Assay Detail

CHEMBL5680958

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Binding

Inhibition of human ABL

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

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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	Homo sapiens
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

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	1	9.12	9.12

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
CHEMBL1738757	REBASTINIB	2.0	1	9.12

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1738757	REBASTINIB	IC50	=	0.75	nM	9.12