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Assay Detail

CHEMBL873369

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Binding
Inhibitory activity against matrix metalloprotease-8
21
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neutrophil collagenase (CHEMBL4588)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and selective carboxylic acid-based inhibitors of matrix metalloproteinases.
Pikul S, Ohler NE, Ciszewski G, Laufersweiler MC, Almstead NG, De B, Natchus MG, Hsieh LC, Janusz MJ, Peng SX, Branch TM, King SL, Taiwo YO, Mieling GE.
J Med Chem (2001) 44 : 2499 -2502
PubMed 11472202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 8.20 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL311266 2 9.30
CHEMBL82169 1 8.92
CHEMBL83368 1 8.82
CHEMBL253680 1 8.82
CHEMBL311004 1 8.74
CHEMBL315114 1 8.62
CHEMBL83955 1 8.57
CHEMBL83282 1 8.52
CHEMBL402745 1 8.52
CHEMBL85374 1 8.49
CHEMBL312100 1 8.44
CHEMBL79267 1 8.28
CHEMBL311097 1 8.17
CHEMBL10454 1 8.03
CHEMBL44383 1 7.97
CHEMBL82113 1 7.59
CHEMBL79906 1 7.52
CHEMBL313340 1 7.35
CHEMBL85026 1 6.53
CHEMBL83616 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL311266 IC50 = 0.5 nM 9.30
CHEMBL82169 IC50 = 1.2 nM 8.92
CHEMBL83368 IC50 = 1.5 nM 8.82
CHEMBL253680 IC50 = 1.5 nM 8.82
CHEMBL311004 IC50 = 1.8 nM 8.74
CHEMBL315114 IC50 = 2.4 nM 8.62
CHEMBL83955 IC50 = 2.7 nM 8.57
CHEMBL83282 IC50 = 3.0 nM 8.52
CHEMBL402745 IC50 = 3.0 nM 8.52
CHEMBL85374 IC50 = 3.2 nM 8.49
CHEMBL311266 IC50 = 3.4 nM 8.47
CHEMBL312100 IC50 = 3.6 nM 8.44
CHEMBL79267 IC50 = 5.3 nM 8.28
CHEMBL311097 IC50 = 6.7 nM 8.17
CHEMBL10454 IC50 = 9.4 nM 8.03
CHEMBL44383 IC50 = 10.6 nM 7.97
CHEMBL82113 IC50 = 25.8 nM 7.59
CHEMBL79906 IC50 = 30.2 nM 7.52
CHEMBL313340 IC50 = 44.8 nM 7.35
CHEMBL85026 IC50 = 294.0 nM 6.53
CHEMBL83616 IC50 = 303.0 nM 6.52