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Assay Detail

CHEMBL5252785

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

Functional
Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

Publication

A Novel Potent Oral Series of VEGFR2 Inhibitors Abrogate Tumor Growth by Inhibiting Angiogenesis.
Bold G, Schnell C, Furet P, McSheehy P, Brüggen J, Mestan J, Manley PW, Drückes P, Burglin M, Dürler U, Loretan J, Reuter R, Wartmann M, Theuer A, Bauer-Probst B, Martiny-Baron G, Allegrini P, Goepfert A, Wood J, Littlewood-Evans A.
J Med Chem (2016) 59 : 132 -146
PubMed 26629594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.91 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5288744 1 8.70
CHEMBL4080062 BFH-772 2.0 1 8.70
CHEMBL4104297 1 8.40
CHEMBL5280119 1 8.30
CHEMBL5276611 1 8.05
CHEMBL153843 1 7.89
CHEMBL1336 SORAFENIB 4.0 1 7.85
CHEMBL75232 1 6.67
CHEMBL535 SUNITINIB 4.0 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5288744 IC50 = 2.0 nM 8.70
CHEMBL4080062 BFH-772 IC50 = 2.0 nM 8.70
CHEMBL4104297 IC50 = 4.0 nM 8.40
CHEMBL5280119 IC50 = 5.0 nM 8.30
CHEMBL5276611 IC50 = 9.0 nM 8.05
CHEMBL153843 IC50 = 13.0 nM 7.89
CHEMBL1336 SORAFENIB IC50 = 14.0 nM 7.85
CHEMBL75232 IC50 = 215.0 nM 6.67
CHEMBL535 SUNITINIB IC50 = 238.0 nM 6.62