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Assay Detail

CHEMBL1103423

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

Binding
Inhibition of MMP1 by fluorometric assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models.
Nuti E, Casalini F, Avramova SI, Santamaria S, Fabbi M, Ferrini S, Marinelli L, La Pietra V, Limongelli V, Novellino E, Cercignani G, Orlandini E, Nencetti S, Rossello A.
J Med Chem (2010) 53 : 2622 -2635
PubMed 20180536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.29 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1092104 1 8.40
CHEMBL514138 CGS-27023A 1 7.25
CHEMBL1090284 1 7.25
CHEMBL1090647 1 6.71
CHEMBL1090283 1 6.57
CHEMBL311932 1 6.52
CHEMBL1089843 1 6.46
CHEMBL1088878 1 6.40
CHEMBL550148 1 6.21
CHEMBL1090035 1 5.96
CHEMBL1089842 1 5.96
CHEMBL1093690 1 5.82
CHEMBL83508 1 5.52
CHEMBL561625 1 5.32
CHEMBL1093689 1 5.30
CHEMBL181244 1 4.92
CHEMBL226439 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1092104 IC50 = 4.0 nM 8.40
CHEMBL514138 CGS-27023A IC50 = 56.0 nM 7.25
CHEMBL1090284 IC50 = 56.0 nM 7.25
CHEMBL1090647 IC50 = 196.0 nM 6.71
CHEMBL1090283 IC50 = 270.0 nM 6.57
CHEMBL311932 IC50 = 300.0 nM 6.52
CHEMBL1089843 IC50 = 350.0 nM 6.46
CHEMBL1088878 IC50 = 400.0 nM 6.40
CHEMBL550148 IC50 = 610.0 nM 6.21
CHEMBL1090035 IC50 = 1100.0 nM 5.96
CHEMBL1089842 IC50 = 1100.0 nM 5.96
CHEMBL1093690 IC50 = 1500.0 nM 5.82
CHEMBL83508 IC50 = 3000.0 nM 5.52
CHEMBL561625 IC50 = 4800.0 nM 5.32
CHEMBL1093689 IC50 = 5000.0 nM 5.30
CHEMBL181244 IC50 = 12000.0 nM 4.92
CHEMBL226439 IC50 = 110000.0 nM -