Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4444359

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
COc1ccccc1C1C(C(=O)C(C)(C)C)=C(O)C(=O)N1c1ccc(-c2ccon2)cc1

Basic Information

ChEMBL ID CHEMBL4444359
Phase Preclinical
Structure Type MOL
InChI Key MLRLUDWLRDYPCT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

432.5
MW (Da)
4.87
ALogP
6
HBA
1
HBD
92.9
PSA (Ų)
0.62
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N2O5
MW 432.48
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.88

Activity Summary

IC50 1 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 6.26 6.26 553.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 1.3 mL.min-1.kg-1 Rattus norvegicus
F 77.9 % Rattus norvegicus
Fu 0.002 - Rattus norvegicus
T1/2 2.6 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 553.0 nM 6.26 Antagonist activity at human P2X3 receptor expressed in rat C6BU-1 cells measure... 30728111

Literature References

PubMed DOI Target Context # Activities
30728111 10.1016/j.bmcl.2019.01.039 ADMET 4
30728111 10.1016/j.bmcl.2019.01.039 P2X purinoceptor 3 1
30728111 10.1016/j.bmcl.2019.01.039 No relevant target 1

Data from ChEMBL 36 via Core Engine