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Compound Detail

CHEMBL4792783

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N#Cc1ccc(Nc2cc(NCCCc3ccccc3)nc(-c3ccccc3)n2)cc1

Basic Information

ChEMBL ID CHEMBL4792783
Phase Preclinical
Structure Type MOL
InChI Key FQZCMALWZKOTSE-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

405.5
MW (Da)
5.80
ALogP
5
HBA
2
HBD
73.6
PSA (Ų)
0.36
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23N5
MW 405.51
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.34

Activity Summary

EC50 1 meas. best 7.17
IC50 1 meas. best 7.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
EC50 7.17 7.17 67.0 1
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 7.02 7.02 96.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33454462 10.1016/j.ejmech.2020.113045 Broad substrate specificity ATP-binding cassette transporter ABCG2 6
33454462 10.1016/j.ejmech.2020.113045 ATP-dependent translocase ABCB1 2
33454462 10.1016/j.ejmech.2020.113045 Multidrug resistance-associated protein 1 2
33454462 10.1016/j.ejmech.2020.113045 MDCK-II 2
33454462 10.1016/j.ejmech.2020.113045 ADMET 1

Data from ChEMBL 36 via Core Engine