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Compound Detail

CHEMBL362200

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O=C(Cc1c(-c2ccc(Cl)cc2)nc2c(Cl)cc(Cl)cn12)NCc1ccccc1

Basic Information

ChEMBL ID CHEMBL362200
Phase Preclinical
Structure Type MOL
InChI Key JRZIGYIBOCKYJT-UHFFFAOYSA-N
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

444.8
MW (Da)
5.82
ALogP
3
HBA
1
HBD
46.4
PSA (Ų)
0.42
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H16Cl3N3O
MW 444.75
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.58

Activity Summary

IC50 2 meas. best 6.77
Ki 2 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Translocator protein
CHEMBL4552
Ki 7.0 7.0 98.8 1
Translocator protein
CHEMBL4552
IC50 6.77 6.77 169.0 1
GABA-A receptor; anion channel
CHEMBL1907607
Ki 5.15 5.15 7010.0 1
GABA-A receptor; anion channel
CHEMBL1907607
IC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15634024 10.1021/jm049610q Translocator protein 4
15634024 10.1021/jm049610q GABA-A receptor; anion channel 2
15634024 10.1021/jm049610q Benzodiazepine receptors; peripheral & central 2

Data from ChEMBL 36 via Core Engine