Assay Detail

CHEMBL3242605

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

Functional

Antiproliferative activity against human U937 cells assessed as incorporation of [3H]thymidine into DNA after 72 hrs by beta-plate counting analysis

ChEMBL ↗

Free Research Context This assay will appear in recent viewed items on this browser. Open the demo workspace to preview project-only review queues.

Research home Demo workspace

Target

U-937 (CHEMBL612794) ↗

Open DB target context

Use one target anchor to keep assay intent, target linkage, and tested compound review aligned.

Loading context

U-937 (CHEMBL612794) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target U-937

CHEMBL612794

Anchored from Assay target.

Protein identity U-937

Disease frame Disease evidence pending

Open the live target snapshot or evidence card before reviewing assay metadata so target fit and disease framing stay reusable.

Review focus Open DB context pending

Open the live target snapshot before relying on this target frame across surface handoff.

Open target snapshot Open evidence card Search with this context

Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Functional
Organism	Homo sapiens
Cell Type	U-937
Confidence	1 — Organism
Curated By	Autocuration

Target

U-937 (CHEMBL612794) ↗

Type	CELL-LINE
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	3	7.07	7.28

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3237719	—	—	1	7.28
CHEMBL189963	PALBOCICLIB	4.0	1	6.85
CHEMBL1336	SORAFENIB	4.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3237719	—	IC50	=	52.0	nM	7.28
CHEMBL189963	PALBOCICLIB	IC50	=	140.0	nM	6.85
CHEMBL1336	SORAFENIB	IC50	>	3000.0	nM	-