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Assay Detail

CHEMBL5735989

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

Binding
Kinase Lanthascreen Binding Assay: A BTK kinase lanthascreen binding assay monitors compound binding to unphosphorylated-BTK kinase domain (UP-BTK), by competing with a fluorescent labeled tracer. UP-BTK, consisting of the kinase domain of non-phosphorylated BTK protein (389-659aa), was produced in a Baculovirus/insect cell expression system. Into a 384-well plate, 2 ng of GST-tagged human BTK (389-659aa) was incubated with compound, 50 nM of Tracer 236 and 2 nM anti-GST antibody for 60 minutes using an optimized Lanthascreen assay. After 60 minutes, plates were read at 340 nM and 615/665 nM in an Infinite F500 (Tecan).
ChEMBL ↗
2811
Total Activities
785
Compounds Tested
3
Activity Types
0
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

Inhibitors of Bruton's tyrosine kinase and methods of their use
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 937 6.87 8.40
kon 937 - -
k_off 937 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5775653 — — 6 8.40
CHEMBL5774785 — — 9 8.30
CHEMBL5874983 — — 3 8.30
CHEMBL5957494 — — 6 8.20
CHEMBL5209441 — — 6 8.20
CHEMBL5936852 — — 3 8.20
CHEMBL5877855 — — 3 8.20
CHEMBL5963061 — — 3 8.20
CHEMBL5171216 — — 3 8.20
CHEMBL5923752 — — 3 8.20
CHEMBL5208792 — — 6 8.20
CHEMBL5930933 — — 3 8.20
CHEMBL4854911 — — 3 8.10
CHEMBL5925938 — — 3 8.10
CHEMBL5875002 — — 3 8.10
CHEMBL5741340 — — 3 8.10
CHEMBL5777190 — — 3 8.10
CHEMBL5188975 — — 12 8.10
CHEMBL5197092 — — 9 8.10
CHEMBL5181715 — — 9 8.10
CHEMBL5757279 — — 3 8.10
CHEMBL5858516 — — 3 8.10
CHEMBL5812313 — — 3 8.10
CHEMBL5821687 — — 3 8.10
CHEMBL5807681 — — 6 8.10
CHEMBL4853403 — — 15 8.10
CHEMBL5779977 — — 6 8.10
CHEMBL4851021 — — 9 8.10
CHEMBL5747624 — — 6 8.00
CHEMBL5763998 — — 6 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5775653 — IC50 = 3.98 nM 8.40
CHEMBL5774785 — IC50 = 5.01 nM 8.30
CHEMBL5874983 — IC50 = 5.01 nM 8.30
CHEMBL5208792 — IC50 = 6.31 nM 8.20
CHEMBL5774785 — IC50 = 6.31 nM 8.20
CHEMBL5963061 — IC50 = 6.31 nM 8.20
CHEMBL5877855 — IC50 = 6.31 nM 8.20
CHEMBL5936852 — IC50 = 6.31 nM 8.20
CHEMBL5923752 — IC50 = 6.31 nM 8.20
CHEMBL5171216 — IC50 = 6.31 nM 8.20
CHEMBL5957494 — IC50 = 6.31 nM 8.20
CHEMBL5930933 — IC50 = 6.31 nM 8.20
CHEMBL5209441 — IC50 = 6.31 nM 8.20
CHEMBL5812313 — IC50 = 7.94 nM 8.10
CHEMBL5858516 — IC50 = 7.94 nM 8.10
CHEMBL5821687 — IC50 = 7.94 nM 8.10
CHEMBL5188975 — IC50 = 7.94 nM 8.10
CHEMBL4854911 — IC50 = 7.94 nM 8.10
CHEMBL4853403 — IC50 = 7.94 nM 8.10
CHEMBL5807681 — IC50 = 7.94 nM 8.10
CHEMBL5777190 — IC50 = 7.94 nM 8.10
CHEMBL5925938 — IC50 = 7.94 nM 8.10
CHEMBL4851021 — IC50 = 7.94 nM 8.10
CHEMBL5181715 — IC50 = 7.94 nM 8.10
CHEMBL5741340 — IC50 = 7.94 nM 8.10
CHEMBL5197092 — IC50 = 7.94 nM 8.10
CHEMBL5779977 — IC50 = 7.94 nM 8.10
CHEMBL5757279 — IC50 = 7.94 nM 8.10
CHEMBL5875002 — IC50 = 7.94 nM 8.10
CHEMBL5879884 — IC50 = 10.0 nM 8.00
CHEMBL5948627 — IC50 = 10.0 nM 8.00
CHEMBL5745475 — IC50 = 10.0 nM 8.00
CHEMBL6024079 — IC50 = 10.0 nM 8.00
CHEMBL5839419 — IC50 = 10.0 nM 8.00
CHEMBL5777162 — IC50 = 10.0 nM 8.00
CHEMBL6057149 — IC50 = 10.0 nM 8.00
CHEMBL5960620 — IC50 = 10.0 nM 8.00
CHEMBL5942476 — IC50 = 10.0 nM 8.00
CHEMBL5763207 — IC50 = 10.0 nM 8.00
CHEMBL5992379 — IC50 = 10.0 nM 8.00
CHEMBL5881717 — IC50 = 10.0 nM 8.00
CHEMBL5763998 — IC50 = 10.0 nM 8.00
CHEMBL5744684 — IC50 = 10.0 nM 8.00
CHEMBL5856608 — IC50 = 10.0 nM 8.00
CHEMBL6054418 — IC50 = 10.0 nM 8.00
CHEMBL5747624 — IC50 = 10.0 nM 8.00
CHEMBL5934435 — IC50 = 10.0 nM 8.00
CHEMBL6035526 — IC50 = 12.6 nM 7.90
CHEMBL6038385 — IC50 = 12.6 nM 7.90
CHEMBL5777981 — IC50 = 12.6 nM 7.90