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Compound Detail

CHEMBL2335007

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COc1cc2c(cc1OC)CN(Cc1ccc(Oc3ccc(-c4nc(-c5cccc(O)c5)cs4)cn3)cc1)CC2

Basic Information

ChEMBL ID CHEMBL2335007
Phase Preclinical
Structure Type MOL
InChI Key RBWQOGHTXCLCOW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

551.7
MW (Da)
6.95
ALogP
8
HBA
1
HBD
76.9
PSA (Ų)
0.22
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H29N3O4S
MW 551.67
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -1.14

Activity Summary

EC50 2 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
EC50 7.75 7.75 18.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
EC50 6.6 6.6 250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23374872 10.1016/j.bmcl.2012.12.084 ATP-dependent translocase ABCB1 3
23374872 10.1016/j.bmcl.2012.12.084 Caco-2 1
23374872 10.1016/j.bmcl.2012.12.084 Multidrug resistance-associated protein 1 1
23374872 10.1016/j.bmcl.2012.12.084 Broad substrate specificity ATP-binding cassette transporter ABCG2 1

Data from ChEMBL 36 via Core Engine