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Assay Detail

CHEMBL710127

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

Binding
Inhibitory activity against human matrix metalloprotease-3 (MMP-3) (at pH 7.4)
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of new carboxylic acid-based MMP inhibitors derived from functionalized propargylglycines.
Natchus MG, Bookland RG, Laufersweiler MJ, Pikul S, Almstead NG, De B, Janusz MJ, Hsieh LC, Gu F, Pokross ME, Patel VS, Garver SM, Peng SX, Branch TM, King SL, Baker TR, Foltz DJ, Mieling GE.
J Med Chem (2001) 44 : 1060 -1071
PubMed 11297453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 5.30 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10953 1 6.11
CHEMBL10672 1 5.88
CHEMBL10952 1 5.74
CHEMBL10454 1 5.64
CHEMBL10266 1 5.63
CHEMBL275130 1 5.62
CHEMBL10908 1 5.54
CHEMBL10809 1 5.48
CHEMBL10671 1 5.47
CHEMBL10673 1 5.45
CHEMBL10655 1 5.45
CHEMBL10935 1 5.43
CHEMBL275700 1 5.41
CHEMBL274881 1 5.39
CHEMBL276016 1 5.37
CHEMBL10257 1 5.36
CHEMBL10822 1 5.34
CHEMBL10760 1 5.34
CHEMBL10335 1 5.30
CHEMBL10674 1 5.29
CHEMBL10881 1 5.26
CHEMBL10431 1 5.18
CHEMBL10761 1 5.06
CHEMBL10848 1 5.05
CHEMBL10469 1 5.05
CHEMBL10590 1 5.00
CHEMBL10806 1 4.97
CHEMBL10792 1 4.84
CHEMBL407640 1 4.81
CHEMBL274174 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10953 IC50 = 777.0 nM 6.11
CHEMBL10672 IC50 = 1320.0 nM 5.88
CHEMBL10952 IC50 = 1810.0 nM 5.74
CHEMBL10454 IC50 = 2280.0 nM 5.64
CHEMBL10266 IC50 = 2340.0 nM 5.63
CHEMBL275130 IC50 = 2428.0 nM 5.62
CHEMBL10908 IC50 = 2850.0 nM 5.54
CHEMBL10809 IC50 = 3330.0 nM 5.48
CHEMBL10671 IC50 = 3400.0 nM 5.47
CHEMBL10673 IC50 = 3570.0 nM 5.45
CHEMBL10655 IC50 = 3520.0 nM 5.45
CHEMBL10935 IC50 = 3700.0 nM 5.43
CHEMBL275700 IC50 = 3920.0 nM 5.41
CHEMBL274881 IC50 = 4090.0 nM 5.39
CHEMBL276016 IC50 = 4270.0 nM 5.37
CHEMBL10257 IC50 = 4360.0 nM 5.36
CHEMBL10822 IC50 = 4560.0 nM 5.34
CHEMBL10760 IC50 = 4560.0 nM 5.34
CHEMBL10335 IC50 = 5060.0 nM 5.30
CHEMBL10674 IC50 = 5100.0 nM 5.29
CHEMBL10881 IC50 = 5440.0 nM 5.26
CHEMBL10431 IC50 = 6600.0 nM 5.18
CHEMBL10761 IC50 = 8620.0 nM 5.06
CHEMBL10848 IC50 = 9000.0 nM 5.05
CHEMBL10469 IC50 = 8900.0 nM 5.05
CHEMBL10590 IC50 = 10100.0 nM 5.00
CHEMBL10806 IC50 = 10700.0 nM 4.97
CHEMBL10792 IC50 = 14600.0 nM 4.84
CHEMBL407640 IC50 = 15400.0 nM 4.81
CHEMBL274174 IC50 = 16300.0 nM 4.79
CHEMBL10296 IC50 = 17400.0 nM 4.76
CHEMBL10180 IC50 = 22100.0 nM 4.66
CHEMBL275754 IC50 > 10000.0 nM -
CHEMBL10193 IC50 > 10000.0 nM -
CHEMBL10646 IC50 > 10000.0 nM -
CHEMBL11188 IC50 > 9999.0 nM -
CHEMBL11005 IC50 > 10000.0 nM -
CHEMBL10492 IC50 > 10000.0 nM -
CHEMBL274997 IC50 > 10000.0 nM -
CHEMBL268050 IC50 > 10000.0 nM -
CHEMBL10851 IC50 > 10000.0 nM -
CHEMBL275345 IC50 > 10000.0 nM -
CHEMBL10885 IC50 > 10000.0 nM -