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Assay Detail

CHEMBL714858

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

Binding
Ability to inhibit the matrix metalloprotease-3 by method of Knight et al using the fluorogenic peptide substrate.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality.
Fray MJ, Burslem MF, Dickinson RP.
Bioorg Med Chem Lett (2001) 11 : 567 -570
PubMed 11229773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.83 9.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL279786 BATIMASTAT 2.0 1 9.14
CHEMBL347595 1 8.36
CHEMBL350231 1 8.17
CHEMBL153914 1 8.05
CHEMBL349124 1 8.00
CHEMBL154317 1 7.89
CHEMBL421985 1 7.75
CHEMBL157112 1 7.72
CHEMBL152592 1 7.68
CHEMBL152531 1 7.66
CHEMBL153446 1 7.60
CHEMBL154551 1 7.40
CHEMBL157163 1 7.40
CHEMBL436230 1 7.32
CHEMBL20154 1 7.32
CHEMBL152855 1 7.14
CHEMBL345445 1 6.56
CHEMBL152805 1 6.39
CHEMBL152625 1 6.32
CHEMBL154215 1 6.25
CHEMBL152267 1 6.24
CHEMBL268992 1 6.20
CHEMBL349099 1 5.55
CHEMBL347594 1 5.50
CHEMBL152769 1 5.47
CHEMBL414626 1 5.30
CHEMBL541456 1 5.27
CHEMBL433934 1 5.21
CHEMBL156663 1 5.07
CHEMBL157048 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL279786 BATIMASTAT IC50 = 0.73 nM 9.14
CHEMBL347595 IC50 = 4.4 nM 8.36
CHEMBL350231 IC50 = 6.8 nM 8.17
CHEMBL153914 IC50 = 9.0 nM 8.05
CHEMBL349124 IC50 = 10.0 nM 8.00
CHEMBL154317 IC50 = 13.0 nM 7.89
CHEMBL421985 IC50 = 18.0 nM 7.75
CHEMBL157112 IC50 = 19.0 nM 7.72
CHEMBL152592 IC50 = 21.0 nM 7.68
CHEMBL152531 IC50 = 22.0 nM 7.66
CHEMBL153446 IC50 = 25.0 nM 7.60
CHEMBL154551 IC50 = 40.0 nM 7.40
CHEMBL157163 IC50 = 40.0 nM 7.40
CHEMBL436230 IC50 = 48.0 nM 7.32
CHEMBL20154 IC50 = 48.0 nM 7.32
CHEMBL152855 IC50 = 73.0 nM 7.14
CHEMBL345445 IC50 = 275.0 nM 6.56
CHEMBL152805 IC50 = 410.0 nM 6.39
CHEMBL152625 IC50 = 475.0 nM 6.32
CHEMBL154215 IC50 = 560.0 nM 6.25
CHEMBL152267 IC50 = 570.0 nM 6.24
CHEMBL268992 IC50 = 625.0 nM 6.20
CHEMBL349099 IC50 = 2800.0 nM 5.55
CHEMBL347594 IC50 = 3200.0 nM 5.50
CHEMBL152769 IC50 = 3400.0 nM 5.47
CHEMBL414626 IC50 = 5000.0 nM 5.30
CHEMBL541456 IC50 = 5350.0 nM 5.27
CHEMBL433934 IC50 = 6100.0 nM 5.21
CHEMBL156663 IC50 = 8500.0 nM 5.07
CHEMBL157048 IC50 = 10000.0 nM 5.00
CHEMBL345818 IC50 > 10000.0 nM -
CHEMBL156614 IC50 > 10000.0 nM -