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Compound Detail

CHEMBL4081623

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COc1ccc(Nc2nc(-c3ccccc3)nc3ncccc23)cc1OC

Basic Information

ChEMBL ID CHEMBL4081623
Phase Preclinical
Structure Type MOL
InChI Key CGZOIAGYXKVWFL-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

358.4
MW (Da)
4.45
ALogP
6
HBA
1
HBD
69.2
PSA (Ų)
0.57
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 C21H18N4O2
MW 358.40
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.18

Activity Summary

EC50 1 meas. best 8.1
IC50 1 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
EC50 8.1 8.1 8.0 1
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 6.46 6.46 343.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29547272 10.1021/acs.jmedchem.7b01012 Broad substrate specificity ATP-binding cassette transporter ABCG2 3

Data from ChEMBL 36 via Core Engine