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Assay Detail

CHEMBL717437

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Binding
Inhibitory activity against matrix metalloprotease-13 (MMP-13)
44
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Collagenase 3 (CHEMBL280)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
Reiter LA, Robinson RP, McClure KF, Jones CS, Reese MR, Mitchell PG, Otterness IG, Bliven ML, Liras J, Cortina SR, Donahue KM, Eskra JD, Griffiths RJ, Lame ME, Lopez-Anaya A, Martinelli GJ, McGahee SM, Yocum SA, Lopresti-Morrow LL, Tobiassen LM, Vaughn-Bowser ML.
Bioorg Med Chem Lett (2004) 14 : 3389 -3395
PubMed 15177439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 8.54 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2111753 2 9.46
CHEMBL326369 1 9.43
CHEMBL4524116 1 9.30
CHEMBL115283 1 9.28
CHEMBL432834 1 9.25
CHEMBL325678 1 9.19
CHEMBL4524115 1 9.19
CHEMBL111856 1 9.12
CHEMBL116219 1 9.11
CHEMBL114906 1 9.06
CHEMBL114815 1 9.05
CHEMBL323612 1 9.05
CHEMBL324806 1 9.03
CHEMBL114884 1 9.03
CHEMBL116287 1 9.01
CHEMBL321257 1 8.92
CHEMBL2111754 1 8.92
CHEMBL114831 1 8.89
CHEMBL116237 1 8.82
CHEMBL112470 1 8.82
CHEMBL114148 1 8.82
CHEMBL114272 1 8.77
CHEMBL117375 1 8.77
CHEMBL112609 1 8.70
CHEMBL4524117 1 8.48
CHEMBL113778 1 8.36
CHEMBL112374 1 8.34
CHEMBL116067 1 8.34
CHEMBL325903 1 8.30
CHEMBL114158 1 8.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2111753 IC50 = 0.35 nM 9.46
CHEMBL326369 IC50 = 0.37 nM 9.43
CHEMBL4524116 IC50 = 0.5 nM 9.30
CHEMBL115283 IC50 = 0.53 nM 9.28
CHEMBL432834 IC50 = 0.56 nM 9.25
CHEMBL325678 IC50 = 0.65 nM 9.19
CHEMBL4524115 IC50 = 0.65 nM 9.19
CHEMBL111856 IC50 = 0.75 nM 9.12
CHEMBL116219 IC50 = 0.77 nM 9.11
CHEMBL114906 IC50 = 0.87 nM 9.06
CHEMBL323612 IC50 = 0.9 nM 9.05
CHEMBL114815 IC50 = 0.9 nM 9.05
CHEMBL324806 IC50 = 0.93 nM 9.03
CHEMBL114884 IC50 = 0.93 nM 9.03
CHEMBL116287 IC50 = 0.97 nM 9.01
CHEMBL2111753 IC50 = 1.0 nM 9.00
CHEMBL2111754 IC50 = 1.2 nM 8.92
CHEMBL321257 IC50 = 1.2 nM 8.92
CHEMBL114831 IC50 = 1.3 nM 8.89
CHEMBL116237 IC50 = 1.5 nM 8.82
CHEMBL112470 IC50 = 1.5 nM 8.82
CHEMBL114148 IC50 = 1.5 nM 8.82
CHEMBL114272 IC50 = 1.7 nM 8.77
CHEMBL117375 IC50 = 1.7 nM 8.77
CHEMBL112609 IC50 = 2.0 nM 8.70
CHEMBL4524117 IC50 = 3.3 nM 8.48
CHEMBL113778 IC50 = 4.4 nM 8.36
CHEMBL116067 IC50 = 4.6 nM 8.34
CHEMBL112374 IC50 = 4.6 nM 8.34
CHEMBL325903 IC50 = 5.0 nM 8.30
CHEMBL114158 IC50 = 5.7 nM 8.24
CHEMBL324615 IC50 = 6.5 nM 8.19
CHEMBL115168 IC50 = 9.7 nM 8.01
CHEMBL114528 IC50 = 11.0 nM 7.96
CHEMBL115666 IC50 = 13.0 nM 7.89
CHEMBL113705 IC50 = 14.0 nM 7.85
CHEMBL114378 IC50 = 17.0 nM 7.77
CHEMBL514138 CGS-27023A IC50 = 18.0 nM 7.75
CHEMBL115877 IC50 = 19.0 nM 7.72
CHEMBL324578 IC50 = 24.0 nM 7.62
CHEMBL115223 IC50 = 25.0 nM 7.60
CHEMBL116904 IC50 = 49.0 nM 7.31
CHEMBL116348 IC50 = 50.0 nM 7.30
CHEMBL324555 IC50 = 210.0 nM 6.68