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Assay Detail

CHEMBL718390

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Binding
In vitro inhibitory activity against the catalytic domain of human matrix metalloprotease-14
15
Total Activities
15
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 15 6.42 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111257 1 7.00
CHEMBL109806 1 6.82
CHEMBL111179 1 6.72
CHEMBL109861 1 6.60
CHEMBL321213 1 6.54
CHEMBL109214 1 6.54
CHEMBL111678 1 6.50
CHEMBL109655 1 6.42
CHEMBL322795 1 6.41
CHEMBL109579 1 6.36
CHEMBL109770 1 6.24
CHEMBL419750 1 6.23
CHEMBL422251 1 6.23
CHEMBL109603 1 6.13
CHEMBL108494 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111257 Ki = 100.0 nM 7.00
CHEMBL109806 Ki = 150.0 nM 6.82
CHEMBL111179 Ki = 190.0 nM 6.72
CHEMBL109861 Ki = 250.0 nM 6.60
CHEMBL321213 Ki = 290.0 nM 6.54
CHEMBL109214 Ki = 290.0 nM 6.54
CHEMBL111678 Ki = 320.0 nM 6.50
CHEMBL109655 Ki = 380.0 nM 6.42
CHEMBL322795 Ki = 390.0 nM 6.41
CHEMBL109579 Ki = 440.0 nM 6.36
CHEMBL109770 Ki = 580.0 nM 6.24
CHEMBL419750 Ki = 590.0 nM 6.23
CHEMBL422251 Ki = 590.0 nM 6.23
CHEMBL109603 Ki = 740.0 nM 6.13
CHEMBL108494 Ki = 3070.0 nM 5.51