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Assay Detail

CHEMBL2168709

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

Binding
Inhibition of human recombinant CatL assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage by QFRET assay
33
Total Activities
33
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

Procathepsin L (CHEMBL3837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): a potent and highly selective cathepsin K inhibitor for the treatment of osteoarthritis.
Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, MacFaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M.
J Med Chem (2012) 55 : 6363 -6374
PubMed 22742641 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 5.51 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164674 1 5.51
CHEMBL2164672 1 -
CHEMBL2163588 1 -
CHEMBL2163587 1 -
CHEMBL2163586 1 -
CHEMBL2163585 1 -
CHEMBL2163584 1 -
CHEMBL2163583 1 -
CHEMBL2163582 1 -
CHEMBL2163349 1 -
CHEMBL2163581 1 -
CHEMBL2164690 1 -
CHEMBL2164689 1 -
CHEMBL2164688 1 -
CHEMBL2163360 1 -
CHEMBL2164671 1 -
CHEMBL2164673 1 -
CHEMBL2164675 1 -
CHEMBL2164676 1 -
CHEMBL2164677 1 -
CHEMBL2164687 1 -
CHEMBL2164679 1 -
CHEMBL2164680 1 -
CHEMBL2164681 1 -
CHEMBL2164682 1 -
CHEMBL2164683 1 -
CHEMBL2164684 1 -
CHEMBL2164685 1 -
CHEMBL2164686 1 -
CHEMBL2164678 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164674 IC50 = 3110.0 nM 5.51
CHEMBL2163584 IC50 - -
CHEMBL2164688 IC50 - -
CHEMBL2164689 IC50 - -
CHEMBL2164690 IC50 - -
CHEMBL2163581 IC50 - -
CHEMBL2163349 IC50 - -
CHEMBL2163582 IC50 - -
CHEMBL2163583 IC50 - -
CHEMBL2164671 IC50 > 40000.0 nM -
CHEMBL2163585 IC50 - -
CHEMBL2163586 IC50 - -
CHEMBL2163587 IC50 - -
CHEMBL2163588 IC50 - -
CHEMBL2163589 IC50 - -
CHEMBL2163590 IC50 - -
CHEMBL2163591 IC50 - -
CHEMBL2163360 IC50 - -
CHEMBL2164672 IC50 > 100000.0 nM -
CHEMBL2164673 IC50 > 100000.0 nM -
CHEMBL2164675 IC50 > 40000.0 nM -
CHEMBL2164676 IC50 > 100000.0 nM -
CHEMBL2164677 IC50 > 40000.0 nM -
CHEMBL2164687 IC50 - -
CHEMBL2164679 IC50 > 100000.0 nM -
CHEMBL2164680 IC50 > 40000.0 nM -
CHEMBL2164681 IC50 > 100000.0 nM -
CHEMBL2164682 IC50 - -
CHEMBL2164683 IC50 - -
CHEMBL2164684 IC50 - -
CHEMBL2164685 IC50 - -
CHEMBL2164686 IC50 - -
CHEMBL2164678 IC50 > 40000.0 nM -