
5
HBA
1
HBD
87.2
PSA (Ų)
0.56
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24N2O5
MW 456.50
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.08

Activity Summary

IC50 1 meas. best 5.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 5.23 5.23 5920.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 5920.0 nM 5.23 Antagonist activity at human P2X3 receptor expressed in C6-BU-1 cells assessed a... 29805055

Literature References

PubMed DOI Target Context # Activities
29805055 10.1016/j.bmcl.2017.04.060 P2X purinoceptor 3 1

Data from ChEMBL 36 via Core Engine