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Compound Detail

CHEMBL3884587

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COc1ccc(-n2nnc(-c3ccccc3NC(=O)c3ccc(C(F)(F)F)cc3)n2)cc1OC

Basic Information

ChEMBL ID CHEMBL3884587
Phase Preclinical
Structure Type MOL
InChI Key RNQGKQSSCCGNPY-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

469.4
MW (Da)
4.62
ALogP
7
HBA
1
HBD
91.2
PSA (Ų)
0.44
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H18F3N5O3
MW 469.42
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.65

Activity Summary

IC50 2 meas. best 6.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 6.48 6.48 330.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 4.99 4.99 10200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27676469 10.1016/j.ejmech.2016.09.010 Broad substrate specificity ATP-binding cassette transporter ABCG2 3
27676469 10.1016/j.ejmech.2016.09.010 ATP-dependent translocase ABCB1 2

Data from ChEMBL 36 via Core Engine