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Compound Detail

CHEMBL200115

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c1ccc(Cn2c(-c3cscn3)nc3ccccc32)cc1

Basic Information

ChEMBL ID CHEMBL200115
Phase Preclinical
Structure Type MOL
InChI Key RWZYJIHLVDIUBB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

291.4
MW (Da)
4.21
ALogP
4
HBA
0
HBD
30.7
PSA (Ų)
0.57
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 C17H13N3S
MW 291.38
Aromatic Rings 4
Heavy Atoms 21
NP-Likeness -1.69

Activity Summary

IC50 2 meas. best 6.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Methionine aminopeptidase
CHEMBL3423
IC50 6.34 6.34 461.0 1
Unchecked
CHEMBL612545
IC50 6.34 6.34 460.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Methionine aminopeptidase IC50 = 461.0 nM 6.34 Inhibition of Co2+ loaded MetAP expressed in Escherichia coli 16420038
Unchecked IC50 = 460.0 nM 6.34 Inhibition of Escherichia coli MetAP 20621724

Literature References

PubMed DOI Target Context # Activities
16420038 10.1021/jm050476z Methionine aminopeptidase 2
20621724 10.1016/j.bmcl.2010.05.093 Unchecked 2
25936258 10.1016/j.bmc.2015.03.085 HUVEC 2
20621724 10.1016/j.bmcl.2010.05.093 Methionine aminopeptidase 1 1
20621724 10.1016/j.bmcl.2010.05.093 Methionine aminopeptidase 2 1

Data from ChEMBL 36 via Core Engine