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Assay Detail

CHEMBL4178259

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of mouse BTK assessed as decrease in anti-mouse IgD antibody stimulated BCR mediated CD69 upregulation in whole blood preincubated for 1 hr followed by antibody challenge after 4 hrs by flow cytometry
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL3259478)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis.
Thakkar M, Bhuniya D, Kaduskar R, Mengawade T, Naik K, Salunkhe V, Bhalerao A, Kurhade S, Mavinahalli J, Jain V, Petla R, Avaragolla S, Ray S, Rouduri S, Dhanave A, De S, Pathade V, Tambe A, Raje AA, Madgula V, Joshi S, Nadeem A, Bala M, Umrani D, Hariharan N, Kulkarni B, Mookhtiar KA.
Bioorg Med Chem Lett (2017) 27 : 1867 -1873
PubMed 28279528 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.62 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3967108 1 6.80
CHEMBL3966346 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3967108 IC50 = 159.0 nM 6.80
CHEMBL3966346 IC50 = 364.0 nM 6.44