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Compound Detail

CHEMBL474757

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COc1cc2c(cc1OC)CN(CCc1ccc(NC(=O)Nc3ccc(N)cc3)cc1)CC2

Basic Information

ChEMBL ID CHEMBL474757
Phase Preclinical
Structure Type MOL
InChI Key GGQMUXQOMIDATF-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

446.6
MW (Da)
4.53
ALogP
5
HBA
3
HBD
88.8
PSA (Ų)
0.46
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H30N4O3
MW 446.55
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.79

Activity Summary

IC50 3 meas. best 4.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 4.51 4.51 31000.0 1
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 4.33 4.23 46400.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19932960 10.1016/j.bmcl.2009.11.004 Broad substrate specificity ATP-binding cassette transporter ABCG2 2
19250834 10.1016/j.bmc.2009.01.072 ATP-dependent translocase ABCB1 1

Data from ChEMBL 36 via Core Engine