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Assay Detail

CHEMBL3825518

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

Binding
Inhibition of recombinant human N-terminal His-tagged cytoplasmic c-MET kinase domain (956 to 1390 residues) phosphorylation expressed in baculovirus expression system using Tyr peptide-6 substrate incubated for 1 hr in presence of ATP by Z-Lyte assay
48
Total Activities
47
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Hepatocyte growth factor receptor (CHEMBL3717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel c-Met inhibitory olive secoiridoid semisynthetic analogs for the control of invasive breast cancer.
Mohyeldin MM, Busnena BA, Akl MR, Dragoi AM, Cardelli JA, El Sayed KA.
Eur J Med Chem (2016) 118 : 299 -315
PubMed 27258622 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 5.31 6.00
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3822800 2 6.00
CHEMBL3823418 1 5.96
CHEMBL3823650 1 5.92
CHEMBL3823321 1 5.92
CHEMBL3823866 1 5.89
CHEMBL3823193 1 5.68
CHEMBL3823617 1 5.64
CHEMBL3823701 1 5.50
CHEMBL3822722 1 5.46
CHEMBL3824070 1 5.28
CHEMBL3823110 1 5.28
CHEMBL3823086 1 5.28
CHEMBL3822615 1 5.24
CHEMBL3824255 1 5.24
CHEMBL3823881 1 5.21
CHEMBL3823395 1 5.16
CHEMBL3822893 1 5.12
CHEMBL3823553 1 5.11
CHEMBL3822574 1 5.10
CHEMBL3824063 1 5.09
CHEMBL3822765 1 5.08
CHEMBL3822560 1 5.07
CHEMBL3823189 1 5.04
CHEMBL3823377 1 4.94
CHEMBL3823470 1 4.91
CHEMBL481245 1 4.89
CHEMBL2348314 TYROSOL SINAPATE 1 4.86
CHEMBL3628211 1 4.70
CHEMBL3822534 1 -
CHEMBL3823265 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3822800 IC50 = 1000.0 nM 6.00
CHEMBL3823418 IC50 = 1100.0 nM 5.96
CHEMBL3823321 IC50 = 1200.0 nM 5.92
CHEMBL3823650 IC50 = 1200.0 nM 5.92
CHEMBL3823866 IC50 = 1300.0 nM 5.89
CHEMBL3823193 IC50 = 2100.0 nM 5.68
CHEMBL3823617 IC50 = 2300.0 nM 5.64
CHEMBL3823701 IC50 = 3200.0 nM 5.50
CHEMBL3822722 IC50 = 3500.0 nM 5.46
CHEMBL3823110 IC50 = 5200.0 nM 5.28
CHEMBL3824070 IC50 = 5300.0 nM 5.28
CHEMBL3823086 IC50 = 5200.0 nM 5.28
CHEMBL3822615 IC50 = 5800.0 nM 5.24
CHEMBL3824255 IC50 = 5800.0 nM 5.24
CHEMBL3823881 IC50 = 6100.0 nM 5.21
CHEMBL3823395 IC50 = 6900.0 nM 5.16
CHEMBL3822893 IC50 = 7600.0 nM 5.12
CHEMBL3823553 IC50 = 7800.0 nM 5.11
CHEMBL3822574 IC50 = 8000.0 nM 5.10
CHEMBL3824063 IC50 = 8200.0 nM 5.09
CHEMBL3822765 IC50 = 8300.0 nM 5.08
CHEMBL3822560 IC50 = 8500.0 nM 5.07
CHEMBL3823189 IC50 = 9100.0 nM 5.04
CHEMBL3823377 IC50 = 11400.0 nM 4.94
CHEMBL3823470 IC50 = 12200.0 nM 4.91
CHEMBL481245 IC50 = 12900.0 nM 4.89
CHEMBL2348314 TYROSOL SINAPATE IC50 = 13700.0 nM 4.86
CHEMBL3628211 IC50 = 20200.0 nM 4.70
CHEMBL3823683 IC50 > 20000.0 nM -
CHEMBL53566 TYROSOL IC50 > 20000.0 nM -
CHEMBL3823869 IC50 > 20000.0 nM -
CHEMBL3823463 IC50 > 20000.0 nM -
CHEMBL3823770 IC50 > 20000.0 nM -
CHEMBL226587 TRANS-N-SINAPOYLTYRAMINE IC50 > 20000.0 nM -
CHEMBL3823033 IC50 > 20000.0 nM -
CHEMBL3823074 IC50 > 20000.0 nM -
CHEMBL3823987 IC50 > 20000.0 nM -
CHEMBL3822697 IC50 > 20000.0 nM -
CHEMBL3822508 IC50 > 20000.0 nM -
CHEMBL3822598 IC50 > 20000.0 nM -
CHEMBL3823804 IC50 > 20000.0 nM -
CHEMBL3822690 IC50 > 20000.0 nM -
CHEMBL3822833 IC50 > 20000.0 nM -
CHEMBL3822800 Inhibition - % -
CHEMBL3823265 IC50 > 20000.0 nM -
CHEMBL3822534 IC50 > 20000.0 nM -
CHEMBL3823769 IC50 > 20000.0 nM -
CHEMBL3823798 IC50 > 20000.0 nM -