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Assay Detail

CHEMBL4193097

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

Binding
Inhibition of recombinant human MMP9 (Ala20 to Asp707 residues) expressed in CHO cells using Mca-Pro-LeuGly-Leu-Dpa-Ala-Arg-NH2 as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Matrix metalloproteinase-9 (CHEMBL321)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of dehydroabietic acid sulfonamide based derivatives as selective matrix metalloproteinases inactivators that inhibit cell migration and proliferation.
Huang RZ, Liang GB, Huang XC, Zhang B, Zhou MM, Liao ZX, Wang HS.
Eur J Med Chem (2017) 138 : 979 -992
PubMed 28756264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 4.50 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267178 1 8.00
CHEMBL4215396 1 5.06
CHEMBL4207542 1 4.68
CHEMBL4216220 1 4.61
CHEMBL4216154 1 4.56
CHEMBL4202778 1 4.47
CHEMBL4213804 1 4.46
CHEMBL4210262 1 4.44
CHEMBL4214436 1 4.36
CHEMBL4203206 1 4.32
CHEMBL4218730 1 4.29
CHEMBL4215930 1 4.29
CHEMBL4206886 1 4.27
CHEMBL4210975 1 4.26
CHEMBL4211708 1 4.25
CHEMBL4203717 1 4.24
CHEMBL4212449 1 4.18
CHEMBL4211189 1 4.14
CHEMBL4202989 1 4.08
CHEMBL4211258 1 4.08
CHEMBL4211771 1 4.03
CHEMBL4206821 1 4.02
CHEMBL4203061 1 -
CHEMBL4215193 1 -
CHEMBL4214656 1 -
CHEMBL12850 DEHYDROABIETIC ACID 1 -
CHEMBL4202455 1 -
CHEMBL4207344 1 -
CHEMBL4211700 1 -
CHEMBL4202528 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267178 IC50 = 10.0 nM 8.00
CHEMBL4215396 IC50 = 8800.0 nM 5.06
CHEMBL4207542 IC50 = 20900.0 nM 4.68
CHEMBL4216220 IC50 = 24300.0 nM 4.61
CHEMBL4216154 IC50 = 27400.0 nM 4.56
CHEMBL4202778 IC50 = 33600.0 nM 4.47
CHEMBL4213804 IC50 = 34800.0 nM 4.46
CHEMBL4210262 IC50 = 36300.0 nM 4.44
CHEMBL4214436 IC50 = 43900.0 nM 4.36
CHEMBL4203206 IC50 = 48300.0 nM 4.32
CHEMBL4218730 IC50 = 51900.0 nM 4.29
CHEMBL4215930 IC50 = 51600.0 nM 4.29
CHEMBL4206886 IC50 = 53600.0 nM 4.27
CHEMBL4210975 IC50 = 54600.0 nM 4.26
CHEMBL4211708 IC50 = 56200.0 nM 4.25
CHEMBL4203717 IC50 = 57800.0 nM 4.24
CHEMBL4212449 IC50 = 66600.0 nM 4.18
CHEMBL4211189 IC50 = 72600.0 nM 4.14
CHEMBL4202989 IC50 = 82600.0 nM 4.08
CHEMBL4211258 IC50 = 83400.0 nM 4.08
CHEMBL4211771 IC50 = 93100.0 nM 4.03
CHEMBL4206821 IC50 = 95900.0 nM 4.02
CHEMBL4203061 IC50 > 100000.0 nM -
CHEMBL4215193 IC50 > 100000.0 nM -
CHEMBL4214656 IC50 > 100000.0 nM -
CHEMBL12850 DEHYDROABIETIC ACID IC50 - -
CHEMBL4202455 IC50 > 100000.0 nM -
CHEMBL4207344 IC50 > 100000.0 nM -
CHEMBL4211700 IC50 > 100000.0 nM -
CHEMBL4202528 IC50 > 100000.0 nM -
CHEMBL4207416 IC50 > 100000.0 nM -
CHEMBL4214716 IC50 > 100000.0 nM -