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Compound Detail

CHEMBL4202725

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O=C(Nc1ccccc1-n1cc(-c2ccccc2)nn1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL4202725
Phase Preclinical
Structure Type MOL
InChI Key PWPQYHFUVPQSBU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
4.19
ALogP
4
HBA
1
HBD
59.8
PSA (Ų)
0.61
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 C21H16N4O
MW 340.39
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.67

Activity Summary

IC50 2 meas. best 4.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 4.82 4.82 15300.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 4.67 4.67 21200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29407974 10.1016/j.ejmech.2018.01.012 Broad substrate specificity ATP-binding cassette transporter ABCG2 6
29407974 10.1016/j.ejmech.2018.01.012 Unchecked 4
29407974 10.1016/j.ejmech.2018.01.012 MDCK-II 2
29407974 10.1016/j.ejmech.2018.01.012 ATP-dependent translocase ABCB1 1
29407974 10.1016/j.ejmech.2018.01.012 ADMET 1

Data from ChEMBL 36 via Core Engine