Assay Detail

CHEMBL5680954

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Binding

Inhibition of human N-terminal his tagged phosphorylated native ABL1 (229 to 499 residues) expressed in Sf9 cells using ABLtide as substrate preincubated for 2 hrs followed by ATP addition and measured every 2 mins for 2.5 hrs by spectrophotometric analysis

ChEMBL ↗

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Target

Tyrosine-protein kinase ABL1 (CHEMBL1862) ↗

Open DB target context

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Tyrosine-protein kinase ABL1 (CHEMBL1862) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase ABL1

CHEMBL1862

Anchored from Assay target.

Protein identity Tyrosine-protein kinase ABL1

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	Sf9
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase ABL1 (CHEMBL1862) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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	4	7.91	9.15

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	MONDO:0004992
EFO_TERM	EFO_TERM	-	—	cancer

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1421	DASATINIB ANHYDROUS	4.0	1	9.15
CHEMBL1738757	REBASTINIB	2.0	1	8.70
CHEMBL255863	NILOTINIB	4.0	1	8.66
CHEMBL941	IMATINIB	4.0	1	5.11

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1421	DASATINIB ANHYDROUS	IC50	=	0.7	nM	9.15
CHEMBL1738757	REBASTINIB	IC50	=	2.0	nM	8.70
CHEMBL255863	NILOTINIB	IC50	=	2.2	nM	8.66
CHEMBL941	IMATINIB	IC50	=	7700.0	nM	5.11