Assay Detail

CHEMBL3242592

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Binding

Inhibition of FLT3 ITD mutant in human MOLM13 cells assessed as inhibition of STAT5 phosphorylation at Tyr694 after 24 hrs

ChEMBL ↗

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Target

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗

Open DB target context

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Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Receptor-type tyrosine-protein kinase FLT3

CHEMBL1974

Anchored from Assay target.

Protein identity Receptor-type tyrosine-protein kinase FLT3

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	MOLM-13
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.

Li Z, Wang X, Eksterowicz J, Gribble MW, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC.
J Med Chem (2014) 57 : 3430 -3449
PubMed 24641103 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	8.09	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1336	SORAFENIB	4.0	1	8.70
CHEMBL3237719	—	—	1	8.30
CHEMBL3237710	—	—	1	7.28
CHEMBL189963	PALBOCICLIB	4.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1336	SORAFENIB	IC50	=	2.0	nM	8.70
CHEMBL3237719	—	IC50	=	5.0	nM	8.30
CHEMBL3237710	—	IC50	=	52.0	nM	7.28
CHEMBL189963	PALBOCICLIB	IC50	>	3000.0	nM	-