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Compound Detail

CHEMBL1277933

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Cn1c(COCc2ccccc2Cl)c2c(=O)n(-c3ccccc3Cl)[nH]c2cc1=O

Basic Information

ChEMBL ID CHEMBL1277933
Phase Preclinical
Structure Type MOL
InChI Key TZPRBPWSPHMJIH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

430.3
MW (Da)
4.04
ALogP
5
HBA
1
HBD
69.0
PSA (Ų)
0.52
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17Cl2N3O3
MW 430.29
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.89

Activity Summary

Ki 1 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NADPH oxidase 4
CHEMBL1250375
Ki 7.09 7.09 82.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 210.0 mL.min-1.g-1 Rattus norvegicus
CL 212.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NADPH oxidase 4 Ki = 82.0 nM 7.09 Inhibition of human NOX4 overexpressed in human PMN cell membrane assessed as RO... 20942471

Literature References

PubMed DOI Target Context # Activities
20942471 10.1021/jm100773e Liver microsomes 2
20942471 10.1021/jm100773e NADPH oxidase 4 1
20942471 10.1021/jm100773e Caco-2 1

Data from ChEMBL 36 via Core Engine