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Assay Detail

CHEMBL4373196

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

Binding
Inhibition of HGFA catalytic domain (unknown origin) preincubated for 30 mins followed by Boc-QLR-AMC substrate addition and measured for 1 hr by fluorescence assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Hepatocyte growth factor activator (CHEMBL3351190)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Selective Matriptase and Hepsin Serine Protease Inhibitors: Useful Chemical Tools for Cancer Cell Biology.
Damalanka VC, Han Z, Karmakar P, O'Donoghue AJ, La Greca F, Kim T, Pant SM, Helander J, Klefström J, Craik CS, Janetka JW.
J Med Chem (2019) 62 : 480 -490
PubMed 30571119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 5.73 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454016 1 7.52
CHEMBL4540950 1 7.48
CHEMBL4561858 1 6.33
CHEMBL4528632 1 6.02
CHEMBL4552828 1 5.92
CHEMBL4460256 1 5.53
CHEMBL4528379 1 5.50
CHEMBL4445232 1 5.37
CHEMBL4472547 1 5.33
CHEMBL4463174 1 5.32
CHEMBL4551624 1 5.21
CHEMBL4567317 1 5.17
CHEMBL4562668 1 5.10
CHEMBL4562796 1 5.06
CHEMBL4548036 1 5.03
CHEMBL4467638 1 -
CHEMBL4571215 1 -
CHEMBL4469801 1 -
CHEMBL4472544 1 -
CHEMBL4462941 1 -
CHEMBL4455095 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454016 Ki = 30.0 nM 7.52
CHEMBL4540950 Ki = 33.0 nM 7.48
CHEMBL4561858 Ki = 468.0 nM 6.33
CHEMBL4528632 Ki = 963.0 nM 6.02
CHEMBL4552828 Ki = 1208.0 nM 5.92
CHEMBL4460256 Ki = 2961.0 nM 5.53
CHEMBL4528379 Ki = 3197.0 nM 5.50
CHEMBL4445232 Ki = 4303.0 nM 5.37
CHEMBL4472547 Ki = 4634.0 nM 5.33
CHEMBL4463174 Ki = 4771.0 nM 5.32
CHEMBL4551624 Ki = 6122.0 nM 5.21
CHEMBL4567317 Ki = 6827.0 nM 5.17
CHEMBL4562668 Ki = 7984.0 nM 5.10
CHEMBL4562796 Ki = 8634.0 nM 5.06
CHEMBL4548036 Ki = 9375.0 nM 5.03
CHEMBL4467638 Ki > 10000.0 nM -
CHEMBL4571215 Ki > 10000.0 nM -
CHEMBL4469801 Ki > 10000.0 nM -
CHEMBL4472544 Ki > 10000.0 nM -
CHEMBL4462941 Ki > 10000.0 nM -
CHEMBL4455095 Ki > 10000.0 nM -