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Assay Detail

CHEMBL2016119

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

Binding
Inhibition of human TRK-A using ATP as substrate
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

Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K, Jones-Bolin S, Zhao H, Bacon ER, Mallamo JP, Ator MA, Ruggeri BA.
J Med Chem (2012) 55 : 903 -913
PubMed 22148921 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.52 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2010872 CEP-11981 2.0 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2010872 CEP-11981 IC50 = 3.0 nM 8.52