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Compound Detail

CHEMBL1735482

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NC1=C(Br)C(=O)c2ncccc2C1=O

Basic Information

ChEMBL ID CHEMBL1735482
Phase Preclinical
Structure Type MOL
InChI Key XZBBOHUCBTXJQY-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

253.1
MW (Da)
1.03
ALogP
4
HBA
1
HBD
73.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H5BrN2O2
MW 253.06
Aromatic Rings 1
Heavy Atoms 14
NP-Likeness 0.13

Activity Summary

IC50 5 meas. best 6.36
EC50 1 meas. best 4.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.36 6.16 435.2 2
Tyrosyl-DNA phosphodiesterase 2
CHEMBL2169736
IC50 5.58 5.58 2661.0 1
Hexokinase HKDC1
CHEMBL1741200
IC50 5.05 4.955 8910.0 2
Protein S100-A4
CHEMBL2362976
EC50 4.8 4.8 16000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27663546 10.1016/j.bmc.2016.09.028 Matrix protein P17 2
27663546 10.1016/j.bmc.2016.09.028 No relevant target 1
27663546 10.1016/j.bmc.2016.09.028 HEK-293T 1
27663546 10.1016/j.bmc.2016.09.028 MT4 1
27663546 10.1016/j.bmc.2016.09.028 CEM-SS 1
30562026 10.1021/acs.jmedchem.8b01720 Cystathionine gamma-lyase 1

Data from ChEMBL 36 via Core Engine