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Assay Detail

CHEMBL5390754

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

Binding
Inhibition of porcine pancreatic elastase using N-succinyl-Ala-Ala-Ala-p-nitroanilide as substrate preincubated with enzyme for 15 mins followed by substrate addition and measured for 30 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Cyclotheonellazoles D-I, Potent Elastase Inhibitory Thiazole-Containing Cyclic Peptides from <i>Theonella</i> sp. (2131).
Holland DC, Schroder WA, Calcott MJ, Kaemmerer E, Avery VM, Ekins MG, Carroll AR.
J Nat Prod (2023) 86 : 2216 -2227
PubMed 37609780 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.45 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5431486 1 7.80
CHEMBL5432223 1 7.75
CHEMBL5418049 1 7.70
CHEMBL5394627 1 7.55
CHEMBL5408836 1 7.46
CHEMBL5414337 1 7.29
CHEMBL5397807 1 7.21
CHEMBL190503 PHENYLMETHYLSULFONYLFLUORIDE 1 6.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5431486 IC50 = 16.0 nM 7.80
CHEMBL5432223 IC50 = 17.6 nM 7.75
CHEMBL5418049 IC50 = 20.1 nM 7.70
CHEMBL5394627 IC50 = 28.0 nM 7.55
CHEMBL5408836 IC50 = 34.8 nM 7.46
CHEMBL5414337 IC50 = 51.3 nM 7.29
CHEMBL5397807 IC50 = 61.8 nM 7.21
CHEMBL190503 PHENYLMETHYLSULFONYLFLUORIDE IC50 = 138.1 nM 6.86