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Assay Detail

CHEMBL4767017

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Binding
Inhibition of recombinant human TRKA (440 to end residues) using KKKSPGEYVNIEFG as substrate incubated for 40 mins in presence of [gamma33P]ATP by scintillation counting based radiometry assay
1
Total Activities
1
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

Target

High affinity nerve growth factor receptor (CHEMBL2815)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structural optimization and structure-activity relationship studies of N-phenyl-7,8-dihydro-6H-pyrimido[5,4-b][1,4]oxazin-4-amine derivatives as a new class of inhibitors of RET and its drug resistance mutants.
Yang J,Chen K,Zhang G,Yang QY,Li YS,Huang SZ,Wang YL,Yang W,Jiang XJ,Yan HX,Zhu JQ,Xiang R,Luo YF,Li WM,Wei YQ,Li LL,Yang SY
Eur J Med Chem (2018) 143 : 1148 -1164
PubMed 29133048 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.15 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4793380 1 7.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4793380 IC50 = 71.0 nM 7.15