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Compound Detail

CHEMBL5201961

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O=C(Nc1cccc(-c2ccn(C(Cc3cc[n+]([O-])cc3)c3ccc(OC(F)F)c(OCC4CC4)c3)n2)c1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL5201961
Phase Preclinical
Structure Type MOL
InChI Key HEGXYQLDVWSIOY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

596.6
MW (Da)
6.66
ALogP
6
HBA
1
HBD
92.3
PSA (Ų)
0.13
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H30F2N4O4
MW 596.63
Aromatic Rings 5
Heavy Atoms 44
NP-Likeness -1.49

Activity Summary

IC50 1 meas. best 5.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 5.01 5.01 9760.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 9760.0 nM 5.01 Antagonist activity at human P2X3R expressed in HEK293 cells assessed as reducti... 35849939

Literature References

PubMed DOI Target Context # Activities
35849939 10.1016/j.ejmech.2022.114556 P2X purinoceptor 3 1

Data from ChEMBL 36 via Core Engine