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Assay Detail

CHEMBL4834294

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

Binding
Inhibition of Tel fused KDR (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation incubated for 48 hrs by cell proliferation assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3-d]pyrimidine RET Inhibitors.
Mathison CJN, Yang Y, Nelson J, Huang Z, Jiang J, Chianelli D, Rucker PV, Roland J, Xie YF, Epple R, Bursulaya B, Lee C, Gao MY, Shaffer J, Briones S, Sarkisova Y, Galkin A, Li L, Li N, Li C, Hua S, Kasibhatla S, Kinyamu-Akunda J, Kikkawa R, Molteni V, Tellew JE.
ACS Med Chem Lett (2021) 12 : 1912 -1919
PubMed 34917254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.87 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4857808 1 6.36
CHEMBL4874648 1 6.18
CHEMBL4853155 1 6.12
CHEMBL4859681 1 6.10
CHEMBL4877264 1 6.08
CHEMBL4855562 1 5.19
CHEMBL4854822 1 5.06
CHEMBL4848347 1 -
CHEMBL4864386 1 -
CHEMBL4860822 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4857808 IC50 = 440.0 nM 6.36
CHEMBL4874648 IC50 = 660.0 nM 6.18
CHEMBL4853155 IC50 = 760.0 nM 6.12
CHEMBL4859681 IC50 = 800.0 nM 6.10
CHEMBL4877264 IC50 = 840.0 nM 6.08
CHEMBL4855562 IC50 = 6500.0 nM 5.19
CHEMBL4854822 IC50 = 8700.0 nM 5.06
CHEMBL4848347 IC50 > 10000.0 nM -
CHEMBL4864386 IC50 > 10000.0 nM -
CHEMBL4860822 IC50 > 10000.0 nM -