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Assay Detail

CHEMBL4381893

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human leukocyte elastase assessed as reduction in pNA release using chromogenic MeO-Suc-Ala-Ala-Pro-Val-pNA substrate measured over 10 mins by spectrophotometry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
Scheeff S, Rivière S, Ruiz J, Abdelrahman A, Schulz-Fincke AC, Köse M, Tiburcy F, Wieczorek H, Gütschow M, Müller CE, Menche D.
J Med Chem (2020) 63 : 1684 -1698
PubMed 31990540 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.01 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411767 ARCHAZOLID B 1 6.50
CHEMBL241106 ARCHAZOLID A 1 6.45
CHEMBL4460252 1 6.22
CHEMBL4593430 1 6.14
CHEMBL1784269 ARCHAZOLID F 1 6.08
CHEMBL4447903 1 5.81
CHEMBL4549217 1 5.63
CHEMBL4471610 1 5.23
CHEMBL290814 BAFILOMYCIN A1 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411767 ARCHAZOLID B IC50 = 316.0 nM 6.50
CHEMBL241106 ARCHAZOLID A IC50 = 352.0 nM 6.45
CHEMBL4460252 IC50 = 595.0 nM 6.22
CHEMBL4593430 IC50 = 721.0 nM 6.14
CHEMBL1784269 ARCHAZOLID F IC50 = 830.0 nM 6.08
CHEMBL4447903 IC50 = 1540.0 nM 5.81
CHEMBL4549217 IC50 = 2340.0 nM 5.63
CHEMBL4471610 IC50 = 5850.0 nM 5.23
CHEMBL290814 BAFILOMYCIN A1 IC50 - -