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Assay Detail

CHEMBL5217290

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Binding
Inhibition of MMP-2 (unknown origin) using fTHP-15(FAM) as substrate
4
Total Activities
4
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

Development of a putative Zn<sup>2+</sup>-chelating but highly selective MMP-13 inhibitor.
Fuerst R, Choi JY, Knapinska AM, Cameron MD, Ruiz C, Delmas A, Sundrud MS, Fields GB, Roush WR.
Bioorg Med Chem Lett (2022) 76 : 129014 -129014
PubMed 36202189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.74 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4081997 1 6.14
CHEMBL5220833 1 6.08
CHEMBL5219839 1 5.46
CHEMBL5220661 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4081997 IC50 = 730.0 nM 6.14
CHEMBL5220833 IC50 = 832.0 nM 6.08
CHEMBL5219839 IC50 = 3500.0 nM 5.46
CHEMBL5220661 IC50 = 5100.0 nM 5.29