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Compound Detail

CHEMBL4095392

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COc1cccc(-n2nnc(-c3ccccc3NC(=O)c3ccc(N)cc3)n2)c1

Basic Information

ChEMBL ID CHEMBL4095392
Phase Preclinical
Structure Type MOL
InChI Key JUSMKRLXJZILHS-UHFFFAOYSA-N
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

386.4
MW (Da)
3.17
ALogP
7
HBA
2
HBD
108.0
PSA (Ų)
0.51
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18N6O2
MW 386.42
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.71

Activity Summary

IC50 6 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H460
CHEMBL396
IC50 6.68 6.67 211.0 3
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 6.52 6.3633 299.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28916341 10.1016/j.bmcl.2017.09.009 Broad substrate specificity ATP-binding cassette transporter ABCG2 5
28916341 10.1016/j.bmcl.2017.09.009 Unchecked 4
28916341 10.1016/j.bmcl.2017.09.009 NCI-H460 4

Data from ChEMBL 36 via Core Engine