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Compound Detail

CHEMBL2010933

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CC(=O)N1CCN(c2nc(NC(c3ccccc3)c3ccccc3)c3c(n2)C(=O)N(C(C)C)C3)CC1

Basic Information

ChEMBL ID CHEMBL2010933
Phase Preclinical
Structure Type MOL
InChI Key GBKVUQVWUBJGLI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
3.71
ALogP
6
HBA
1
HBD
81.7
PSA (Ų)
0.57
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 C28H32N6O2
MW 484.60
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.06

Activity Summary

IC50 1 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 6.57 6.57 268.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 268.0 nM 6.57 Antagonist activity at human P2X3 receptor expressed in RLE cells assessed as in... 22370269

Literature References

PubMed DOI Target Context # Activities
22370269 10.1016/j.bmcl.2012.01.124 P2X purinoceptor 3 1
22370269 10.1016/j.bmcl.2012.01.124 No relevant target 1

Data from ChEMBL 36 via Core Engine