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Assay Detail

CHEMBL5540409

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

Binding
Inhibition of recombinant human MMP7 assessed as enzyme activity by measuring fluorescence using fluorogenic peptide substrate
18
Total Activities
18
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

Matrilysin (CHEMBL4073)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of TP0628103: A Highly Potent and Selective MMP-7 Inhibitor with Reduced OATP-Mediated Clearance Designed by Shifting Isoelectric Points.
Oka Y, Abe-Sato K, Tabuse H, Yasukawa Y, Yahara T, Nishimoto T, Kamitani M, Fukunaga T, Ochiai N, Kumasaka-Abe T, Hitaka K, Gunji E, Ohara H, Takeda T, Kojima N, Asami T.
J Med Chem (2024) 67 : 1406 -1420
PubMed 38214909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 9.48 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5574207 1 10.22
CHEMBL5590289 1 9.92
CHEMBL5575564 1 9.89
CHEMBL5584155 1 9.77
CHEMBL5575333 1 9.77
CHEMBL5573957 1 9.77
CHEMBL5590711 1 9.77
CHEMBL5572317 1 9.70
CHEMBL5572421 1 9.66
CHEMBL5573293 1 9.60
CHEMBL5569043 1 9.59
CHEMBL5570298 1 9.59
CHEMBL5575734 1 9.49
CHEMBL5570760 1 9.30
CHEMBL5567332 1 9.02
CHEMBL5590933 1 8.80
CHEMBL5417105 1 8.55
CHEMBL5565065 1 8.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5574207 IC50 = 0.06 nM 10.22
CHEMBL5590289 IC50 = 0.12 nM 9.92
CHEMBL5575564 IC50 = 0.13 nM 9.89
CHEMBL5584155 IC50 = 0.17 nM 9.77
CHEMBL5575333 IC50 = 0.17 nM 9.77
CHEMBL5573957 IC50 = 0.17 nM 9.77
CHEMBL5590711 IC50 = 0.17 nM 9.77
CHEMBL5572317 IC50 = 0.2 nM 9.70
CHEMBL5572421 IC50 = 0.22 nM 9.66
CHEMBL5573293 IC50 = 0.25 nM 9.60
CHEMBL5569043 IC50 = 0.26 nM 9.59
CHEMBL5570298 IC50 = 0.26 nM 9.59
CHEMBL5575734 IC50 = 0.32 nM 9.49
CHEMBL5570760 IC50 = 0.5 nM 9.30
CHEMBL5567332 IC50 = 0.96 nM 9.02
CHEMBL5590933 IC50 = 1.6 nM 8.80
CHEMBL5417105 IC50 = 2.8 nM 8.55
CHEMBL5565065 IC50 = 7.3 nM 8.14