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Compound Detail

CHEMBL3740645

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Cc1ccc(-c2ccnn(CCO)c2=O)cc1NC(=O)C1=CN(C)C(=O)C[C@H]1c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL3740645
Phase Preclinical
Structure Type MOL
InChI Key HGEOVIQRQNEECN-NRFANRHFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

476.5
MW (Da)
2.82
ALogP
6
HBA
2
HBD
104.5
PSA (Ų)
0.57
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25FN4O4
MW 476.51
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.08

Activity Summary

IC50 1 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2X purinoceptor 7
CHEMBL4805
IC50 7.77 7.77 17.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2X purinoceptor 7 IC50 = 17.0 nM 7.77 Antagonist activity at P2X7R in human whole blood assessed as inhibition of LPS-... 26460788

Literature References

PubMed DOI Target Context # Activities
26460788 10.1021/acs.jmedchem.5b00365 P2X purinoceptor 7 1
26460788 10.1021/acs.jmedchem.5b00365 Salmonella typhimurium 1

Data from ChEMBL 36 via Core Engine