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Assay Detail

CHEMBL2388548

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

Binding
Inhibition of MMP8 (unknown origin)-mediated Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorimetric assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neutrophil collagenase (CHEMBL4588)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold.
Mori M, Massaro A, Calderone V, Fragai M, Luchinat C, Mordini A.
ACS Med Chem Lett (2013) 4 : 565 -569
PubMed 24900710 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.53 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2385487 1 8.52
CHEMBL2385483 1 8.40
CHEMBL2385492 1 8.22
CHEMBL2385486 1 8.15
CHEMBL550148 1 8.05
CHEMBL2385489 1 7.89
CHEMBL2385482 1 7.85
CHEMBL2385488 1 7.70
CHEMBL2385484 1 7.50
CHEMBL2385490 1 7.43
CHEMBL2385481 1 7.37
CHEMBL83508 1 7.23
CHEMBL2385480 1 7.12
CHEMBL2385485 1 7.01
CHEMBL2385479 1 6.62
CHEMBL2385493 1 6.56
CHEMBL2385491 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2385487 Ki = 3.0 nM 8.52
CHEMBL2385483 Ki = 4.0 nM 8.40
CHEMBL2385492 Ki = 6.0 nM 8.22
CHEMBL2385486 Ki = 7.0 nM 8.15
CHEMBL550148 Ki = 9.0 nM 8.05
CHEMBL2385489 Ki = 13.0 nM 7.89
CHEMBL2385482 Ki = 14.0 nM 7.85
CHEMBL2385488 Ki = 20.0 nM 7.70
CHEMBL2385484 Ki = 32.0 nM 7.50
CHEMBL2385490 Ki = 37.0 nM 7.43
CHEMBL2385481 Ki = 43.0 nM 7.37
CHEMBL83508 Ki = 59.0 nM 7.23
CHEMBL2385480 Ki = 75.0 nM 7.12
CHEMBL2385485 Ki = 98.0 nM 7.01
CHEMBL2385479 Ki = 240.0 nM 6.62
CHEMBL2385493 Ki = 275.0 nM 6.56
CHEMBL2385491 Ki = 364.0 nM 6.44