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Assay Detail

CHEMBL1937507

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

Binding
Inhibition of human MMP-12
28
Total Activities
28
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

Macrophage metalloelastase (CHEMBL4393)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Wu Y, Li J, Wu J, Morgan P, Xu X, Rancati F, Vallese S, Raveglia L, Hotchandani R, Fuller N, Bard J, Cunningham K, Fish S, Krykbaev R, Tam S, Goldman SJ, Williams C, Mansour TS, Saiah E, Sypek J, Li W.
Bioorg Med Chem Lett (2012) 22 : 138 -143
PubMed 22153340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 8.73 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1935286 1 10.00
CHEMBL1935285 1 10.00
CHEMBL1935287 1 9.70
CHEMBL1935288 1 9.70
CHEMBL1935304 1 9.52
CHEMBL1935290 1 9.40
CHEMBL1935284 1 9.40
CHEMBL1935280 1 9.15
CHEMBL1935291 1 9.00
CHEMBL1935292 1 8.92
CHEMBL1935300 1 8.80
CHEMBL1935298 1 8.72
CHEMBL550038 1 8.70
CHEMBL1935283 1 8.66
CHEMBL1935299 1 8.66
CHEMBL1935301 1 8.64
CHEMBL1935294 1 8.54
CHEMBL1935303 1 8.40
CHEMBL1935295 1 8.35
CHEMBL1935297 1 8.27
CHEMBL1935302 1 8.14
CHEMBL1935293 1 8.07
CHEMBL1935278 1 7.89
CHEMBL1935279 1 7.82
CHEMBL1935296 1 7.77
CHEMBL1935282 1 7.75
CHEMBL1935281 1 7.64
CHEMBL1935289 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1935286 IC50 = 0.1 nM 10.00
CHEMBL1935285 IC50 = 0.1 nM 10.00
CHEMBL1935287 IC50 = 0.2 nM 9.70
CHEMBL1935288 IC50 = 0.2 nM 9.70
CHEMBL1935304 IC50 = 0.3 nM 9.52
CHEMBL1935290 IC50 = 0.4 nM 9.40
CHEMBL1935284 IC50 = 0.4 nM 9.40
CHEMBL1935280 IC50 = 0.7 nM 9.15
CHEMBL1935291 IC50 = 1.0 nM 9.00
CHEMBL1935292 IC50 = 1.2 nM 8.92
CHEMBL1935300 IC50 = 1.6 nM 8.80
CHEMBL1935298 IC50 = 1.9 nM 8.72
CHEMBL550038 IC50 = 2.0 nM 8.70
CHEMBL1935283 IC50 = 2.2 nM 8.66
CHEMBL1935299 IC50 = 2.2 nM 8.66
CHEMBL1935301 IC50 = 2.3 nM 8.64
CHEMBL1935294 IC50 = 2.9 nM 8.54
CHEMBL1935303 IC50 = 4.0 nM 8.40
CHEMBL1935295 IC50 = 4.5 nM 8.35
CHEMBL1935297 IC50 = 5.4 nM 8.27
CHEMBL1935302 IC50 = 7.2 nM 8.14
CHEMBL1935293 IC50 = 8.6 nM 8.07
CHEMBL1935278 IC50 = 13.0 nM 7.89
CHEMBL1935279 IC50 = 15.0 nM 7.82
CHEMBL1935296 IC50 = 17.0 nM 7.77
CHEMBL1935282 IC50 = 18.0 nM 7.75
CHEMBL1935281 IC50 = 23.0 nM 7.64
CHEMBL1935289 IC50 < 1.0 nM -