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Assay Detail

CHEMBL2176198

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

Binding
Inhibition of human recombinant Myc-His10-tagged cathepsin A expressed in baculovirus infected Sf9 cells using BodipyFL labeled bradykinin as substrate incubated for 15 mins prior to substrate addition measured after 15 mins by fluorimetric analysis
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysosomal protective protein (CHEMBL6115)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel β-amino acid derivatives as inhibitors of cathepsin A.
Ruf S, Buning C, Schreuder H, Horstick G, Linz W, Olpp T, Pernerstorfer J, Hiss K, Kroll K, Kannt A, Kohlmann M, Linz D, Hübschle T, Rütten H, Wirth K, Schmidt T, Sadowski T.
J Med Chem (2012) 55 : 7636 -7649
PubMed 22861813 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.06 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2171390 1 8.52
CHEMBL2171392 1 8.30
CHEMBL2171394 1 8.00
CHEMBL2171397 1 7.82
CHEMBL2171398 1 7.82
CHEMBL3145342 1 7.60
CHEMBL2171396 1 7.58
CHEMBL2171399 1 7.52
CHEMBL3145341 1 7.42
CHEMBL2171393 1 7.30
CHEMBL3145343 1 7.24
CHEMBL3145344 1 7.23
CHEMBL2171391 1 7.22
CHEMBL2171395 1 7.16
CHEMBL3145334 1 7.16
CHEMBL3145345 1 7.12
CHEMBL3145347 1 7.06
CHEMBL3145346 1 7.00
CHEMBL2171402 1 7.00
CHEMBL3145349 1 6.99
CHEMBL2171401 1 6.96
CHEMBL2171400 1 6.96
CHEMBL3145348 1 6.92
CHEMBL3145350 1 6.70
CHEMBL3145351 1 6.65
CHEMBL3145340 1 6.60
CHEMBL3145353 1 6.56
CHEMBL3145336 1 6.45
CHEMBL3145337 1 6.43
CHEMBL3145338 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2171390 IC50 = 3.0 nM 8.52
CHEMBL2171392 IC50 = 5.0 nM 8.30
CHEMBL2171394 IC50 = 10.0 nM 8.00
CHEMBL2171397 IC50 = 15.0 nM 7.82
CHEMBL2171398 IC50 = 15.0 nM 7.82
CHEMBL3145342 IC50 = 25.0 nM 7.60
CHEMBL2171396 IC50 = 26.0 nM 7.58
CHEMBL2171399 IC50 = 30.0 nM 7.52
CHEMBL3145341 IC50 = 38.0 nM 7.42
CHEMBL2171393 IC50 = 50.0 nM 7.30
CHEMBL3145343 IC50 = 57.0 nM 7.24
CHEMBL3145344 IC50 = 59.0 nM 7.23
CHEMBL2171391 IC50 = 60.0 nM 7.22
CHEMBL2171395 IC50 = 70.0 nM 7.16
CHEMBL3145334 IC50 = 70.0 nM 7.16
CHEMBL3145345 IC50 = 76.0 nM 7.12
CHEMBL3145347 IC50 = 87.0 nM 7.06
CHEMBL3145346 IC50 = 100.0 nM 7.00
CHEMBL2171402 IC50 = 100.0 nM 7.00
CHEMBL3145349 IC50 = 102.0 nM 6.99
CHEMBL2171401 IC50 = 110.0 nM 6.96
CHEMBL2171400 IC50 = 110.0 nM 6.96
CHEMBL3145348 IC50 = 120.0 nM 6.92
CHEMBL3145350 IC50 = 200.0 nM 6.70
CHEMBL3145351 IC50 = 226.0 nM 6.65
CHEMBL3145340 IC50 = 252.0 nM 6.60
CHEMBL3145353 IC50 = 274.0 nM 6.56
CHEMBL3145336 IC50 = 357.0 nM 6.45
CHEMBL3145337 IC50 = 375.0 nM 6.43
CHEMBL3145338 IC50 = 803.0 nM 6.09
CHEMBL3145339 IC50 = 5380.0 nM 5.27
CHEMBL3145335 IC50 = 7800.0 nM 5.11
CHEMBL3145333 IC50 > 30000.0 nM -