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Compound Detail

CHEMBL4060914

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Oc1cccc(Nc2nc(-c3cccnc3)nc3ncccc23)c1

Basic Information

ChEMBL ID CHEMBL4060914
Phase Preclinical
Structure Type MOL
InChI Key RGRNSYKOFJZXDA-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

315.3
MW (Da)
3.54
ALogP
6
HBA
2
HBD
83.8
PSA (Ų)
0.60
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H13N5O
MW 315.34
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.19

Activity Summary

EC50 1 meas. best 7.8
IC50 1 meas. best 4.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
EC50 7.8 7.8 16.0 1
Broad substrate specificity ATP-binding cassette transporter ABCG2
CHEMBL5393
IC50 4.77 4.77 16900.0 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