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Compound Detail

CHEMBL3617836

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O=[N+]([O-])c1cccc(-c2cn(-c3cccc(I)c3)nn2)c1

Basic Information

ChEMBL ID CHEMBL3617836
Phase Preclinical
Structure Type MOL
InChI Key LSVWEYNSNZJEGB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

392.2
MW (Da)
3.45
ALogP
5
HBA
0
HBD
73.8
PSA (Ų)
0.39
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H9IN4O2
MW 392.16
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -2.45

Activity Summary

EC50 1 meas. best 5.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Keap1/Nrf2
CHEMBL3038498
EC50 5.15 5.15 7100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Keap1/Nrf2 EC50 = 7100.0 nM 5.15 Inhibition of kelch domain of Keap1 (unknown origin) interaction to high affinit... 26348784

Literature References

PubMed DOI Target Context # Activities
31411465 10.1021/acs.jmedchem.9b00723 Kelch-like ECH-associated protein 1 6
26348784 10.1021/acs.jmedchem.5b00602 Keap1/Nrf2 5
26348784 10.1021/acs.jmedchem.5b00602 Nuclear factor erythroid 2-related factor 2 4
26348784 10.1021/acs.jmedchem.5b00602 Unchecked 3
26348784 10.1021/acs.jmedchem.5b00602 ADMET 2
31411465 10.1021/acs.jmedchem.9b00723 No relevant target 2
26348784 10.1021/acs.jmedchem.5b00602 Kelch-like ECH-associated protein 1 1

Data from ChEMBL 36 via Core Engine