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Compound Detail

CHEMBL3785910

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CNc1nc2ccccc2n2c(Br)cnc12

Basic Information

ChEMBL ID CHEMBL3785910
Phase Preclinical
Structure Type MOL
InChI Key OPNSZLLOUYDIGN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

277.1
MW (Da)
2.69
ALogP
4
HBA
1
HBD
42.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H9BrN4
MW 277.12
Aromatic Rings 3
Heavy Atoms 16
NP-Likeness -1.26

Activity Summary

IC50 1 meas. best 5.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
A-375
CHEMBL613859
IC50 5.63 5.63 2354.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
A-375 IC50 = 2354.0 nM 5.63 Antiproliferative activity against human A-375 cells assessed as reduction in ce... 33309473

Literature References

PubMed DOI Target Context # Activities
27017554 10.1016/j.ejmech.2016.03.006 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
27017554 10.1016/j.ejmech.2016.03.006 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
28750313 10.1016/j.ejmech.2017.07.021 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
28750313 10.1016/j.ejmech.2017.07.021 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
33309473 10.1016/j.ejmech.2020.113031 A-375 1

Data from ChEMBL 36 via Core Engine