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Assay Detail

CHEMBL2016221

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

Functional
Antiangiogenic activity in rat aortic rings assessed as inhibition of peak phase microvessel growth
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 1 — Organism
Curated By Autocuration

Target

Aorta (CHEMBL613606)
Type TISSUE
Organism Rattus norvegicus

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
Activity 1 - -
EC50 1 8.40 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2010872 CEP-11981 2.0 2 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2010872 CEP-11981 EC50 = 4.0 nM 8.40
CHEMBL2010872 CEP-11981 Activity - -