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Assay Detail

CHEMBL2429273

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

Binding
Inhibition of MMP-8 (unknown origin) using 7-methoxycoumarin-4-yl)acetyl-Pro-Leu-Gly-Leu-(3-(2,4-dinitrophenyl)-L-2,3-diamino-propionyl)Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
20
Total Activities
20
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

Neutrophil collagenase (CHEMBL4588)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inverse 1,2,3-triazole-1-yl-ethyl substituted hydroxamates as highly potent matrix metalloproteinase inhibitors: (radio)synthesis, in vitro and first in vivo evaluation.
Hugenberg V, Riemann B, Hermann S, Schober O, Schäfers M, Szardenings K, Lebedev A, Gangadharmath U, Kolb H, Walsh J, Zhang W, Kopka K, Wagner S.
J Med Chem (2013) 56 : 6858 -6870
PubMed 23899323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 9.07 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2425938 1 10.30
CHEMBL2425943 1 9.70
CHEMBL2425950 1 9.70
CHEMBL2425944 1 9.52
CHEMBL2425941 1 9.52
CHEMBL2425947 1 9.40
CHEMBL2425936 1 9.40
CHEMBL2425949 1 9.30
CHEMBL2425939 1 9.15
CHEMBL2425932 1 9.05
CHEMBL2425948 1 9.00
CHEMBL2425930 1 9.00
CHEMBL2425931 1 9.00
CHEMBL2425935 1 9.00
CHEMBL2425946 1 8.70
CHEMBL2425933 1 8.70
CHEMBL2425942 1 8.70
CHEMBL2425934 1 8.40
CHEMBL2425940 1 8.30
CHEMBL2425937 1 7.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2425938 IC50 = 0.05 nM 10.30
CHEMBL2425943 IC50 = 0.2 nM 9.70
CHEMBL2425950 IC50 = 0.2 nM 9.70
CHEMBL2425944 IC50 = 0.3 nM 9.52
CHEMBL2425941 IC50 = 0.3 nM 9.52
CHEMBL2425947 IC50 = 0.4 nM 9.40
CHEMBL2425936 IC50 = 0.4 nM 9.40
CHEMBL2425949 IC50 = 0.5 nM 9.30
CHEMBL2425939 IC50 = 0.7 nM 9.15
CHEMBL2425932 IC50 = 0.9 nM 9.05
CHEMBL2425948 IC50 = 1.0 nM 9.00
CHEMBL2425930 IC50 = 1.0 nM 9.00
CHEMBL2425931 IC50 = 1.0 nM 9.00
CHEMBL2425935 IC50 = 1.0 nM 9.00
CHEMBL2425946 IC50 = 2.0 nM 8.70
CHEMBL2425933 IC50 = 2.0 nM 8.70
CHEMBL2425942 IC50 = 2.0 nM 8.70
CHEMBL2425934 IC50 = 4.0 nM 8.40
CHEMBL2425940 IC50 = 5.0 nM 8.30
CHEMBL2425937 IC50 = 35.0 nM 7.46