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Compound Detail

CHEMBL2381126

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Brc1cccc(/C=C/c2nnc(-c3ccc4c(c3)OCCO4)o2)c1

Basic Information

ChEMBL ID CHEMBL2381126
Phase Preclinical
Structure Type MOL
InChI Key FXYKNQQGXRTHKG-QPJJXVBHSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

385.2
MW (Da)
4.44
ALogP
5
HBA
0
HBD
57.4
PSA (Ų)
0.67
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 C18H13BrN2O3
MW 385.22
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.81

Activity Summary

IC50 2 meas. best 4.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Methionine aminopeptidase 2
CHEMBL3922
IC50 4.97 4.97 10710.0 1
HUVEC
CHEMBL613979
IC50 4.87 4.87 13530.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Methionine aminopeptidase 2 IC50 = 10710.0 nM 4.97 Inhibition of MetAP2 (unknown origin) after 4 hrs 23582273
HUVEC IC50 = 13530.0 nM 4.87 Antiproliferative against HUVEC after 48 hrs by MTT assay 23582273

Literature References

PubMed DOI Target Context # Activities
23582273 10.1016/j.bmcl.2013.03.068 HUVEC 2
23582273 10.1016/j.bmcl.2013.03.068 Methionine aminopeptidase 2 1

Data from ChEMBL 36 via Core Engine