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Compound Detail

CHEMBL4458893

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COc1ccc(C(=O)C2=C(O)C(=O)N(c3ccc(-c4ccon4)cc3)C2C2CCCCC2)cn1

Basic Information

ChEMBL ID CHEMBL4458893
Phase Preclinical
Structure Type MOL
InChI Key VINGOJRLECRAOW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

459.5
MW (Da)
4.74
ALogP
7
HBA
1
HBD
105.8
PSA (Ų)
0.53
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 C26H25N3O5
MW 459.50
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.08

Activity Summary

IC50 1 meas. best 7.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 3
CHEMBL2998
IC50 7.36 7.36 44.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.6 mL.min-1.kg-1 Rattus norvegicus
F 28.1 % Rattus norvegicus
Fu 0.003 - Rattus norvegicus
T1/2 1.4 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 3 IC50 = 44.0 nM 7.36 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 No relevant target 1
30728111 10.1016/j.bmcl.2019.01.039 P2X purinoceptor 3 1

Data from ChEMBL 36 via Core Engine