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Assay Detail

CHEMBL711201

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

Binding
Inhibitory activity against human stromelysin-3 (MMP-3)
25
Total Activities
25
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

Inhibition of matrix metalloproteinases by N-carboxyalkyl dipeptides: Enhanced potency and selectivity with substituted P1 homophenylalanines
Sahoo SP, Caldwell CG, Chapman KT, Durette PL, Esser CK, Kopka IE, Polo SA, Sperow KM, Niedzwiecki LM, Izquierdo-Martin M, Chang BC, Harrison RK, Stein RL, MacCoss M, Hagmann WK
Bioorg Med Chem Lett (1995) 5 : 2441 -2446
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.62 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8474 1 7.75
CHEMBL251482 1 7.48
CHEMBL249449 1 7.44
CHEMBL81270 1 7.37
CHEMBL310438 1 7.14
CHEMBL310834 1 6.96
CHEMBL81264 1 6.75
CHEMBL78081 1 6.72
CHEMBL310767 1 6.72
CHEMBL310118 1 6.66
CHEMBL310823 1 6.66
CHEMBL400163 1 6.66
CHEMBL81672 1 6.64
CHEMBL251481 1 6.64
CHEMBL312649 1 6.48
CHEMBL8494 L-696418 1 6.33
CHEMBL310587 1 6.08
CHEMBL309247 1 5.80
CHEMBL311324 1 5.75
CHEMBL81014 1 5.75
CHEMBL80102 1 5.33
CHEMBL79712 1 -
CHEMBL78919 1 -
CHEMBL84031 1 -
CHEMBL78598 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8474 Ki = 18.0 nM 7.75
CHEMBL251482 Ki = 33.0 nM 7.48
CHEMBL249449 Ki = 36.0 nM 7.44
CHEMBL81270 Ki = 43.0 nM 7.37
CHEMBL310438 Ki = 72.0 nM 7.14
CHEMBL310834 Ki = 110.0 nM 6.96
CHEMBL81264 Ki = 180.0 nM 6.75
CHEMBL78081 Ki = 190.0 nM 6.72
CHEMBL310767 Ki = 190.0 nM 6.72
CHEMBL310118 Ki = 220.0 nM 6.66
CHEMBL310823 Ki = 220.0 nM 6.66
CHEMBL400163 Ki = 220.0 nM 6.66
CHEMBL81672 Ki = 230.0 nM 6.64
CHEMBL251481 Ki = 230.0 nM 6.64
CHEMBL312649 Ki = 330.0 nM 6.48
CHEMBL8494 L-696418 Ki = 470.0 nM 6.33
CHEMBL310587 Ki = 830.0 nM 6.08
CHEMBL309247 Ki = 1600.0 nM 5.80
CHEMBL311324 Ki = 1800.0 nM 5.75
CHEMBL81014 Ki = 1800.0 nM 5.75
CHEMBL80102 Ki = 4700.0 nM 5.33
CHEMBL79712 Ki > 10000.0 nM -
CHEMBL78919 Ki > 10000.0 nM -
CHEMBL84031 Ki > 10000.0 nM -
CHEMBL78598 Ki > 10000.0 nM -