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Compound Detail

CHEMBL142750

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O=C1CCC2c3c(-c4noc(C5CC5)n4)ncn3-c3ccccc3N12

Basic Information

ChEMBL ID CHEMBL142750
Phase Preclinical
Structure Type MOL
InChI Key KIGZWNHARYMTNM-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

333.4
MW (Da)
2.98
ALogP
6
HBA
0
HBD
77.0
PSA (Ų)
0.72
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 C18H15N5O2
MW 333.35
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.24

Activity Summary

Ki 3 meas. best 9.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
GABA-A receptor; anion channel
CHEMBL1907607
Ki 9.06 9.06 0.9 2
GABA A receptor alpha-6/beta-2/gamma-2
CHEMBL2111365
Ki 7.88 7.88 13.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8917654 10.1021/jm960401i GABA-A receptor; anion channel 2
8145225 10.1021/jm00032a008 GABA-A receptor; anion channel 2
8917654 10.1021/jm960401i GABA-A receptor; alpha-1/beta-2/gamma-2 1
8917654 10.1021/jm960401i Rattus norvegicus 1
8917654 10.1021/jm960401i GABA A receptor alpha-6/beta-2/gamma-2 1
8145225 10.1021/jm00032a008 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine