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Assay Detail

CHEMBL1686372

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

Binding
Inhibition of recombinant human MMP14 assessed as substrate cleavage by measuring increase in fluorescence after 16 hrs
22
Total Activities
22
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

Matrix metalloproteinase-14 (CHEMBL3869)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis.
De Savi C, Pape A, Cumming JG, Ting A, Smith PD, Burrows JN, Mills M, Davies C, Lamont S, Milne D, Cook C, Moore P, Sawyer Y, Gerhardt S.
Bioorg Med Chem Lett (2011) 21 : 1376 -1381
PubMed 21300546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.02 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1683445 1 8.12
CHEMBL1683443 1 7.96
CHEMBL1683452 1 7.25
CHEMBL1683454 1 6.80
CHEMBL1683444 1 6.75
CHEMBL1683450 1 6.44
CHEMBL1683451 1 6.41
CHEMBL1615186 1 6.37
CHEMBL1683449 1 6.05
CHEMBL1683460 1 5.58
CHEMBL1683453 1 5.44
CHEMBL1683457 1 5.38
CHEMBL1683455 1 5.34
CHEMBL1683458 1 4.77
CHEMBL1683456 1 4.75
CHEMBL1683465 1 4.54
CHEMBL1683463 1 4.40
CHEMBL1683462 1 -
CHEMBL1683464 1 -
CHEMBL1683461 1 -
CHEMBL1683459 1 -
CHEMBL1615187 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1683445 IC50 = 7.6 nM 8.12
CHEMBL1683443 IC50 = 11.0 nM 7.96
CHEMBL1683452 IC50 = 56.0 nM 7.25
CHEMBL1683454 IC50 = 160.0 nM 6.80
CHEMBL1683444 IC50 = 180.0 nM 6.75
CHEMBL1683450 IC50 = 360.0 nM 6.44
CHEMBL1683451 IC50 = 390.0 nM 6.41
CHEMBL1615186 IC50 = 430.0 nM 6.37
CHEMBL1683449 IC50 = 900.0 nM 6.05
CHEMBL1683460 IC50 = 2600.0 nM 5.58
CHEMBL1683453 IC50 = 3600.0 nM 5.44
CHEMBL1683457 IC50 = 4200.0 nM 5.38
CHEMBL1683455 IC50 = 4600.0 nM 5.34
CHEMBL1683458 IC50 = 17000.0 nM 4.77
CHEMBL1683456 IC50 = 18000.0 nM 4.75
CHEMBL1683465 IC50 = 29000.0 nM 4.54
CHEMBL1683463 IC50 = 40000.0 nM 4.40
CHEMBL1683462 IC50 > 18000.0 nM -
CHEMBL1683464 IC50 > 3600.0 nM -
CHEMBL1683461 IC50 > 3700.0 nM -
CHEMBL1683459 IC50 > 8000.0 nM -
CHEMBL1615187 IC50 > 8900.0 nM -