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Compound Detail

CHEMBL570992

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Cn1cc(C(=O)OC[C@H]2CN(Cc3ccc(Cl)cc3)c3cn(CCc4ccccc4)nc3C(=O)N2)c2ccccc21

Basic Information

ChEMBL ID CHEMBL570992
Phase Preclinical
Structure Type MOL
InChI Key HWRGZLMRUZLFLA-RUZDIDTESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

568.1
MW (Da)
5.25
ALogP
7
HBA
1
HBD
81.4
PSA (Ų)
0.26
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H30ClN5O3
MW 568.08
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -0.83

Activity Summary

IC50 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL4805
IC50 6.6 6.6 250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 IC50 = 250.0 nM 6.6 Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as... 19800793

Literature References

PubMed DOI Target Context # Activities
19800793 10.1016/j.bmcl.2009.09.053 P2X purinoceptor 7 3

Data from ChEMBL 36 via Core Engine