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Assay Detail

CHEMBL828503

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Binding
Inhibitory concentration against MMP-1
24
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

Interstitial collagenase (CHEMBL332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13.
Noe MC, Natarajan V, Snow SL, Wolf-Gouveia LA, Mitchell PG, Lopresti-Morrow L, Reeves LM, Yocum SA, Otterness I, Bliven MA, Carty TJ, Barberia JT, Sweeney FJ, Liras JL, Vaughn M.
Bioorg Med Chem Lett (2005) 15 : 3385 -3388
PubMed 15953722 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.20 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446697 1 6.92
CHEMBL360854 1 6.92
CHEMBL182306 1 6.75
CHEMBL365247 1 6.72
CHEMBL365283 1 6.66
CHEMBL183474 1 6.57
CHEMBL187092 1 6.51
CHEMBL186663 1 6.51
CHEMBL369115 1 6.47
CHEMBL183995 2 6.38
CHEMBL365658 1 6.30
CHEMBL187474 1 6.28
CHEMBL186500 1 6.22
CHEMBL187245 1 6.07
CHEMBL435102 1 5.96
CHEMBL185168 1 5.96
CHEMBL363126 1 5.89
CHEMBL186743 1 5.80
CHEMBL187141 1 5.80
CHEMBL187852 1 5.58
CHEMBL426975 1 5.57
CHEMBL364643 1 5.54
CHEMBL436277 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446697 IC50 = 120.0 nM 6.92
CHEMBL360854 IC50 = 120.0 nM 6.92
CHEMBL182306 IC50 = 180.0 nM 6.75
CHEMBL365247 IC50 = 190.0 nM 6.72
CHEMBL365283 IC50 = 220.0 nM 6.66
CHEMBL183474 IC50 = 270.0 nM 6.57
CHEMBL187092 IC50 = 310.0 nM 6.51
CHEMBL186663 IC50 = 310.0 nM 6.51
CHEMBL369115 IC50 = 340.0 nM 6.47
CHEMBL183995 IC50 = 420.0 nM 6.38
CHEMBL183995 IC50 = 420.0 nM 6.38
CHEMBL365658 IC50 = 500.0 nM 6.30
CHEMBL187474 IC50 = 520.0 nM 6.28
CHEMBL186500 IC50 = 600.0 nM 6.22
CHEMBL187245 IC50 = 860.0 nM 6.07
CHEMBL435102 IC50 = 1100.0 nM 5.96
CHEMBL185168 IC50 = 1100.0 nM 5.96
CHEMBL363126 IC50 = 1300.0 nM 5.89
CHEMBL186743 IC50 = 1600.0 nM 5.80
CHEMBL187141 IC50 = 1600.0 nM 5.80
CHEMBL187852 IC50 = 2600.0 nM 5.58
CHEMBL426975 IC50 = 2700.0 nM 5.57
CHEMBL364643 IC50 = 2900.0 nM 5.54
CHEMBL436277 IC50 = 7800.0 nM 5.11