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Assay Detail

CHEMBL827219

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Binding
In vitro inhibitory activity against matrix metalloprotease-13
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Collagenase 3 (CHEMBL280)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Benzodiazepine inhibitors of the MMPs and TACE. Part 2.
Levin JI, Nelson FC, Delos Santos E, Du MT, MacEwan G, Chen JM, Ayral-Kaloustian S, Xu J, Jin G, Cummons T, Barone D.
Bioorg Med Chem Lett (2004) 14 : 4147 -4151
PubMed 15261259 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.54 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL366257 1 8.15
CHEMBL183732 1 7.92
CHEMBL184007 1 7.77
CHEMBL359969 1 7.77
CHEMBL365892 1 7.72
CHEMBL185375 1 7.70
CHEMBL183924 1 7.70
CHEMBL183735 1 7.68
CHEMBL184119 1 7.55
CHEMBL184168 1 7.50
CHEMBL363758 1 7.48
CHEMBL184943 1 7.38
CHEMBL184745 1 7.33
CHEMBL363938 1 7.28
CHEMBL183228 1 7.17
CHEMBL97790 1 7.11
CHEMBL183404 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL366257 IC50 = 7.0 nM 8.15
CHEMBL183732 IC50 = 12.0 nM 7.92
CHEMBL184007 IC50 = 17.0 nM 7.77
CHEMBL359969 IC50 = 17.0 nM 7.77
CHEMBL365892 IC50 = 19.0 nM 7.72
CHEMBL185375 IC50 = 20.0 nM 7.70
CHEMBL183924 IC50 = 20.0 nM 7.70
CHEMBL183735 IC50 = 21.0 nM 7.68
CHEMBL184119 IC50 = 28.0 nM 7.55
CHEMBL184168 IC50 = 32.0 nM 7.50
CHEMBL363758 IC50 = 33.0 nM 7.48
CHEMBL184943 IC50 = 42.0 nM 7.38
CHEMBL184745 IC50 = 47.0 nM 7.33
CHEMBL363938 IC50 = 53.0 nM 7.28
CHEMBL183228 IC50 = 67.0 nM 7.17
CHEMBL97790 IC50 = 77.0 nM 7.11
CHEMBL183404 IC50 = 97.0 nM 7.01