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Compound Detail

CHEMBL2335006

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COc1cccc(-c2csc(-c3ccc(Oc4ccc(CN5CCc6cc(OC)c(OC)cc6C5)cc4)nc3)n2)c1

Basic Information

ChEMBL ID CHEMBL2335006
Phase Preclinical
Structure Type MOL
InChI Key XTIXUZDDNPXVTI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

565.7
MW (Da)
7.25
ALogP
8
HBA
0
HBD
65.9
PSA (Ų)
0.19
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H31N3O4S
MW 565.70
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -1.33

Activity Summary

EC50 2 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
EC50 6.3 6.3 500.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
EC50 6.02 6.02 950.0 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