Assay Detail
Binding
CHEMBL4024931
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human N-terminal His tagged BKT expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr)4:1 as substrate pretreated for 60 mins followed by substrate addition after 1 hr by ADP-Glo luminescence assay
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of N-(3-(5-((3-acrylamido-4-(morpholine-4-carbonyl)phenyl)amino)-1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-2-methylphenyl)-4-(tert-butyl)benzamide (CHMFL-BTK-01) as a highly selective irreversible Bruton's tyrosine kinase (BTK) inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 6.88 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085868 | — | — | 1 | 8.24 |
| CHEMBL4077123 | — | — | 1 | 8.15 |
| CHEMBL3301625 | SPEBRUTINIB | 2.0 | 1 | 8.05 |
| CHEMBL2216827 | — | — | 1 | 8.02 |
| CHEMBL4077064 | — | — | 1 | 7.92 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.92 |
| CHEMBL4096207 | — | — | 1 | 7.78 |
| CHEMBL4074840 | — | — | 1 | 7.72 |
| CHEMBL4076543 | — | — | 1 | 7.68 |
| CHEMBL4088999 | — | — | 1 | 7.68 |
| CHEMBL3290142 | — | — | 1 | 7.60 |
| CHEMBL4059850 | — | — | 1 | 7.50 |
| CHEMBL4066223 | — | — | 1 | 7.47 |
| CHEMBL4101519 | — | — | 1 | 7.39 |
| CHEMBL4067226 | — | — | 1 | 7.24 |
| CHEMBL4077618 | — | — | 1 | 7.20 |
| CHEMBL4066966 | — | — | 1 | 7.19 |
| CHEMBL4071818 | — | — | 1 | 7.17 |
| CHEMBL4064326 | — | — | 1 | 7.12 |
| CHEMBL4093610 | — | — | 1 | 7.07 |
| CHEMBL4088485 | — | — | 1 | 7.05 |
| CHEMBL4074645 | — | — | 1 | 6.94 |
| CHEMBL4076040 | — | — | 1 | 6.90 |
| CHEMBL4081428 | — | — | 1 | 6.79 |
| CHEMBL4105457 | — | — | 1 | 6.73 |
| CHEMBL4093800 | — | — | 1 | 6.71 |
| CHEMBL4081768 | — | — | 1 | 6.68 |
| CHEMBL4063526 | — | — | 1 | 6.64 |
| CHEMBL4103674 | — | — | 1 | 6.61 |
| CHEMBL4094515 | — | — | 1 | 6.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085868 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4077123 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3301625 | SPEBRUTINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL2216827 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL4077064 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1873475 | IBRUTINIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4096207 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL4074840 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4076543 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4088999 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3290142 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4059850 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4066223 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4101519 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4067226 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4077618 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4066966 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4071818 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4064326 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4093610 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4088485 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4074645 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL4076040 | — | IC50 | = | 127.0 | nM | 6.90 |
| CHEMBL4081428 | — | IC50 | = | 163.0 | nM | 6.79 |
| CHEMBL4105457 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4093800 | — | IC50 | = | 197.0 | nM | 6.71 |
| CHEMBL4081768 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4063526 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4103674 | — | IC50 | = | 244.0 | nM | 6.61 |
| CHEMBL4094515 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4071893 | — | IC50 | = | 282.0 | nM | 6.55 |
| CHEMBL4068683 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL4079595 | — | IC50 | = | 596.0 | nM | 6.22 |
| CHEMBL4069186 | — | IC50 | = | 667.0 | nM | 6.18 |
| CHEMBL4102259 | — | IC50 | = | 1191.0 | nM | 5.92 |
| CHEMBL4077998 | — | IC50 | = | 1261.0 | nM | 5.90 |
| CHEMBL4078155 | — | IC50 | = | 1426.0 | nM | 5.85 |
| CHEMBL4075774 | — | IC50 | = | 1697.0 | nM | 5.77 |
| CHEMBL4072911 | — | IC50 | = | 2610.0 | nM | 5.58 |
| CHEMBL4093722 | — | IC50 | = | 2946.0 | nM | 5.53 |
| CHEMBL4062079 | — | IC50 | = | 3187.0 | nM | 5.50 |
| CHEMBL4069348 | — | IC50 | = | 3736.0 | nM | 5.43 |
| CHEMBL4098885 | — | IC50 | = | 4996.0 | nM | 5.30 |
| CHEMBL4097628 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4074757 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4103968 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4066147 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4101439 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4067041 | — | IC50 | > | 10000.0 | nM | - |