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Assay Detail

CHEMBL1008221

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Binding
Inhibition of human recombinant furin assessed as fluorescent Pyr-RTKR-AMC substrate cleavage
ChEMBL ↗
265
Total Activities
265
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

Furin (CHEMBL2611) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.
Shiryaev SA, Remacle AG, Ratnikov BI, Nelson NA, Savinov AY, Wei G, Bottini M, Rega MF, Parent A, Desjardins R, Fugere M, Day R, Sabet M, Pellecchia M, Liddington RC, Smith JW, Mustelin T, Guiney DG, Lebl M, Strongin AY.
J Biol Chem (2007) 282 : 20847 -20853
PubMed 17537721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 265 7.26 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL525961 — — 1 7.64
CHEMBL502642 — — 1 7.64
CHEMBL525748 — — 1 7.52
CHEMBL504578 — — 1 7.52
CHEMBL455792 — — 1 7.48
CHEMBL503520 — — 1 7.47
CHEMBL524695 — — 1 7.42
CHEMBL500184 — — 1 7.42
CHEMBL451290 — — 1 7.42
CHEMBL526518 — — 1 7.41
CHEMBL504271 — — 1 7.38
CHEMBL526181 — — 1 7.35
CHEMBL501270 — — 1 7.35
CHEMBL506161 — — 1 7.35
CHEMBL499438 — — 1 7.33
CHEMBL501011 — — 1 7.33
CHEMBL509337 — — 1 7.33
CHEMBL505833 — — 1 7.33
CHEMBL525632 — — 1 7.32
CHEMBL500506 — — 1 7.30
CHEMBL2372270 — — 1 7.28
CHEMBL448278 — — 1 7.28
CHEMBL524356 — — 1 7.27
CHEMBL506175 — — 1 7.25
CHEMBL524315 — — 1 7.25
CHEMBL525574 — — 1 7.25
CHEMBL499187 — — 1 7.24
CHEMBL504132 — — 1 7.24
CHEMBL524690 — — 1 7.24
CHEMBL509645 — — 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL525961 — Ki = 23.0 nM 7.64
CHEMBL502642 — Ki = 23.0 nM 7.64
CHEMBL504578 — Ki = 30.0 nM 7.52
CHEMBL525748 — Ki = 30.0 nM 7.52
CHEMBL455792 — Ki = 33.0 nM 7.48
CHEMBL503520 — Ki = 34.0 nM 7.47
CHEMBL524695 — Ki = 38.0 nM 7.42
CHEMBL500184 — Ki = 38.0 nM 7.42
CHEMBL451290 — Ki = 38.0 nM 7.42
CHEMBL526518 — Ki = 39.0 nM 7.41
CHEMBL504271 — Ki = 42.0 nM 7.38
CHEMBL506161 — Ki = 45.0 nM 7.35
CHEMBL501270 — Ki = 45.0 nM 7.35
CHEMBL526181 — Ki = 45.0 nM 7.35
CHEMBL505833 — Ki = 47.0 nM 7.33
CHEMBL509337 — Ki = 47.0 nM 7.33
CHEMBL499438 — Ki = 47.0 nM 7.33
CHEMBL501011 — Ki = 47.0 nM 7.33
CHEMBL525632 — Ki = 48.0 nM 7.32
CHEMBL500506 — Ki = 50.0 nM 7.30
CHEMBL2372270 — Ki = 53.0 nM 7.28
CHEMBL448278 — Ki = 53.0 nM 7.28
CHEMBL524356 — Ki = 54.0 nM 7.27
CHEMBL525574 — Ki = 56.0 nM 7.25
CHEMBL506175 — Ki = 56.0 nM 7.25
CHEMBL524315 — Ki = 56.0 nM 7.25
CHEMBL504132 — Ki = 58.0 nM 7.24
CHEMBL524690 — Ki = 57.0 nM 7.24
CHEMBL509645 — Ki = 57.0 nM 7.24
CHEMBL499187 — Ki = 57.0 nM 7.24
CHEMBL527041 — Ki = 59.0 nM 7.23
CHEMBL506239 — Ki = 59.0 nM 7.23
CHEMBL501797 — Ki = 65.0 nM 7.19
CHEMBL454768 — Ki = 65.0 nM 7.19
CHEMBL524837 — Ki = 66.0 nM 7.18
CHEMBL504445 — Ki = 67.0 nM 7.17
CHEMBL505375 — Ki = 67.0 nM 7.17
CHEMBL503500 — Ki = 80.0 nM 7.10
CHEMBL526675 — Ki = 80.0 nM 7.10
CHEMBL526506 — Ki = 81.0 nM 7.09
CHEMBL503035 — Ki = 81.0 nM 7.09
CHEMBL510847 — Ki = 88.0 nM 7.06
CHEMBL446203 — Ki = 93.0 nM 7.03
CHEMBL507415 — Ki = 103.0 nM 6.99
CHEMBL526873 — Ki = 115.0 nM 6.94
CHEMBL446476 — Ki = 127.0 nM 6.90
CHEMBL507627 — Ki = 138.0 nM 6.86
CHEMBL510969 — Ki > 100.0 nM -
CHEMBL504326 — Ki > 100.0 nM -
CHEMBL509593 — Ki > 100.0 nM -