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Compound Detail

CHEMBL4542665

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Cc1c(N2CCN(C)CC2)ccc2c3c(c(=O)oc12)CN(C(=O)c1ccc(NS(C)(=O)=O)c(Br)c1)CC3

Basic Information

ChEMBL ID CHEMBL4542665
Phase Preclinical
Structure Type MOL
InChI Key QJDXVNDMZAZDDR-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

589.5
MW (Da)
3.19
ALogP
7
HBA
1
HBD
103.2
PSA (Ų)
0.47
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29BrN4O5S
MW 589.51
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.32

Activity Summary

IC50 2 meas. best 7.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bifunctional methylenetetrahydrofolate dehydrogenase/cyclohydrolase, mitochondrial
CHEMBL3621036
IC50 7.48 7.48 33.0 1
C-1-tetrahydrofolate synthase, cytoplasmic
CHEMBL2541
IC50 5.38 5.38 4200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31638799 10.1021/acs.jmedchem.9b01113 No relevant target 3
31638799 10.1021/acs.jmedchem.9b01113 Unchecked 2
31638799 10.1021/acs.jmedchem.9b01113 Bifunctional methylenetetrahydrofolate dehydrogenase/cyclohydrolase, mitochondrial 1
31638799 10.1021/acs.jmedchem.9b01113 C-1-tetrahydrofolate synthase, cytoplasmic 1

Data from ChEMBL 36 via Core Engine