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Assay Detail

CHEMBL3373435

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

Binding
Inhibition of human recombinant MMP10 using fluorescence peptide Cy3-PLGLK(Cy5Q)AR-NH2 substrate by fluorescence assay
3
Total Activities
3
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

Stromelysin-2 (CHEMBL4270)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site.
Nara H, Sato K, Naito T, Mototani H, Oki H, Yamamoto Y, Kuno H, Santou T, Kanzaki N, Terauchi J, Uchikawa O, Kori M.
Bioorg Med Chem (2014) 22 : 5487 -5505
PubMed 25192810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.18 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440498 CTS-1027 2.0 1 9.27
CHEMBL3337894 T-26c 1 6.80
CHEMBL3337869 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440498 CTS-1027 IC50 = 0.54 nM 9.27
CHEMBL3337894 T-26c IC50 = 160.0 nM 6.80
CHEMBL3337869 IC50 = 3400.0 nM 5.47