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Assay Detail

CHEMBL927859

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Binding
Inhibition of MMP9
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.
Burns DM, He C, Li Y, Scherle P, Liu X, Marando CA, Covington MB, Yang G, Pan M, Turner S, Fridman JS, Hollis G, Vaddi K, Yeleswaram S, Newton R, Friedman S, Metcalf B, Yao W.
Bioorg Med Chem Lett (2008) 18 : 560 -564
PubMed 18068976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.94 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL404409 1 7.66
CHEMBL251820 1 7.60
CHEMBL399351 1 7.11
CHEMBL252627 1 7.00
CHEMBL254295 1 6.27
CHEMBL254510 1 6.02
CHEMBL252024 1 -
CHEMBL253665 1 -
CHEMBL253035 1 -
CHEMBL256157 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL404409 IC50 = 22.0 nM 7.66
CHEMBL251820 IC50 = 25.0 nM 7.60
CHEMBL399351 IC50 = 78.0 nM 7.11
CHEMBL252627 IC50 = 100.0 nM 7.00
CHEMBL254295 IC50 = 535.0 nM 6.27
CHEMBL254510 IC50 = 955.0 nM 6.02
CHEMBL252024 IC50 > 5000.0 nM -
CHEMBL253665 IC50 > 5000.0 nM -
CHEMBL253035 IC50 > 5000.0 nM -
CHEMBL256157 IC50 < 1.5 nM -