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Assay Detail

CHEMBL818574

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

Binding
Binding affinity for human leukocyte elastase (HLE); Kreact/Kinact
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of human leukocyte elastase. 2.1 synthesis and sar of benzisothiazolinylmethyl aryl ethers
Subramanyam C, Bell MR, Ferguson E, Gordon RG, Dunlap RP, Franke C, Mura AJ
Bioorg Med Chem Lett (1995) 5 : 319 -324
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.26 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3085439 1 9.40
CHEMBL109234 1 9.10
CHEMBL109411 1 8.80
CHEMBL446371 1 8.66
CHEMBL109488 1 8.46
CHEMBL322104 1 8.40
CHEMBL111770 1 8.00
CHEMBL111174 1 7.87
CHEMBL111419 1 7.47
CHEMBL110267 1 7.38
CHEMBL323411 1 7.29
CHEMBL325756 1 -
CHEMBL325098 1 -
CHEMBL262709 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3085439 Ki = 0.4 nM 9.40
CHEMBL109234 Ki = 0.8 nM 9.10
CHEMBL109411 Ki = 1.6 nM 8.80
CHEMBL446371 Ki = 2.2 nM 8.66
CHEMBL109488 Ki = 3.5 nM 8.46
CHEMBL322104 Ki = 4.0 nM 8.40
CHEMBL111770 Ki = 10.0 nM 8.00
CHEMBL111174 Ki = 13.6 nM 7.87
CHEMBL111419 Ki = 34.0 nM 7.47
CHEMBL110267 Ki = 42.0 nM 7.38
CHEMBL323411 Ki = 51.6 nM 7.29
CHEMBL325756 Ki > 1000.0 nM -
CHEMBL325098 Ki > 100.0 nM -
CHEMBL262709 Ki > 100.0 nM -