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Compound Detail

CHEMBL5405329

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COC(=O)/C(C#N)=C/c1cn(CC(=O)Nc2cccc(OC)c2)c2ccccc12

Basic Information

ChEMBL ID CHEMBL5405329
Phase Preclinical
Structure Type MOL
InChI Key GOQXHMPUSQNADT-XNTDXEJSSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

389.4
MW (Da)
3.37
ALogP
6
HBA
1
HBD
93.3
PSA (Ų)
0.40
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19N3O4
MW 389.41
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.68

Activity Summary

IC50 4 meas. best 6.98

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Monocarboxylate transporter 1
CHEMBL4360
IC50 6.98 6.98 105.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 5.27 5.27 5320.0 1
Multidrug resistance-associated protein 1
CHEMBL3004
IC50 4.72 4.72 19100.0 1
Unchecked
CHEMBL612545
IC50 4.36 4.36 43500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
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
36584238 10.1021/acs.jmedchem.2c01612 ATP-dependent translocase ABCB1 1
36584238 10.1021/acs.jmedchem.2c01612 Multidrug resistance-associated protein 1 1
36584238 10.1021/acs.jmedchem.2c01612 Unchecked 1

Data from ChEMBL 36 via Core Engine