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Compound Detail

CHEMBL577977

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

Basic Information

ChEMBL ID CHEMBL577977
Phase Preclinical
Structure Type MOL
InChI Key RBGNXJHKDGUQME-XMMPIXPASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

578.6
MW (Da)
4.50
ALogP
9
HBA
1
HBD
124.5
PSA (Ų)
0.16
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H30N6O5
MW 578.63
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -0.90

Activity Summary

IC50 1 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL4805
IC50 5.85 5.85 1420.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 IC50 = 1420.0 nM 5.85 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