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Assay Detail

CHEMBL4834318

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

Binding
Inhibition of human ERG expressed in CHO cells by manual patch clamp assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

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 4 5.28 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4857808 1 5.52
CHEMBL4874648 1 5.28
CHEMBL4859681 1 5.22
CHEMBL4877264 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4857808 IC50 = 3000.0 nM 5.52
CHEMBL4874648 IC50 = 5300.0 nM 5.28
CHEMBL4859681 IC50 = 6000.0 nM 5.22
CHEMBL4877264 IC50 = 7900.0 nM 5.10