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Compound Detail

CHEMBL4161145

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COc1cc2c(cc1-c1c(C)noc1C)[nH]c1nc(C)nc(Nc3c4c(nn3C)CCCC4)c12

Basic Information

ChEMBL ID CHEMBL4161145
Phase Preclinical
Structure Type MOL
InChI Key BUKRITMNZGTIOZ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
5.06
ALogP
8
HBA
2
HBD
106.7
PSA (Ų)
0.39
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27N7O2
MW 457.54
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.03

Activity Summary

IC50 3 meas. best 8.31

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bromodomain-containing protein 4
CHEMBL1163125
IC50 8.31 8.31 4.9 1
MOLM-13
CHEMBL3706572
IC50 7.95 7.95 11.3 1
MDA-MB-231
CHEMBL400
IC50 7.76 7.76 17.5 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30015487 10.1021/acs.jmedchem.8b00483 ADMET 4
30015487 10.1021/acs.jmedchem.8b00483 Bromodomain-containing protein 4 2
30015487 10.1021/acs.jmedchem.8b00483 MOLM-13 1
30015487 10.1021/acs.jmedchem.8b00483 MDA-MB-231 1

Data from ChEMBL 36 via Core Engine