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Assay Detail

CHEMBL710554

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

Binding
Inhibition of the Gelatinase-A enzyme was determined from purified NSO cells.
20
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent and selective inhibitors of gelatinase-A 2. carboxylic and phosphonic acid derivatives
Morphy J, Beeley NR, Boyce BA, Leonard J, Mason B, Millican A, Millar K, O'Connell JP, Porter J
Bioorg Med Chem Lett (1994) 4 : 2747 -2752
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.04 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75403 1 10.22
CHEMBL78335 1 9.05
CHEMBL307365 1 9.00
CHEMBL420376 1 8.99
CHEMBL75148 1 8.93
CHEMBL309067 1 8.74
CHEMBL76869 2 8.60
CHEMBL77956 1 8.51
CHEMBL306177 1 8.42
CHEMBL78047 1 8.22
CHEMBL432346 1 8.19
CHEMBL77461 1 8.00
CHEMBL307027 1 7.99
CHEMBL74977 1 7.72
CHEMBL307211 1 7.33
CHEMBL307207 1 6.91
CHEMBL91054 1 6.80
CHEMBL91055 1 6.68
CHEMBL306779 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75403 Ki = 0.06 nM 10.22
CHEMBL78335 Ki = 0.9 nM 9.05
CHEMBL307365 Ki = 1.0 nM 9.00
CHEMBL420376 Ki = 1.03 nM 8.99
CHEMBL75148 Ki = 1.17 nM 8.93
CHEMBL309067 Ki = 1.83 nM 8.74
CHEMBL76869 Ki = 2.5 nM 8.60
CHEMBL77956 Ki = 3.06 nM 8.51
CHEMBL306177 Ki = 3.82 nM 8.42
CHEMBL78047 Ki = 6.0 nM 8.22
CHEMBL432346 Ki = 6.4 nM 8.19
CHEMBL77461 Ki = 10.0 nM 8.00
CHEMBL307027 Ki = 10.3 nM 7.99
CHEMBL74977 Ki = 18.9 nM 7.72
CHEMBL307211 Ki = 46.5 nM 7.33
CHEMBL307207 Ki = 123.0 nM 6.91
CHEMBL91054 Ki = 157.0 nM 6.80
CHEMBL91055 Ki = 210.0 nM 6.68
CHEMBL76869 Ki = 366.0 nM 6.44
CHEMBL306779 Ki = 812.0 nM 6.09