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Assay Detail

CHEMBL3578499

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

Binding
Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A-375
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Ephrin type-A receptor 2 (CHEMBL2068)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL.
J Med Chem (2015) 58 : 4165 -4179
PubMed 25965804 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.70 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3577124 LY-3009120 1.0 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3577124 LY-3009120 IC50 = 20.0 nM 7.70