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Compound Detail

CHEMBL485756

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NCc1cccc(COc2nc(N)nc3nc[nH]c23)c1

Basic Information

ChEMBL ID CHEMBL485756
Phase Preclinical
Structure Type MOL
InChI Key VHRDYCCJQBXLBG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

270.3
MW (Da)
0.97
ALogP
6
HBA
3
HBD
115.7
PSA (Ų)
0.65
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H14N6O
MW 270.30
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.67

Activity Summary

IC50 1 meas. best 8.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Methylated-DNA--protein-cysteine methyltransferase
CHEMBL2864
IC50 8.05 8.05 9.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18973327 10.1021/jm800675p Methylated-DNA--protein-cysteine methyltransferase 5
34731767 10.1016/j.ejmech.2021.113909 T98G 4
22932317 10.1016/j.bmcl.2012.08.008 Methylated-DNA--protein-cysteine methyltransferase 3
27041398 10.1016/j.bmc.2016.03.041 No relevant target 3
27041398 10.1016/j.bmc.2016.03.041 NON-PROTEIN TARGET 3
22932317 10.1016/j.bmcl.2012.08.008 EMT6 2
22932317 10.1016/j.bmcl.2012.08.008 No relevant target 2
34731767 10.1016/j.ejmech.2021.113909 Methylated-DNA--protein-cysteine methyltransferase 1

Data from ChEMBL 36 via Core Engine