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Compound Detail

CHEMBL1643120

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O=C(Nc1ccccc1)c1coc2ccccc2c1=O

Basic Information

ChEMBL ID CHEMBL1643120
Phase Preclinical
Structure Type MOL
InChI Key NVUUCSMDDBUOOH-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

265.3
MW (Da)
3.05
ALogP
3
HBA
1
HBD
59.3
PSA (Ų)
0.77
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H11NO3
MW 265.27
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.68

Activity Summary

IC50 3 meas. best 7.15
Ki 1 meas. best 5.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amine oxidase [flavin-containing] B
CHEMBL2039
IC50 7.15 6.65 70.7 3
Adenosine receptor A2b
CHEMBL255
Ki 5.07 5.07 8510.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22703703 10.1016/j.ejmech.2012.05.033 Adenosine receptor A2b 2
21194943 10.1016/j.bmcl.2010.11.128 Amine oxidase [flavin-containing] B 1
21194943 10.1016/j.bmcl.2010.11.128 Amine oxidase [flavin-containing] A 1
21194943 10.1016/j.bmcl.2010.11.128 Unchecked 1
21696156 10.1021/jm2004267 Amine oxidase [flavin-containing] B 1
21696156 10.1021/jm2004267 Unchecked 1
21696156 10.1021/jm2004267 Amine oxidase [flavin-containing] A 1
22703703 10.1016/j.ejmech.2012.05.033 Adenosine receptor A1 1
22703703 10.1016/j.ejmech.2012.05.033 Adenosine receptor A2a 1
22703703 10.1016/j.ejmech.2012.05.033 Unchecked 1
27244485 10.1021/acs.jmedchem.6b00527 Amine oxidase [flavin-containing] B 1
27244485 10.1021/acs.jmedchem.6b00527 Amine oxidase [flavin-containing] A 1
27244485 10.1021/acs.jmedchem.6b00527 Unchecked 1

Data from ChEMBL 36 via Core Engine