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Assay Detail

CHEMBL675337

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

Binding
Binding affinity against human Elastase
17
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Chymotrypsin-like elastase family member 1 (CHEMBL3000)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of peptidyl fluoromethyl ketones and peptidyl alpha-keto esters as inhibitors of porcine pancreatic elastase, human neutrophil elastase, and rat and human neutrophil cathepsin G.
Peet NP, Burkhart JP, Angelastro MR, Giroux EL, Mehdi S, Bey P, Kolb M, Neises B, Schirlin D.
J Med Chem (1990) 33 : 394 -407
PubMed 2296031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.67 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130253 1 9.24
CHEMBL336171 1 9.00
CHEMBL130271 1 7.85
CHEMBL337396 1 7.36
CHEMBL446422 1 6.80
CHEMBL436383 1 6.70
CHEMBL130128 2 6.60
CHEMBL131188 1 6.52
CHEMBL132768 1 6.18
CHEMBL131780 1 6.07
CHEMBL340062 1 5.37
CHEMBL130718 2 4.39
CHEMBL130006 1 -
CHEMBL339870 1 -
CHEMBL132171 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130253 Ki = 0.58 nM 9.24
CHEMBL336171 Ki = 1.0 nM 9.00
CHEMBL130271 Ki = 14.0 nM 7.85
CHEMBL337396 Ki = 44.0 nM 7.36
CHEMBL446422 Ki = 160.0 nM 6.80
CHEMBL436383 Ki = 200.0 nM 6.70
CHEMBL130128 Ki = 250.0 nM 6.60
CHEMBL131188 Ki = 300.0 nM 6.52
CHEMBL132768 Ki = 660.0 nM 6.18
CHEMBL131780 Ki = 850.0 nM 6.07
CHEMBL340062 Ki = 4300.0 nM 5.37
CHEMBL130128 Ki = 24000.0 nM 4.62
CHEMBL130718 Ki = 41000.0 nM 4.39
CHEMBL130006 Ki > 1000000.0 nM -
CHEMBL339870 Ki = 1000000.0 nM -
CHEMBL132171 Ki > 1500000.0 nM -
CHEMBL130718 Ki > 800000.0 nM -