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Assay Detail

CHEMBL4605822

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

Binding
Inhibition of TRKC (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability incubated for 48 hrs by brightglo-luciferase reporter gene assay
3
Total Activities
3
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

NT-3 growth factor receptor (CHEMBL5608)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Efficacy and Tolerability of Pyrazolo[1,5-<i>a</i>]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma.
Mathison CJN, Chianelli D, Rucker PV, Nelson J, Roland J, Huang Z, Yang Y, Jiang 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 (2020) 11 : 558 -565
PubMed 32292564 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.08 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4636995 1 6.30
CHEMBL4634073 1 5.85
CHEMBL4640601 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4636995 IC50 = 500.0 nM 6.30
CHEMBL4634073 IC50 = 1400.0 nM 5.85
CHEMBL4640601 IC50 > 11000.0 nM -