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Assay Detail

CHEMBL973093

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Binding
Inhibition of KDR by cellular assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vascular endothelial growth factor receptor 2 (CHEMBL279)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J.
Proc Natl Acad Sci U S A (2007) 104 : 19936 -19941
PubMed 18077425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.98 7.66
Kd 1 9.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL535 SUNITINIB 4.0 1 9.70
CHEMBL459850 1 7.66
CHEMBL1336 SORAFENIB 4.0 1 6.30
CHEMBL509032 TAE-684 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL535 SUNITINIB Kd = 0.2 nM 9.70
CHEMBL459850 EC50 = 22.0 nM 7.66
CHEMBL1336 SORAFENIB EC50 = 500.0 nM 6.30
CHEMBL509032 TAE-684 EC50 > 1000.0 nM -