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Compound Detail

CHEMBL3183219

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Nc1[nH]c(C(=O)c2ccc(Br)cc2)c(-c2ccccn2)c1C(=O)NCCc1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL3183219
Phase Preclinical
Structure Type MOL
InChI Key WOPLFGSURRTEMY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

528.4
MW (Da)
5.11
ALogP
4
HBA
4
HBD
116.7
PSA (Ų)
0.22
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H22BrN5O2
MW 528.41
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -0.72

Activity Summary

IC50 1 meas. best 4.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 4.79 4.79 16374.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 16374.0 nM 4.79 PubChem BioAssay. Counterscreen for exosite inhibitors of ADAM17: Fluorescence r... -

Literature References

PubMed DOI Target Context # Activities
28843180 10.1016/j.ejmech.2017.07.047 Polyunsaturated fatty acid lipoxygenase ALOX15 1

Data from ChEMBL 36 via Core Engine