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Assay Detail

CHEMBL3266696

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

Binding
Inhibition of recombinant human cathepsin C using H-Gly-Arg-AMC as substrate preincubated for 30 mins before substrate addition measured after 60 mins by fluorescence assay
12
Total Activities
12
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

Dipeptidyl peptidase 1 (CHEMBL2252)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cathepsin C inhibitors: property optimization and identification of a clinical candidate.
Furber M, Tiden AK, Gardiner P, Mete A, Ford R, Millichip I, Stein L, Mather A, Kinchin E, Luckhurst C, Barber S, Cage P, Sanganee H, Austin R, Chohan K, Beri R, Thong B, Wallace A, Oreffo V, Hutchinson R, Harper S, Debreczeni J, Breed J, Wissler L, Edman K.
J Med Chem (2014) 57 : 2357 -2367
PubMed 24592859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.28 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3261927 1 9.10
CHEMBL3261926 1 9.00
CHEMBL212521 1 8.70
CHEMBL3261925 1 8.70
CHEMBL3261924 1 8.60
CHEMBL3261920 1 8.40
CHEMBL3261923 1 8.40
CHEMBL3261922 1 8.30
CHEMBL3261928 1 8.30
CHEMBL3261921 1 7.60
CHEMBL3261919 1 7.40
CHEMBL3261918 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3261927 IC50 = 0.7943 nM 9.10
CHEMBL3261926 IC50 = 1.0 nM 9.00
CHEMBL212521 IC50 = 1.995 nM 8.70
CHEMBL3261925 IC50 = 1.995 nM 8.70
CHEMBL3261924 IC50 = 2.512 nM 8.60
CHEMBL3261920 IC50 = 3.981 nM 8.40
CHEMBL3261923 IC50 = 3.981 nM 8.40
CHEMBL3261922 IC50 = 5.012 nM 8.30
CHEMBL3261928 IC50 = 5.012 nM 8.30
CHEMBL3261921 IC50 = 25.12 nM 7.60
CHEMBL3261919 IC50 = 39.81 nM 7.40
CHEMBL3261918 IC50 = 125.89 nM 6.90