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Assay Detail

CHEMBL718391

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Binding
In vitro inhibitory activity against the ectodomain of the human matrix metalloprotease-14
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Matrix metalloproteinase-14 (CHEMBL3869)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design and synthesis of potent matrix metalloproteinase inhibitors derived from a 6H-1,3,4-thiadiazine scaffold.
Schröder J, Henke A, Wenzel H, Brandstetter H, Stammler HG, Stammler A, Pfeiffer WD, Tschesche H.
J Med Chem (2001) 44 : 3231 -3243
PubMed 11563922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.63 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109806 1 6.96
CHEMBL109214 1 6.82
CHEMBL110970 1 6.75
CHEMBL111179 1 6.75
CHEMBL111678 1 6.70
CHEMBL111257 1 6.68
CHEMBL109353 1 6.68
CHEMBL322795 1 6.48
CHEMBL422251 1 6.48
CHEMBL109770 1 6.41
CHEMBL111450 1 6.40
CHEMBL422250 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109806 Ki = 110.0 nM 6.96
CHEMBL109214 Ki = 150.0 nM 6.82
CHEMBL110970 Ki = 180.0 nM 6.75
CHEMBL111179 Ki = 180.0 nM 6.75
CHEMBL111678 Ki = 200.0 nM 6.70
CHEMBL111257 Ki = 210.0 nM 6.68
CHEMBL109353 Ki = 210.0 nM 6.68
CHEMBL322795 Ki = 330.0 nM 6.48
CHEMBL422251 Ki = 330.0 nM 6.48
CHEMBL109770 Ki = 390.0 nM 6.41
CHEMBL111450 Ki = 400.0 nM 6.40
CHEMBL422250 Ki = 400.0 nM 6.40