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Compound Detail

CHEMBL1277767

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COc1cccc(N2CCN(Cc3c4c(=O)n(-c5ccccc5Cl)[nH]c4cc(=O)n3C)CC2)c1

Basic Information

ChEMBL ID CHEMBL1277767
Phase Preclinical
Structure Type MOL
InChI Key PHGJTVIQXZDFDQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

480.0
MW (Da)
3.00
ALogP
7
HBA
1
HBD
75.5
PSA (Ų)
0.48
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 C25H26ClN5O3
MW 479.97
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.31

Activity Summary

Ki 1 meas. best 7.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NADPH oxidase 4
CHEMBL1250375
Ki 7.19 7.19 65.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 121.0 mL.min-1.g-1 Rattus norvegicus
CL 57.9 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 = 65.0 nM 7.19 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

Data from ChEMBL 36 via Core Engine