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Assay Detail

CHEMBL715873

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

Binding
Inhibitory activity against matrix metalloprotease-3 (MMP-3)(stromelysin-1).
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Stromelysin-1 (CHEMBL283)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New type of metalloproteinase inhibitor: design and synthesis of new phosphonamide-based hydroxamic acids.
Sawa M, Kiyoi T, Kurokawa K, Kumihara H, Yamamoto M, Miyasaka T, Ito Y, Hirayama R, Inoue T, Kirii Y, Nishiwaki E, Ohmoto H, Maeda Y, Ishibushi E, Inoue Y, Yoshino K, Kondo H.
J Med Chem (2002) 45 : 919 -929
PubMed 11831904 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.84 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL425316 1 9.30
CHEMBL355797 1 9.28
CHEMBL172249 1 8.69
CHEMBL173846 1 8.61
CHEMBL170315 1 8.53
CHEMBL539171 1 8.36
CHEMBL173686 1 8.31
CHEMBL170429 1 8.29
CHEMBL366478 1 8.28
CHEMBL173316 1 8.28
CHEMBL368857 1 8.27
CHEMBL173027 1 8.19
CHEMBL174315 1 8.09
CHEMBL177072 1 7.97
CHEMBL175164 1 7.94
CHEMBL171962 1 7.91
CHEMBL173754 1 7.89
CHEMBL173235 1 7.83
CHEMBL368205 1 7.62
CHEMBL173744 1 7.61
CHEMBL172722 1 7.53
CHEMBL353536 1 7.53
CHEMBL172548 1 7.46
CHEMBL173326 1 7.32
CHEMBL172415 1 7.29
CHEMBL172885 1 7.19
CHEMBL367710 1 7.17
CHEMBL172886 1 7.14
CHEMBL171292 1 7.08
CHEMBL436049 1 6.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL425316 Ki = 0.5 nM 9.30
CHEMBL355797 Ki = 0.53 nM 9.28
CHEMBL172249 Ki = 2.04 nM 8.69
CHEMBL173846 Ki = 2.43 nM 8.61
CHEMBL170315 Ki = 2.95 nM 8.53
CHEMBL539171 Ki = 4.36 nM 8.36
CHEMBL173686 Ki = 4.85 nM 8.31
CHEMBL170429 Ki = 5.19 nM 8.29
CHEMBL366478 Ki = 5.2 nM 8.28
CHEMBL173316 Ki = 5.2 nM 8.28
CHEMBL368857 Ki = 5.43 nM 8.27
CHEMBL173027 Ki = 6.41 nM 8.19
CHEMBL174315 Ki = 8.15 nM 8.09
CHEMBL177072 Ki = 10.7 nM 7.97
CHEMBL175164 Ki = 11.6 nM 7.94
CHEMBL171962 Ki = 12.3 nM 7.91
CHEMBL173754 Ki = 12.8 nM 7.89
CHEMBL173235 Ki = 14.9 nM 7.83
CHEMBL368205 Ki = 24.0 nM 7.62
CHEMBL173744 Ki = 24.4 nM 7.61
CHEMBL172722 Ki = 29.7 nM 7.53
CHEMBL353536 Ki = 29.6 nM 7.53
CHEMBL172548 Ki = 34.9 nM 7.46
CHEMBL173326 Ki = 47.8 nM 7.32
CHEMBL172415 Ki = 51.4 nM 7.29
CHEMBL172885 Ki = 64.4 nM 7.19
CHEMBL367710 Ki = 67.0 nM 7.17
CHEMBL172886 Ki = 72.9 nM 7.14
CHEMBL171292 Ki = 82.4 nM 7.08
CHEMBL436049 Ki = 162.0 nM 6.79
CHEMBL171986 Ki = 190.0 nM 6.72
CHEMBL172181 Ki = 527.0 nM 6.28
CHEMBL433981 Ki > 650.0 nM -
CHEMBL418655 Ki > 650.0 nM -
CHEMBL174014 Ki > 650.0 nM -