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Assay Detail

CHEMBL709520

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

Binding
In vitro inhibition of recombinant human matrix metalloprotease-3 (MMP-3)
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Stromelysin-1 (CHEMBL283)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships and pharmacokinetic analysis for a series of potent, systemically available biphenylsulfonamide matrix metalloproteinase inhibitors.
O'Brien PM, Ortwine DF, Pavlovsky AG, Picard JA, Sliskovic DR, Roth BD, Dyer RD, Johnson LL, Man CF, Hallak H.
J Med Chem (2000) 43 : 156 -166
PubMed 10649971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.84 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43113 1 8.52
CHEMBL432882 1 8.40
CHEMBL433262 1 8.30
CHEMBL42938 1 8.30
CHEMBL43479 1 8.30
CHEMBL45040 1 8.22
CHEMBL43152 1 8.15
CHEMBL44062 1 8.15
CHEMBL47076 1 8.15
CHEMBL42420 1 8.10
CHEMBL44383 1 8.10
CHEMBL46830 1 8.10
CHEMBL296196 1 8.05
CHEMBL47254 1 8.05
CHEMBL44898 1 8.00
CHEMBL418442 1 8.00
CHEMBL43063 1 8.00
CHEMBL432307 1 7.92
CHEMBL44455 1 7.82
CHEMBL46818 1 7.80
CHEMBL539683 1 7.77
CHEMBL43276 1 7.70
CHEMBL297749 1 7.68
CHEMBL295871 1 7.66
CHEMBL291133 1 7.55
CHEMBL42114 1 7.44
CHEMBL43147 1 7.42
CHEMBL42067 1 6.87
CHEMBL43206 1 6.54
CHEMBL43644 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43113 IC50 = 3.0 nM 8.52
CHEMBL432882 IC50 = 4.0 nM 8.40
CHEMBL433262 IC50 = 5.0 nM 8.30
CHEMBL42938 IC50 = 5.0 nM 8.30
CHEMBL43479 IC50 = 5.0 nM 8.30
CHEMBL45040 IC50 = 6.0 nM 8.22
CHEMBL43152 IC50 = 7.0 nM 8.15
CHEMBL44062 IC50 = 7.0 nM 8.15
CHEMBL47076 IC50 = 7.0 nM 8.15
CHEMBL42420 IC50 = 8.0 nM 8.10
CHEMBL44383 IC50 = 8.0 nM 8.10
CHEMBL46830 IC50 = 8.0 nM 8.10
CHEMBL296196 IC50 = 9.0 nM 8.05
CHEMBL47254 IC50 = 9.0 nM 8.05
CHEMBL44898 IC50 = 10.0 nM 8.00
CHEMBL418442 IC50 = 10.0 nM 8.00
CHEMBL43063 IC50 = 10.0 nM 8.00
CHEMBL432307 IC50 = 12.0 nM 7.92
CHEMBL44455 IC50 = 15.0 nM 7.82
CHEMBL46818 IC50 = 16.0 nM 7.80
CHEMBL539683 IC50 = 17.0 nM 7.77
CHEMBL43276 IC50 = 20.0 nM 7.70
CHEMBL297749 IC50 = 21.0 nM 7.68
CHEMBL295871 IC50 = 22.0 nM 7.66
CHEMBL291133 IC50 = 28.0 nM 7.55
CHEMBL42114 IC50 = 36.0 nM 7.44
CHEMBL43147 IC50 = 38.0 nM 7.42
CHEMBL42067 IC50 = 135.0 nM 6.87
CHEMBL43206 IC50 = 290.0 nM 6.54
CHEMBL43644 IC50 = 810.0 nM 6.09