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Compound Detail

CHEMBL3092490

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COc1ccc(-c2nc(Nc3cccc(O)c3)c3ccccc3n2)cc1OC

Basic Information

ChEMBL ID CHEMBL3092490
Phase Preclinical
Structure Type MOL
InChI Key AJAJIMATEVMQTD-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

373.4
MW (Da)
4.76
ALogP
6
HBA
2
HBD
76.5
PSA (Ų)
0.53
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 C22H19N3O3
MW 373.41
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.91

Activity Summary

IC50 3 meas. best 6.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 6.96 6.905 110.0 2
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 4.74 4.74 18210.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24184213 10.1016/j.bmc.2013.10.007 Multidrug resistance-associated protein 1 2
24184213 10.1016/j.bmc.2013.10.007 ATP-dependent translocase ABCB1 2
24184213 10.1016/j.bmc.2013.10.007 Broad substrate specificity ATP-binding cassette transporter ABCG2 2
24184213 10.1016/j.bmc.2013.10.007 ADMET 1
24184213 10.1016/j.bmc.2013.10.007 MDCK 1

Data from ChEMBL 36 via Core Engine