Assay Detail

CHEMBL4375216

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Binding

Inhibition of BTK Cys481S mutant (unknown origin)

ChEMBL ↗

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Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

Open DB target context

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Tyrosine-protein kinase BTK (CHEMBL5251) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase BTK

CHEMBL5251

Anchored from Assay target.

Protein identity Tyrosine-protein kinase BTK

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	9 — Direct single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.

Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L.
J Med Chem (2019) 62 : 7643 -7655
PubMed 31368705 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	5.07	5.07

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4072833	EVOBRUTINIB	3.0	1	5.07
CHEMBL4553343	—	—	1	5.07

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4072833	EVOBRUTINIB	IC50	=	8600.0	nM	5.07
CHEMBL4553343	—	IC50	=	8600.0	nM	5.07