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Compound Detail

CHEMBL142100

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COc1cc(C(C)C)c2c(c1)S(=O)(=O)N(COC1=C(Cc3ccccc3)C(=O)OC1)C2=O

Basic Information

ChEMBL ID CHEMBL142100
Phase Preclinical
Structure Type MOL
InChI Key PQLKMBLZCLXMTN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
2.99
ALogP
7
HBA
0
HBD
99.2
PSA (Ų)
0.59
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23NO7S
MW 457.50
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.02

Activity Summary

Ki 1 meas. best 10.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neutrophil elastase
CHEMBL248
Ki 10.89 10.89 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.9667 hr Homo sapiens
T1/2 1.25 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neutrophil elastase Ki = 0.013 nM 10.89 Potency of inhibition of human leukocyte elastase is expressed as apparent bindi... 7473596

Literature References

PubMed DOI Target Context # Activities
7473596 10.1021/jm00023a008 Homo sapiens 2
7473596 10.1021/jm00023a008 Neutrophil elastase 1

Data from ChEMBL 36 via Core Engine