Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3270595

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

Binding
Inhibition of full length human wild type his-tagged BTK expressed in Sf9 cells using biotinylated peptide as substrate after 1 hr by Fluorescence assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
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 BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
Shi Q, Tebben A, Dyckman AJ, Li H, Liu C, Lin J, Spergel S, Burke JR, McIntyre KW, Olini GC, Strnad J, Surti N, Muckelbauer JK, Chang C, An Y, Cheng L, Ruan Q, Leftheris K, Carter PH, Tino J, De Lucca GV.
Bioorg Med Chem Lett (2014) 24 : 2206 -2211
PubMed 24685542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.06 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3263640 1 8.10
CHEMBL3263634 1 7.77
CHEMBL3263656 1 7.75
CHEMBL3263639 1 7.72
CHEMBL3263632 1 7.60
CHEMBL3263648 1 7.58
CHEMBL3263658 1 7.57
CHEMBL3263633 1 7.55
CHEMBL3263649 1 7.50
CHEMBL3263646 1 7.48
CHEMBL3263655 1 7.46
CHEMBL3263628 1 7.42
CHEMBL3263659 1 7.39
CHEMBL3263636 1 7.37
CHEMBL3263650 1 7.32
CHEMBL3263657 1 7.31
CHEMBL3263631 1 7.19
CHEMBL3263647 1 7.19
CHEMBL3263314 1 7.17
CHEMBL3263654 1 7.11
CHEMBL3263651 1 7.08
CHEMBL3263637 1 7.06
CHEMBL3263653 1 6.96
CHEMBL3263638 1 6.90
CHEMBL3263642 1 6.85
CHEMBL3263635 1 6.84
CHEMBL3263313 1 6.82
CHEMBL3263652 1 6.77
CHEMBL3263641 1 6.77
CHEMBL3263629 1 6.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3263640 IC50 = 8.0 nM 8.10
CHEMBL3263634 IC50 = 17.0 nM 7.77
CHEMBL3263656 IC50 = 18.0 nM 7.75
CHEMBL3263639 IC50 = 19.0 nM 7.72
CHEMBL3263632 IC50 = 25.0 nM 7.60
CHEMBL3263648 IC50 = 26.0 nM 7.58
CHEMBL3263658 IC50 = 27.0 nM 7.57
CHEMBL3263633 IC50 = 28.0 nM 7.55
CHEMBL3263649 IC50 = 32.0 nM 7.50
CHEMBL3263646 IC50 = 33.0 nM 7.48
CHEMBL3263655 IC50 = 35.0 nM 7.46
CHEMBL3263628 IC50 = 38.0 nM 7.42
CHEMBL3263659 IC50 = 41.0 nM 7.39
CHEMBL3263636 IC50 = 43.0 nM 7.37
CHEMBL3263650 IC50 = 48.0 nM 7.32
CHEMBL3263657 IC50 = 49.0 nM 7.31
CHEMBL3263631 IC50 = 64.0 nM 7.19
CHEMBL3263647 IC50 = 65.0 nM 7.19
CHEMBL3263314 IC50 = 67.0 nM 7.17
CHEMBL3263654 IC50 = 77.0 nM 7.11
CHEMBL3263651 IC50 = 83.0 nM 7.08
CHEMBL3263637 IC50 = 87.0 nM 7.06
CHEMBL3263653 IC50 = 109.0 nM 6.96
CHEMBL3263638 IC50 = 126.0 nM 6.90
CHEMBL3263642 IC50 = 140.0 nM 6.85
CHEMBL3263635 IC50 = 143.0 nM 6.84
CHEMBL3263313 IC50 = 150.0 nM 6.82
CHEMBL3263641 IC50 = 170.0 nM 6.77
CHEMBL3263652 IC50 = 169.0 nM 6.77
CHEMBL3263629 IC50 = 213.0 nM 6.67
CHEMBL3263630 IC50 = 574.0 nM 6.24
CHEMBL3263645 IC50 = 970.0 nM 6.01
CHEMBL3263315 IC50 = 12700.0 nM 4.90
CHEMBL3263644 IC50 = 29000.0 nM 4.54
CHEMBL3263643 IC50 > 50000.0 nM -
CHEMBL3263317 IC50 > 50000.0 nM -
CHEMBL3263316 IC50 > 50000.0 nM -