Assay Detail

CHEMBL3578500

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Binding

Competitive binding affinity to ZAK in human A375 cells after 15 mins in presence of ATP analogue

ChEMBL ↗

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Target

Mitogen-activated protein kinase kinase kinase 20 (CHEMBL3886) ↗

Open DB target context

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Mitogen-activated protein kinase kinase kinase 20 (CHEMBL3886) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Mitogen-activated protein kinase kinase kinase 20

CHEMBL3886

Anchored from Assay target.

Protein identity Mitogen-activated protein kinase kinase kinase 20

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase kinase kinase 20 (CHEMBL3886) ↗

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	7.41	7.41

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3577124	LY-3009120	1.0	1	7.41

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3577124	LY-3009120	IC50	=	39.0	nM	7.41