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Compound Detail

CHEMBL3972677

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COc1ccc2[nH]c3c(C(=O)NCCN)c4ccncc4c(C)c3c2c1

Basic Information

ChEMBL ID CHEMBL3972677
Phase Preclinical
Structure Type MOL
InChI Key FOROPWCELHCZJL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

348.4
MW (Da)
2.87
ALogP
4
HBA
3
HBD
93.0
PSA (Ų)
0.53
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 C20H20N4O2
MW 348.41
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -0.19

Activity Summary

IC50 1 meas. best 5.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.98 5.98 1040.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ka 3.88 10'5/M -
Ka 20.5 10'5/M -
Ka 25.1 10'5/M -
Ka 3.2 10'5/M -
Ka 20.5 10'5/M -
Ka 7.41 10'5/M -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET IC50 = 1040.0 nM 5.98 Cytotoxicity against human HeLaS3 cells assessed as reduction in cell viability ... 28063783

Literature References

PubMed DOI Target Context # Activities
28063783 10.1016/j.bmc.2016.12.031 Unchecked 9
28063783 10.1016/j.bmc.2016.12.031 NON-PROTEIN TARGET 2
28063783 10.1016/j.bmc.2016.12.031 Mus musculus 1

Data from ChEMBL 36 via Core Engine