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Assay Detail

CHEMBL5133804

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

Functional
Inhibition of CD69 expression on CD19 positive B cells in anti-IgD stimulated human whole blood
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Cell Type CD19 positive B cell
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Optimization of a novel piperazinone series as potent selective peripheral covalent BTK inhibitors.
Ma B, Metrick CM, Gu C, Hoemberger M, Bajrami B, Bame E, Huang J, Mingueneau M, Murugan P, Santoro JC, Tang H, Wang T, Hopkins BT.
Bioorg Med Chem Lett (2022) 60 : 128549 -128549
PubMed 35041943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.35 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5188786 1 7.52
CHEMBL4483575 REMIBRUTINIB 3.0 1 7.44
CHEMBL5186635 1 6.89
CHEMBL5197765 1 6.89
CHEMBL5197926 1 6.80
CHEMBL5188750 1 6.52
CHEMBL5173641 1 6.52
CHEMBL5170448 1 6.44
CHEMBL5180944 1 6.20
CHEMBL5172575 1 6.05
CHEMBL5189311 1 6.04
CHEMBL5182804 1 5.97
CHEMBL5204339 1 5.97
CHEMBL5179299 1 5.70
CHEMBL5207401 1 5.36
CHEMBL5207026 1 5.33
CHEMBL5207396 1 -
CHEMBL5188545 1 -
CHEMBL5206619 1 -
CHEMBL5191642 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5188786 IC50 = 30.0 nM 7.52
CHEMBL4483575 REMIBRUTINIB IC50 = 36.0 nM 7.44
CHEMBL5186635 IC50 = 130.0 nM 6.89
CHEMBL5197765 IC50 = 130.0 nM 6.89
CHEMBL5197926 IC50 = 160.0 nM 6.80
CHEMBL5188750 IC50 = 300.0 nM 6.52
CHEMBL5173641 IC50 = 300.0 nM 6.52
CHEMBL5170448 IC50 = 360.0 nM 6.44
CHEMBL5180944 IC50 = 630.0 nM 6.20
CHEMBL5172575 IC50 = 890.0 nM 6.05
CHEMBL5189311 IC50 = 920.0 nM 6.04
CHEMBL5182804 IC50 = 1080.0 nM 5.97
CHEMBL5204339 IC50 = 1080.0 nM 5.97
CHEMBL5179299 IC50 = 1990.0 nM 5.70
CHEMBL5207401 IC50 = 4410.0 nM 5.36
CHEMBL5207026 IC50 = 4700.0 nM 5.33
CHEMBL5207396 IC50 > 10000.0 nM -
CHEMBL5188545 IC50 > 10000.0 nM -
CHEMBL5206619 IC50 > 10000.0 nM -
CHEMBL5191642 IC50 > 10000.0 nM -