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Compound Detail

CHEMBL454606

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CCOC(=O)c1cc2c(cn1)[nH]c1ccccc12

Basic Information

ChEMBL ID CHEMBL454606
Phase Preclinical
Structure Type MOL
InChI Key KOVRZNUMIKACTB-UHFFFAOYSA-N
9
Targets
9
Activities
2
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

240.3
MW (Da)
2.89
ALogP
3
HBA
1
HBD
55.0
PSA (Ų)
0.70
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C14H12N2O2
MW 240.26
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -0.26

Activity Summary

Ki 6 meas. best 9.0
IC50 3 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Gamma-aminobutyric acid receptor subunit alpha-1
CHEMBL1962
Ki 9.0 9.0 1.0 1
GABA-A receptor; anion channel
CHEMBL2093872
IC50 9.0 9.0 1.0 1
Gamma-aminobutyric acid receptor subunit alpha-2
CHEMBL4956
Ki 8.3 8.3 5.0 1
Unchecked
CHEMBL612545
IC50 8.3 8.3 5.0 1
Gamma-aminobutyric acid receptor subunit alpha-3
CHEMBL3026
Ki 8.22 8.22 6.0 1
Gamma-aminobutyric acid receptor subunit alpha-5
CHEMBL5112
Ki 7.57 7.57 27.0 1
cGMP-specific 3',5'-cyclic phosphodiesterase
CHEMBL1827
IC50 6.1 6.1 794.3 1
Gamma-aminobutyric acid receptor subunit alpha-4
CHEMBL2472
Ki 6.0 6.0 1000.0 1
Gamma-aminobutyric acid receptor subunit alpha-6
CHEMBL2579
Ki 5.57 5.57 2700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26235951 10.1016/j.bmcl.2015.07.058 NON-PROTEIN TARGET 3
- 10.1007/s00044-008-9111-6 Unchecked 1
26235951 10.1016/j.bmcl.2015.07.058 HL-60 1
26235951 10.1016/j.bmcl.2015.07.058 A498 1
26235951 10.1016/j.bmcl.2015.07.058 COLO 205 1
26235951 10.1016/j.bmcl.2015.07.058 SK-OV-3 1
26235951 10.1016/j.bmcl.2015.07.058 Detroit 551 1
26982523 10.1021/acs.jmedchem.6b00034 Unchecked 1
29620890 10.1021/acs.jmedchem.8b00180 cGMP-specific 3',5'-cyclic phosphodiesterase 1
33528252 10.1021/acs.jmedchem.0c01887 GABA-A receptor; anion channel 1
33528252 10.1021/acs.jmedchem.0c01887 Gamma-aminobutyric acid receptor subunit alpha-1 1
33528252 10.1021/acs.jmedchem.0c01887 Gamma-aminobutyric acid receptor subunit alpha-2 1
33528252 10.1021/acs.jmedchem.0c01887 Gamma-aminobutyric acid receptor subunit alpha-3 1
33528252 10.1021/acs.jmedchem.0c01887 Gamma-aminobutyric acid receptor subunit alpha-4 1
33528252 10.1021/acs.jmedchem.0c01887 Gamma-aminobutyric acid receptor subunit alpha-5 1
33528252 10.1021/acs.jmedchem.0c01887 Gamma-aminobutyric acid receptor subunit alpha-6 1

Data from ChEMBL 36 via Core Engine