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Assay Detail

CHEMBL715833

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

Binding
Inhibitory activity against human gelatinase A (matrix metalloprotease-2 MMP2)
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

72 kDa type IV collagenase (CHEMBL333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly selective and orally active inhibitors of type IV collagenase (MMP-9 and MMP-2): N-sulfonylamino acid derivatives.
Tamura Y, Watanabe F, Nakatani T, Yasui K, Fuji M, Komurasaki T, Tsuzuki H, Maekawa R, Yoshioka T, Kawada K, Sugita K, Ohtani M.
J Med Chem (1998) 41 : 640 -649
PubMed 9484512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 48 7.50 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL155923 1 8.89
CHEMBL432882 1 8.70
CHEMBL155874 1 8.59
CHEMBL157704 1 8.19
CHEMBL160232 1 8.17
CHEMBL346265 1 8.08
CHEMBL345200 1 8.00
CHEMBL160305 1 8.00
CHEMBL347138 1 7.89
CHEMBL160153 1 7.89
CHEMBL346118 1 7.77
CHEMBL345597 1 7.72
CHEMBL297792 S-3304 1.0 1 7.70
CHEMBL440921 1 7.64
CHEMBL160969 1 7.47
CHEMBL159229 1 7.30
CHEMBL157705 1 7.30
CHEMBL157363 1 7.30
CHEMBL155959 1 7.30
CHEMBL351363 1 7.28
CHEMBL298699 1 7.28
CHEMBL160940 1 7.18
CHEMBL350674 1 7.08
CHEMBL347658 1 6.96
CHEMBL288750 1 6.89
CHEMBL347847 1 6.55
CHEMBL49411 1 6.51
CHEMBL349798 1 6.00
CHEMBL155815 1 6.00
CHEMBL160712 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL155923 IC50 = 1.3 nM 8.89
CHEMBL432882 IC50 = 2.0 nM 8.70
CHEMBL155874 IC50 = 2.6 nM 8.59
CHEMBL157704 IC50 = 6.5 nM 8.19
CHEMBL160232 IC50 = 6.7 nM 8.17
CHEMBL346265 IC50 = 8.3 nM 8.08
CHEMBL345200 IC50 = 10.0 nM 8.00
CHEMBL160305 IC50 = 10.0 nM 8.00
CHEMBL347138 IC50 = 13.0 nM 7.89
CHEMBL160153 IC50 = 13.0 nM 7.89
CHEMBL346118 IC50 = 17.0 nM 7.77
CHEMBL345597 IC50 = 19.0 nM 7.72
CHEMBL297792 S-3304 IC50 = 20.0 nM 7.70
CHEMBL440921 IC50 = 23.0 nM 7.64
CHEMBL160969 IC50 = 34.0 nM 7.47
CHEMBL159229 IC50 = 50.0 nM 7.30
CHEMBL155959 IC50 = 50.0 nM 7.30
CHEMBL157363 IC50 = 50.0 nM 7.30
CHEMBL157705 IC50 = 50.0 nM 7.30
CHEMBL351363 IC50 = 53.0 nM 7.28
CHEMBL298699 IC50 = 53.0 nM 7.28
CHEMBL160940 IC50 = 66.0 nM 7.18
CHEMBL350674 IC50 = 84.0 nM 7.08
CHEMBL347658 IC50 = 110.0 nM 6.96
CHEMBL288750 IC50 = 130.0 nM 6.89
CHEMBL347847 IC50 = 280.0 nM 6.55
CHEMBL49411 IC50 = 310.0 nM 6.51
CHEMBL349798 IC50 = 1000.0 nM 6.00
CHEMBL155815 IC50 = 1000.0 nM 6.00
CHEMBL348129 IC50 < 1000.0 nM -
CHEMBL158798 IC50 > 1000.0 nM -
CHEMBL160667 IC50 > 1000.0 nM -
CHEMBL159013 IC50 < 40.0 nM -
CHEMBL351110 IC50 > 1000.0 nM -
CHEMBL160465 IC50 < 40.0 nM -
CHEMBL157289 IC50 > 1000.0 nM -
CHEMBL348088 IC50 < 200.0 nM -
CHEMBL49671 IC50 > 1000.0 nM -
CHEMBL345238 IC50 > 1000.0 nM -
CHEMBL160245 IC50 < 40.0 nM -
CHEMBL158674 IC50 > 1000.0 nM -
CHEMBL291194 IC50 > 1000.0 nM -
CHEMBL347612 IC50 > 1000.0 nM -
CHEMBL348335 IC50 < 100.0 nM -
CHEMBL157243 IC50 > 1000.0 nM -
CHEMBL155848 IC50 > 1000.0 nM -
CHEMBL157592 IC50 > 1000.0 nM -
CHEMBL160712 IC50 > 1000.0 nM -