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Assay Detail

CHEMBL2432398

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

Binding
Inhibition of recombinant human MMP-2 using Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 as substrate incubated for 4 hrs measured every 15 secs for 20 mins by fluorimetric assay
20
Total Activities
20
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

72 kDa type IV collagenase (CHEMBL333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models.
Nuti E, Casalini F, Santamaria S, Fabbi M, Carbotti G, Ferrini S, Marinelli L, La Pietra V, Novellino E, Camodeca C, Orlandini E, Nencetti S, Rossello A.
J Med Chem (2013) 56 : 8089 -8103
PubMed 24044434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.05 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431029 1 8.92
CHEMBL2431030 1 8.52
CHEMBL2337691 1 8.42
CHEMBL2431031 1 8.12
CHEMBL2431016 1 8.11
CHEMBL2431015 1 7.82
CHEMBL2431020 1 7.75
CHEMBL2431017 1 7.70
CHEMBL2431018 1 7.39
CHEMBL2431032 1 7.32
CHEMBL94715 1 6.96
CHEMBL2431028 1 6.62
CHEMBL2431019 1 6.17
CHEMBL2431025 1 5.98
CHEMBL2431027 1 5.84
CHEMBL2431021 1 5.76
CHEMBL2431022 1 5.73
CHEMBL2431024 1 5.42
CHEMBL2431026 1 5.39
CHEMBL2431023 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431029 IC50 = 1.2 nM 8.92
CHEMBL2431030 IC50 = 3.0 nM 8.52
CHEMBL2337691 IC50 = 3.8 nM 8.42
CHEMBL2431031 IC50 = 7.5 nM 8.12
CHEMBL2431016 IC50 = 7.8 nM 8.11
CHEMBL2431015 IC50 = 15.0 nM 7.82
CHEMBL2431020 IC50 = 18.0 nM 7.75
CHEMBL2431017 IC50 = 20.0 nM 7.70
CHEMBL2431018 IC50 = 41.0 nM 7.39
CHEMBL2431032 IC50 = 48.0 nM 7.32
CHEMBL94715 IC50 = 110.0 nM 6.96
CHEMBL2431028 IC50 = 240.0 nM 6.62
CHEMBL2431019 IC50 = 670.0 nM 6.17
CHEMBL2431025 IC50 = 1045.0 nM 5.98
CHEMBL2431027 IC50 = 1440.0 nM 5.84
CHEMBL2431021 IC50 = 1750.0 nM 5.76
CHEMBL2431022 IC50 = 1870.0 nM 5.73
CHEMBL2431024 IC50 = 3800.0 nM 5.42
CHEMBL2431026 IC50 = 4100.0 nM 5.39
CHEMBL2431023 IC50 = 125000.0 nM -