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Compound Detail

CHEMBL192554

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COc1ccc(-c2nn3c(=O)[nH]c4ccccc4n3c2=O)cc1

Basic Information

ChEMBL ID CHEMBL192554
Phase Preclinical
Structure Type MOL
InChI Key PKJGSRHYDOGGLB-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

308.3
MW (Da)
1.31
ALogP
6
HBA
1
HBD
80.9
PSA (Ų)
0.61
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 C16H12N4O3
MW 308.30
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -0.72

Activity Summary

Ki 6 meas. best 8.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; alpha-1/beta-2/gamma-2
CHEMBL2095167
Ki 8.43 8.43 3.8 1
GABA-A receptor; anion channel
CHEMBL2093872
Ki 7.96 7.96 11.0 1
GABA A receptor alpha-2/beta-2/gamma-2
CHEMBL2111327
Ki 7.84 7.84 14.3 1
GABA A receptor alpha-5/beta-3/gamma-2
CHEMBL2111374
Ki 7.76 7.76 17.2 1
Adenosine receptor A3
CHEMBL256
Ki 7.3 7.3 49.8 1
Adenosine receptor A1
CHEMBL226
Ki 5.97 5.97 1070.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15828832 10.1021/jm0408722 GABA-A receptor; anion channel 1
15828832 10.1021/jm0408722 GABA-A receptor; alpha-1/beta-2/gamma-2 1
15828832 10.1021/jm0408722 GABA A receptor alpha-2/beta-2/gamma-2 1
15828832 10.1021/jm0408722 GABA A receptor alpha-5/beta-3/gamma-2 1
17927167 10.1021/jm0708376 Adenosine receptor A1 1
17927167 10.1021/jm0708376 Adenosine receptor A2a 1
17927167 10.1021/jm0708376 Adenosine receptor A3 1

Data from ChEMBL 36 via Core Engine