Assay Detail

CHEMBL2033404

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Binding

Inhibition of Abl1 in human HEK293 cells after 1 hr by competition binding assay

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	HEK293
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase ABL1 (CHEMBL1862) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (BRAF) V600E.

Rowbottom MW, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC, Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA, Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW.
J Med Chem (2012) 55 : 1082 -1105
PubMed 22168626 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	1	8.52	8.52

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2029988	CEP-32496	2.0	1	8.52

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2029988	CEP-32496	Kd	=	3.0	nM	8.52