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Compound Detail

CHEMBL2152098

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C=CC(=O)NC1CCN(S(=O)(=O)c2ccc(C(=O)NCCc3ccccc3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL2152098
Phase Preclinical
Structure Type MOL
InChI Key WZJJPWFLFPNPFQ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

441.6
MW (Da)
2.11
ALogP
4
HBA
2
HBD
95.6
PSA (Ų)
0.61
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N3O4S
MW 441.55
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.31

Activity Summary

IC50 1 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein-glutamine gamma-glutamyltransferase
CHEMBL2730
IC50 6.75 6.75 180.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 99.0 mL.min-1.g-1 Mus musculus
CL 595.0 mL.min-1.g-1 Homo sapiens
T1/2 6.0 hr Mus musculus
T1/2 6.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein-glutamine gamma-glutamyltransferase IC50 = 180.0 nM 6.75 Inhibition of human TGM2 24900540

Literature References

PubMed DOI Target Context # Activities
24900540 10.1021/ml3001352 Plasma 2
24900540 10.1021/ml3001352 MDCK 2
24900540 10.1021/ml3001352 Protein-glutamine gamma-glutamyltransferase 1
24900540 10.1021/ml3001352 No relevant target 1
24900540 10.1021/ml3001352 Liver 1
24900540 10.1021/ml3001352 Liver microsomes 1

Data from ChEMBL 36 via Core Engine