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Assay Detail

CHEMBL872557

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

Binding
Inhibition of human matrix metalloprotease-9
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Matrix metalloproteinase-9 (CHEMBL321)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Xue CB, He X, Corbett RL, Roderick J, Wasserman ZR, Liu RQ, Jaffee BD, Covington MB, Qian M, Trzaskos JM, Newton RC, Magolda RL, Wexler RR, Decicco CP.
J Med Chem (2001) 44 : 3351 -3354
PubMed 11585440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.01 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91636 1 8.92
CHEMBL432990 1 7.68
CHEMBL325421 1 7.04
CHEMBL324550 1 6.74
CHEMBL323929 1 5.93
CHEMBL431680 1 5.75
CHEMBL324549 1 -
CHEMBL115263 1 -
CHEMBL325163 1 -
CHEMBL114878 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91636 Ki = 1.2 nM 8.92
CHEMBL432990 Ki = 21.0 nM 7.68
CHEMBL325421 Ki = 91.0 nM 7.04
CHEMBL324550 Ki = 183.0 nM 6.74
CHEMBL323929 Ki = 1170.0 nM 5.93
CHEMBL431680 Ki = 1787.0 nM 5.75
CHEMBL324549 Ki > 2000.0 nM -
CHEMBL115263 Ki > 2000.0 nM -
CHEMBL325163 Ki > 2000.0 nM -
CHEMBL114878 Ki > 2000.0 nM -