Assay Detail

CHEMBL5716188

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Binding

Inhibition of BCR-ABL H396P mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by methane-thiosulfonate-based CellTiter96 viability analysis

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

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	Mus musculus
Cell Type	BaF3
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants.

O'Hare T, Walters DK, Stoffregen EP, Jia T, Manley PW, Mestan J, Cowan-Jacob SW, Lee FY, Heinrich MC, Deininger MW, Druker BJ.
Cancer Res (2005) 65 : 4500 -4505
PubMed 15930265 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	7.56	9.22
IC90	2	-	-

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0000339
EFO_TERM	EFO_TERM	-	—	chronic myelogenous leukemia

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1421	DASATINIB ANHYDROUS	4.0	2	9.22
CHEMBL255863	NILOTINIB	4.0	2	7.39
CHEMBL941	IMATINIB	4.0	1	6.07

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1421	DASATINIB ANHYDROUS	IC50	=	0.6	nM	9.22
CHEMBL255863	NILOTINIB	IC50	=	41.0	nM	7.39
CHEMBL941	IMATINIB	IC50	=	850.0	nM	6.07
CHEMBL255863	NILOTINIB	IC90	=	69.0	nM	-
CHEMBL1421	DASATINIB ANHYDROUS	IC90	=	1.2	nM	-