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Assay Detail

CHEMBL694281

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

Binding
Ratio of Koff to that of Kon was determined on human leukocyte elastase(HLE)
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neutrophil elastase (CHEMBL248)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design of potent and stable benzisothiazolone inhibitors of human leukocyte elastase
Hlasta DJ, Bell MR, Court JJ, Cundy KC, Desai RC, Ferguson EW, Gordon RJ, Kumar V, Maycock AL, Subramanyam C, Dunlap RP, Eiff SL, Franke CA, Mura AJ, Rowlands AG
Bioorg Med Chem Lett (1995) 5 : 331 -336
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 9.01 10.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL115827 1 10.64
CHEMBL325155 1 10.52
CHEMBL314218 1 10.52
CHEMBL112575 1 9.70
CHEMBL98422 1 9.57
CHEMBL50974 1 9.52
CHEMBL50830 1 9.22
CHEMBL319723 1 9.22
CHEMBL299656 1 9.15
CHEMBL333152 1 8.96
CHEMBL296159 1 8.70
CHEMBL100620 1 8.70
CHEMBL323694 1 8.66
CHEMBL112205 1 8.28
CHEMBL432890 1 7.85
CHEMBL323545 1 7.84
CHEMBL50803 1 7.82
CHEMBL298107 1 7.22
CHEMBL300430 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL115827 Ki = 0.023 nM 10.64
CHEMBL325155 Ki = 0.03 nM 10.52
CHEMBL314218 Ki = 0.03 nM 10.52
CHEMBL112575 Ki = 0.2 nM 9.70
CHEMBL98422 Ki = 0.27 nM 9.57
CHEMBL50974 Ki = 0.3 nM 9.52
CHEMBL50830 Ki = 0.6 nM 9.22
CHEMBL319723 Ki = 0.6 nM 9.22
CHEMBL299656 Ki = 0.7 nM 9.15
CHEMBL333152 Ki = 1.1 nM 8.96
CHEMBL296159 Ki = 2.0 nM 8.70
CHEMBL100620 Ki = 2.0 nM 8.70
CHEMBL323694 Ki = 2.2 nM 8.66
CHEMBL112205 Ki = 5.2 nM 8.28
CHEMBL432890 Ki = 14.0 nM 7.85
CHEMBL323545 Ki = 14.5 nM 7.84
CHEMBL50803 Ki = 15.0 nM 7.82
CHEMBL298107 Ki = 60.0 nM 7.22
CHEMBL300430 Ki > 2000.0 nM -