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Assay Detail

CHEMBL827914

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

Binding
Inhibitory concentration against Matrix metalloprotease-1 (MMP-1)
16
Total Activities
16
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 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13.
Noe MC, Natarajan V, Snow SL, Mitchell PG, Lopresti-Morrow L, Reeves LM, Yocum SA, Carty TJ, Barberia JA, Sweeney FJ, Liras JL, Vaughn M, Hardink JR, Hawkins JM, Tokar C.
Bioorg Med Chem Lett (2005) 15 : 2808 -2811
PubMed 15911259 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.23 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370312 1 7.00
CHEMBL190506 1 6.77
CHEMBL191359 1 6.70
CHEMBL190415 1 6.59
CHEMBL189975 1 6.54
CHEMBL179552 1 6.37
CHEMBL372878 1 6.23
CHEMBL189216 1 6.17
CHEMBL190563 1 6.16
CHEMBL372261 1 6.15
CHEMBL192773 1 6.11
CHEMBL189052 1 6.10
CHEMBL190686 1 5.96
CHEMBL189156 1 5.82
CHEMBL190441 1 5.64
CHEMBL191030 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370312 IC50 = 100.0 nM 7.00
CHEMBL190506 IC50 = 170.0 nM 6.77
CHEMBL191359 IC50 = 198.0 nM 6.70
CHEMBL190415 IC50 = 255.0 nM 6.59
CHEMBL189975 IC50 = 290.0 nM 6.54
CHEMBL179552 IC50 = 430.0 nM 6.37
CHEMBL372878 IC50 = 592.0 nM 6.23
CHEMBL189216 IC50 = 679.0 nM 6.17
CHEMBL190563 IC50 = 690.0 nM 6.16
CHEMBL372261 IC50 = 715.0 nM 6.15
CHEMBL192773 IC50 = 773.0 nM 6.11
CHEMBL189052 IC50 = 790.0 nM 6.10
CHEMBL190686 IC50 = 1100.0 nM 5.96
CHEMBL189156 IC50 = 1500.0 nM 5.82
CHEMBL190441 IC50 = 2300.0 nM 5.64
CHEMBL191030 IC50 = 5100.0 nM 5.29