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Assay Detail

CHEMBL709090

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

Binding
Inhibition of fibroblast collagenase (MMP-1)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors.
Steinman DH, Curtin ML, Garland RB, Davidsen SK, Heyman HR, Holms JH, Albert DH, Magoc TJ, Nagy IB, Marcotte PA, Li J, Morgan DW, Hutchins C, Summers JB.
Bioorg Med Chem Lett (1998) 8 : 2087 -2092
PubMed 9873491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.94 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418292 1 8.74
CHEMBL62007 1 8.68
CHEMBL293003 1 8.66
CHEMBL66134 1 8.57
CHEMBL45631 1 8.52
CHEMBL66532 1 8.52
CHEMBL65159 1 8.34
CHEMBL64013 1 8.21
CHEMBL303298 1 8.18
CHEMBL418291 1 7.27
CHEMBL302227 1 6.96
CHEMBL304243 1 6.68
CHEMBL304221 1 5.85
CHEMBL433250 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418292 IC50 = 1.8 nM 8.74
CHEMBL62007 IC50 = 2.1 nM 8.68
CHEMBL293003 IC50 = 2.2 nM 8.66
CHEMBL66134 IC50 = 2.7 nM 8.57
CHEMBL45631 IC50 = 3.0 nM 8.52
CHEMBL66532 IC50 = 3.0 nM 8.52
CHEMBL65159 IC50 = 4.6 nM 8.34
CHEMBL64013 IC50 = 6.1 nM 8.21
CHEMBL303298 IC50 = 6.6 nM 8.18
CHEMBL418291 IC50 = 54.0 nM 7.27
CHEMBL302227 IC50 = 110.0 nM 6.96
CHEMBL304243 IC50 = 210.0 nM 6.68
CHEMBL304221 IC50 = 1400.0 nM 5.85
CHEMBL433250 IC50 > 10000.0 nM -