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Assay Detail

CHEMBL5366136

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

Binding
Binding affinity to human recombinant MMP-2 CD assessed as inhibition constant using OMNIMMP as substrate incubated for 30 mins by fluorescence based analysis
8
Total Activities
8
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

Kinetics, Thermodynamics, and Structural Effects of Quinoline-2-Carboxylates, Zinc-Binding Inhibitors of New Delhi Metallo-β-lactamase-1 Re-sensitizing Multidrug-Resistant Bacteria for Carbapenems.
Jia Y, Schroeder B, Pfeifer Y, Fröhlich C, Deng L, Arkona C, Kuropka B, Sticht J, Ataka K, Bergemann S, Wolber G, Nitsche C, Mielke M, Leiros HS, Werner G, Rademann J.
J Med Chem (2023) 66 : 11761 -11791
PubMed 37585683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.25 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5434080 1 6.22
CHEMBL5397784 1 5.67
CHEMBL5439532 1 5.39
CHEMBL5421999 1 5.24
CHEMBL5434850 1 5.16
CHEMBL5436058 1 5.11
CHEMBL5405077 1 4.68
CHEMBL5424619 1 4.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5434080 Ki = 600.0 nM 6.22
CHEMBL5397784 Ki = 2120.0 nM 5.67
CHEMBL5439532 Ki = 4080.0 nM 5.39
CHEMBL5421999 Ki = 5780.0 nM 5.24
CHEMBL5434850 Ki = 6920.0 nM 5.16
CHEMBL5436058 Ki = 7750.0 nM 5.11
CHEMBL5405077 Ki = 20730.0 nM 4.68
CHEMBL5424619 Ki = 27630.0 nM 4.56