Assay Detail

CHEMBL5681159

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Functional

Antiproliferative activity against native mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay

ChEMBL ↗

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Target

BaF3 (CHEMBL614524) ↗

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Primary target BaF3

CHEMBL614524

Anchored from Assay target.

Protein identity BaF3

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	Functional
Organism	Mus musculus
Cell Type	BaF3
Confidence	1 — Organism
Curated By	Autocuration

Target

BaF3 (CHEMBL614524) ↗

Type	CELL-LINE
Organism	Mus musculus

Publication

Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036.

Chan WW, Wise SC, Kaufman MD, Ahn YM, Ensinger CL, Haack T, Hood MM, Jones J, Lord JW, Lu WP, Miller D, Patt WC, Smith BD, Petillo PA, Rutkoski TJ, Telikepalli H, Vogeti L, Yao T, Chun L, Clark R, Evangelista P, Gavrilescu LC, Lazarides K, Zaleskas VM, Stewart LJ, Van Etten RA, Flynn DL.
Cancer Cell (2011) 19 : 556 -568
PubMed 21481795 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	5	8.13	9.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1421	DASATINIB ANHYDROUS	4.0	1	9.40
CHEMBL255863	NILOTINIB	4.0	1	8.68
CHEMBL1738757	REBASTINIB	2.0	1	8.27
CHEMBL941	IMATINIB	4.0	1	7.32
CHEMBL572878	TOZASERTIB	2.0	1	6.98

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1421	DASATINIB ANHYDROUS	IC50	=	0.4	nM	9.40
CHEMBL255863	NILOTINIB	IC50	=	2.1	nM	8.68
CHEMBL1738757	REBASTINIB	IC50	=	5.4	nM	8.27
CHEMBL941	IMATINIB	IC50	=	48.0	nM	7.32
CHEMBL572878	TOZASERTIB	IC50	=	104.0	nM	6.98