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Assay Detail

CHEMBL677606

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Binding
In vitro inhibition constant of human leukocyte elastase.
18
Total Activities
18
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

2,6-Disubstituted aryl carboxylic acids, leaving groups "par excellence" for benzisothiazolone inhibitors of human leukocyte elastase.
Subramanyam C, Bell MR, Carabateas P, Court JJ, Dority JA, Ferguson E, Gordon R, Hlasta DJ, Kumar V, Saindane M.
J Med Chem (1994) 37 : 2623 -2626
PubMed 8064791 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.61 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL538776 1 11.00
CHEMBL314218 1 10.52
CHEMBL91944 1 10.22
CHEMBL432049 1 9.77
CHEMBL421162 1 9.00
CHEMBL90327 1 8.70
CHEMBL274085 1 8.57
CHEMBL89549 1 8.40
CHEMBL88117 1 8.10
CHEMBL89299 1 8.10
CHEMBL88975 1 8.07
CHEMBL86364 1 7.75
CHEMBL90730 1 7.58
CHEMBL329376 1 7.51
CHEMBL85128 1 7.43
CHEMBL51377 1 6.99
CHEMBL553298 1 -
CHEMBL539031 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL538776 Ki = 0.01 nM 11.00
CHEMBL314218 Ki = 0.03 nM 10.52
CHEMBL91944 Ki = 0.06 nM 10.22
CHEMBL432049 Ki = 0.17 nM 9.77
CHEMBL421162 Ki = 1.0 nM 9.00
CHEMBL90327 Ki = 2.0 nM 8.70
CHEMBL274085 Ki = 2.7 nM 8.57
CHEMBL89549 Ki = 4.0 nM 8.40
CHEMBL88117 Ki = 8.0 nM 8.10
CHEMBL89299 Ki = 8.0 nM 8.10
CHEMBL88975 Ki = 8.5 nM 8.07
CHEMBL86364 Ki = 18.0 nM 7.75
CHEMBL90730 Ki = 26.0 nM 7.58
CHEMBL329376 Ki = 31.0 nM 7.51
CHEMBL85128 Ki = 37.0 nM 7.43
CHEMBL51377 Ki = 102.0 nM 6.99
CHEMBL553298 Ki = 0.007 nM -
CHEMBL539031 Ki = 0.008 nM -