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Assay Detail

CHEMBL716609

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Binding
In vitro inhibition of human matrix metalloprotease-2
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

72 kDa type IV collagenase (CHEMBL333)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

N-Aryl sulfonyl homocysteine hydroxamate inhibitors of matrix metalloproteinases: further probing of the S(1), S(1)', and S(2)' pockets.
Hanessian S, Moitessier N, Gauchet C, Viau M.
J Med Chem (2001) 44 : 3066 -3073
PubMed 11543675 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.40 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL323090 1 9.52
CHEMBL105311 1 9.40
CHEMBL102798 1 9.15
CHEMBL104022 1 9.15
CHEMBL102438 1 9.15
CHEMBL102785 1 9.00
CHEMBL421029 1 8.92
CHEMBL106016 1 8.92
CHEMBL407443 1 8.80
CHEMBL104599 1 8.80
CHEMBL420656 1 8.64
CHEMBL320442 1 8.49
CHEMBL105279 1 8.42
CHEMBL319040 1 8.39
CHEMBL104021 1 8.38
CHEMBL105535 1 8.20
CHEMBL322619 1 8.05
CHEMBL316978 1 7.80
CHEMBL105422 1 7.80
CHEMBL104722 1 7.70
CHEMBL102504 1 7.52
CHEMBL105142 1 7.28
CHEMBL102441 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL323090 IC50 = 0.3 nM 9.52
CHEMBL105311 IC50 = 0.4 nM 9.40
CHEMBL102798 IC50 = 0.7 nM 9.15
CHEMBL104022 IC50 = 0.7 nM 9.15
CHEMBL102438 IC50 = 0.7 nM 9.15
CHEMBL102785 IC50 = 1.0 nM 9.00
CHEMBL421029 IC50 = 1.2 nM 8.92
CHEMBL106016 IC50 = 1.2 nM 8.92
CHEMBL407443 IC50 = 1.6 nM 8.80
CHEMBL104599 IC50 = 1.6 nM 8.80
CHEMBL420656 IC50 = 2.3 nM 8.64
CHEMBL320442 IC50 = 3.2 nM 8.49
CHEMBL105279 IC50 = 3.78 nM 8.42
CHEMBL319040 IC50 = 4.1 nM 8.39
CHEMBL104021 IC50 = 4.22 nM 8.38
CHEMBL105535 IC50 = 6.3 nM 8.20
CHEMBL322619 IC50 = 8.82 nM 8.05
CHEMBL316978 IC50 = 16.0 nM 7.80
CHEMBL105422 IC50 = 16.0 nM 7.80
CHEMBL104722 IC50 = 20.0 nM 7.70
CHEMBL102504 IC50 = 30.0 nM 7.52
CHEMBL105142 IC50 = 53.0 nM 7.28
CHEMBL102441 IC50 = 1810.0 nM 5.74