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Assay Detail

CHEMBL4605859

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Binding
Inhibition of human ERG expressed in human embryonic kidney 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
Confidence 9 — Direct single protein target
Curated By Autocuration

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 4 5.93 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644274 1 6.30
CHEMBL4636056 1 5.55
CHEMBL4643578 1 -
CHEMBL4639022 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644274 IC50 = 500.0 nM 6.30
CHEMBL4636056 IC50 = 2800.0 nM 5.55
CHEMBL4643578 IC50 - -
CHEMBL4639022 IC50 - -