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Assay Detail

CHEMBL2344189

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

Functional
Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 1 — Organism
Curated By Autocuration

Publication

Optimization of inhibitors of the tyrosine kinase EphB4. 2. Cellular potency improvement and binding mode validation by X-ray crystallography.
Lafleur K, Dong J, Huang D, Caflisch A, Nevado C.
J Med Chem (2013) 56 : 84 -96
PubMed 23253074 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 4.99 5.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5416410 DASATINIB 4.0 1 5.65
CHEMBL2333593 1 5.30
CHEMBL2333602 1 4.90
CHEMBL2333603 1 4.84
CHEMBL2333595 1 4.83
CHEMBL2333597 1 4.74
CHEMBL566515 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5416410 DASATINIB IC50 = 2250.0 nM 5.65
CHEMBL2333593 IC50 = 4980.0 nM 5.30
CHEMBL2333602 IC50 = 12500.0 nM 4.90
CHEMBL2333603 IC50 = 14600.0 nM 4.84
CHEMBL2333595 IC50 = 14900.0 nM 4.83
CHEMBL2333597 IC50 = 18200.0 nM 4.74
CHEMBL566515 IC50 = 20200.0 nM 4.70