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Assay Detail

CHEMBL714997

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

Binding
Inhibition of matrix metalloprotease-2 (MMP-2), gelatinase-A
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 Expert

Target

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

Publication

Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.
Groneberg RD, Burns CJ, Morrissette MM, Ullrich JW, Morris RL, Darnbrough S, Djuric SW, Condon SM, McGeehan GM, Labaudiniere R, Neuenschwander K, Scotese AC, Kline JA.
J Med Chem (1999) 42 : 541 -544
PubMed 10052961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.53 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114116 1 8.00
CHEMBL153469 1 7.70
CHEMBL44250 1 7.70
CHEMBL42521 1 7.52
CHEMBL151996 1 7.30
CHEMBL44225 1 7.30
CHEMBL151249 1 7.22
CHEMBL432299 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114116 Ki = 10.0 nM 8.00
CHEMBL153469 Ki = 20.0 nM 7.70
CHEMBL44250 Ki = 20.0 nM 7.70
CHEMBL42521 Ki = 30.0 nM 7.52
CHEMBL151996 Ki = 50.0 nM 7.30
CHEMBL44225 Ki = 50.0 nM 7.30
CHEMBL151249 Ki = 60.0 nM 7.22
CHEMBL432299 Ki > 10000.0 nM -