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Assay Detail

CHEMBL714563

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

Binding
In vitro inhibition of Matrix metalloprotease-1.
21
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.
Levin JI, Chen JM, Du MT, Nelson FC, Wehr T, DiJoseph JF, Killar LM, Skala S, Sung A, Sharr MA, Roth CE, Jin G, Cowling R, Di L, Sherman M, Xu ZB, March CJ, Mohler KM, Black RA, Skotnicki JS.
Bioorg Med Chem Lett (2001) 11 : 2975 -2978
PubMed 11677139 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.54 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99745 1 7.46
CHEMBL319887 1 6.89
CHEMBL318922 1 6.85
CHEMBL70176 3 6.84
CHEMBL100134 1 6.82
CHEMBL319341 1 6.81
CHEMBL100081 1 6.75
CHEMBL101864 1 6.71
CHEMBL100950 1 6.67
CHEMBL100512 1 6.51
CHEMBL100777 1 6.46
CHEMBL319902 1 6.35
CHEMBL320383 1 6.33
CHEMBL100564 1 6.29
CHEMBL100280 1 6.22
CHEMBL101210 1 6.17
CHEMBL102057 1 6.13
CHEMBL101981 1 6.13
CHEMBL101413 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99745 IC50 = 35.0 nM 7.46
CHEMBL319887 IC50 = 129.0 nM 6.89
CHEMBL318922 IC50 = 142.0 nM 6.85
CHEMBL70176 IC50 = 143.0 nM 6.84
CHEMBL100134 IC50 = 150.0 nM 6.82
CHEMBL319341 IC50 = 155.0 nM 6.81
CHEMBL100081 IC50 = 176.0 nM 6.75
CHEMBL101864 IC50 = 194.0 nM 6.71
CHEMBL100950 IC50 = 213.0 nM 6.67
CHEMBL100512 IC50 = 306.0 nM 6.51
CHEMBL70176 IC50 = 329.0 nM 6.48
CHEMBL100777 IC50 = 343.0 nM 6.46
CHEMBL70176 IC50 = 391.0 nM 6.41
CHEMBL319902 IC50 = 444.0 nM 6.35
CHEMBL320383 IC50 = 470.0 nM 6.33
CHEMBL100564 IC50 = 517.0 nM 6.29
CHEMBL100280 IC50 = 608.0 nM 6.22
CHEMBL101210 IC50 = 674.0 nM 6.17
CHEMBL101981 IC50 = 744.0 nM 6.13
CHEMBL102057 IC50 = 745.0 nM 6.13
CHEMBL101413 IC50 = 781.0 nM 6.11