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Compound Detail

CHEMBL5439235

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COC(=O)/C(C#N)=C/c1cn(CC(=O)Nc2ccc(Br)cn2)c2ccccc12

Basic Information

ChEMBL ID CHEMBL5439235
Phase Preclinical
Structure Type MOL
InChI Key UZDACVNULBHFBS-MDWZMJQESA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

439.3
MW (Da)
3.52
ALogP
6
HBA
1
HBD
97.0
PSA (Ų)
0.37
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15BrN4O3
MW 439.27
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.86

Activity Summary

IC50 3 meas. best 6.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Monocarboxylate transporter 1
CHEMBL4360
IC50 6.67 6.67 214.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 5.92 5.885 1190.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36584238 10.1021/acs.jmedchem.2c01612 ATP-dependent translocase ABCB1 4
36584238 10.1021/acs.jmedchem.2c01612 Monocarboxylate transporter 1 1
36584238 10.1021/acs.jmedchem.2c01612 Monocarboxylate transporter 4 1
36584238 10.1021/acs.jmedchem.2c01612 A549 1
36584238 10.1021/acs.jmedchem.2c01612 MCF7 1
36584238 10.1021/acs.jmedchem.2c01612 NIH3T3 1

Data from ChEMBL 36 via Core Engine